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Sunitinib (SU11248) Malate Tyrosinekinase-remmer

Name: Sunitinib (SU11248) Malate
Brand: Selleck Chemicals
SKU: S1042
Rating: 5 (171 reviews)

Cat.Nr.S1042

Sunitinib malate is een multi-target RTK-remmer die zich richt op VEGFR2 (Flk-1) en PDGFRβ met IC50 van 80 nM en 2 nM in celvrije assays, en remt ook c-Kit. Sunitinib Malate remt effectief de autofosforylering van Ire1α. Sunitinib Malate verhoogt zowel de doodreceptor als de mitochondriale-afhankelijke apoptose.

Sunitinib (SU11248) Malate PDGFR remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 532.56

Ga naar

Kwaliteitscontrole

Batch: Zuiverheid: 99.60%

99.60

Gerelateerde doelwitten	EGFR VEGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Overige PDGFR Inhibitoren	CP-673451 Orantinib (SU6668) Tyrphostin AG 1296 Trapidil PP121 AZD2932 Sennoside B Tyrphostin AG1433 Seralutinib (GB002) N-(p-Coumaroyl) Serotonin

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	PMID
3T3	Kinase Assay				Inhibition of PDGF-induced BrdU incorporation with IC50 of 0.007 μM	12646019
3T3	Growth Inhibition Assay				Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation with IC50 of 0.01 μM	12646019
3T3	Function Assay				Inhibition of Vascular endothelial growth factor receptor with IC50 of 0.05 μM	12646019
3T3	Kinase Assay		20 min	DMSO	Cellular inhibition of VEGF induced human KDR phosphorylation with IC50 of 0.022 μM	16162008
NIH3T3	Kinase Assay		20 min	DMSO	inhibit human KDR kinase expressed with IC50 of 0.018 μM	16162008
A549	Function Assay			DMSO	Inhibition of c-Met dependent HGF-induced human A549 cell migration with IC50 of 2 μM	18434145
DU145	Function Assay			DMSO	Inhibition of c-Met dependent HGF-induced human DU145 cell scattering with IC50 of 10 μM	18434145
KB3-1	Cytotoxic Assay		72 h	DMSO	Cytotoxicity against human P-gp-negative KB-3-1 cells with IC50 of 2.3 μM	19397322
KBV1	Cytotoxic Assay		72 h	DMSO	Cytotoxicity against human P-glycoprotein-expressing KBV1 cells with IC50 of 4.1 μM	19397322
A375	Cytotoxic Assay		72 h	DMSO	IC50=5.4 μM	19654408
RS4-11	Function Assay		2 h		Inhibition of FLT3 autophosphorylation with IC50 of 0.0099 μM	19654408
RS4-11	Function Assay		2 h		Inhibition of FLT3 ITD mutant autophosphorylation with IC50 of 0.034 μM	19654408
Sf9	Kinase Assay		30 min		Inhibition of GST-tagged VEGFR expressed with IC50 of 0.185 μM	19854051
Ba/F3	Growth Inhibition Assay		72 h		IC50=1.2 μM	20117004
BaPTC2	Growth Inhibition Assay		72 h		IC50=0.22 μM	20117004
Sf9	Function Assay		1 h	DMSO	Inhibition of human recombinant His-tagged RET expressed with IC50 of 1.3 μM	20117004
H4	Cytotoxic Assay	10 μM			Toxicity in human H4 cells	20350806
SF-539	Kinase Assay	333 μM	60 min	DMSO	Inhibition of PDGFRbeta phosphorylation with IC50 of 12.2 μM	20403700
U251	Kinase Assay	333 μM	60 min	DMSO	Inhibition of VEGFR2 phosphorylation with IC50 of 18.9 μM	20403700
A431	Kinase Assay				Inhibition of PDGFRbeta expressed with IC50 of 12.2 μM	20558072
A431	Kinase Assay				Inhibition of VEGFR2 expressed with IC50 of 18.9 μM	20558072
HepG2	Growth Inhibition Assay		72 h		IC50=3.81 μM	20570526
Kasumi-1	Growth Inhibition Assay		72 h		IC50=0.016 μM	20570526
RS4-11	Growth Inhibition Assay		72 h		IC50=1 μM	20570526
THP1	Growth Inhibition Assay		72 h		IC50=0.5 μM	20570526
Kasumi-1	Function Assay				Inhibition of c-Kit autophosphorylation with IC50 of 0.015 μM	20833039
A549	Growth Inhibition Assay		16 h		Antitumor activity against human A549 cells	21450463
HL60	Growth Inhibition Assay		16 h		Antitumor activity against human HL60 cells	21450463
HUVEC	Growth Inhibition Assay		16 h		Inhibition of VEGF-induced cell proliferation with IC50 of 2.75 μM	21450463
HUVEC	Growth Inhibition Assay		16 h		Inhibition of bFGF-induced cell proliferation with IC50 of 4.04 μM	21450463
IM9	Growth Inhibition Assay		16 h		Antitumor activity against human IM9 cells	21450463
K562	Growth Inhibition Assay		16 h		Antitumor activity against human K562 cells	21450463
MDA-MB-231	Growth Inhibition Assay		16 h		Antitumor activity against human MDA-MB-231 cells	21450463
H460	Cytotoxic Assay		72 h		IC50=2.7 μM	21621880
SMMC7721	Cytotoxic Assay		72 h		IC50=6.47 μM	21621880
WI38	Cytotoxic Assay		72 h		IC50=8.56 μM	21621880
HEK293	Kinase Assay	100 nM	1 h		does not inhibit VEGF-induced autophosphorylation of tyrosine 1175 residue on VEGFR2 expressed in HEK293 cells	21885287
HUVEC	Function Assay	1 μM	24 h		Antiangiogenic activity assessed as decrease in VEGF-induced cell migration	21963305
HUVEC	Function Assay	1 μM	1 h		Inhibition of ERK phosphorylation at Thr202/Tyr204 in VEGF-stimulated HUVEC	21963305
HUVEC	Function Assay	1 μM	1 h		Inhibition of eNOS phosphorylation at Ser-1172 in VEGF-stimulated HUVEC	21963305
HUVEC	Kinase Assay	1 μM	1 h		Inhibition of VEGFR2 phosphorylation at tyr-1175 in VEGF-stimulated HUVEC	21963305
HUVEC	Function Assay	1 μM	1 h		does not inhibit AKT phosphorylation at Ser-473 in VEGF-stimulated HUVEC	21963305
HL60	Cytotoxic Assay	50 μM	48 h	DMSO	IC50=15.5 μM	22019188
K562	Cytotoxic Assay	50 μM	48 h	DMSO	IC50=21.9 μM	22019188
PC3	Cytotoxic Assay	50 μM	48 h	DMSO	IC50=25.1 μM	22019188
SF-539	Kinase Assay	333 μM	60 min		Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells with IC50 of 12.2 μM	22204741
HAEC	Growth Inhibition Assay	100 μM	72 h		Antiproliferative activity against human HAEC cells expressing VEGFR with IC50 of 0.1 μM	22444679
HT-29	Growth Inhibition Assay	100 μM	72 h		Antiproliferative activity against human HT-29 cells expressing VEGFR with IC50 of 0.33 μM	22444679
MV4-11	Cytotoxic Assay		72 h		IC50=0.003 μM	22452518
HepG2	Cytotoxic Assay		48 h		IC50=13.24 μM	22483608
PC9	Cytotoxic Assay		48 h		IC50=10.97 μM	22483608
CAKI-1	Growth Inhibition Assay	100 μM	48 h	DMSO	GI50=0.63 μM	22560627
EKVX	Growth Inhibition Assay	100 μM	48 h	DMSO	GI50=7.9 μM	22560627
MCF7	Growth Inhibition Assay	100 μM	48 h	DMSO	GI51=2 μM	22560627
MDA-MB-435	Growth Inhibition Assay	100 μM	48 h	DMSO	GI52=2 μM	22560627
OVCAR3	Growth Inhibition Assay	100 μM	48 h	DMSO	GI53=3.2 μM	22560627
SNB19	Growth Inhibition Assay	100 μM	48 h	DMSO	GI54=10 μM	22560627
SW620	Growth Inhibition Assay	100 μM	48 h	DMSO	GI55=1.3 μM	22560627
TK10	Growth Inhibition Assay	100 μM	48 h	DMSO	GI56=6.3 μM	22560627
UACC257	Growth Inhibition Assay	100 μM	48 h	DMSO	GI57=4 μM	22560627
HAEC	Cytotoxic Assay	100 μM	72 h	DMSO	Cytotoxicity against VEGFR expressing HAEC with IC50 of 0.1 μM	23131541
HT-29	Cytotoxic Assay	100 μM	72 h	DMSO	Cytotoxicity against VEGFR expressing human HT-29 cells with IC50 of 0.33 μM	23131541
HCT116	Function Assay		24 h	DMSO	Antimigratory activity assessed as inhibition of cell migration	23153200
HUVEC	Function Assay	2 μM	18 h	DMSO	Antiangiogenic activity in HUVECs under hypoxic condition assessed as inhibition of tube formation	23153200
ACHN	Cytotoxic Assay		6 d		IC50=2.5 μM	23360104
A498	Cytotoxic Assay	100 μM	72 h	DMSO	IC50=4.3 μM	23489626
HUVEC	Growth Inhibition Assay	3 μM	24 h	DMSO	Antiangiogenic activity assessed as inhibition of VEGF-induced tube formation with EC50 of 0.645 μM	23583911
HUVEC	Kinase Assay	200 μM		DMSO	Inhibition of VEGFR2 phosphorylation in growth factor-stimulated HUVEC	23583911
HUVEC	Kinase Assay	200 μM		DMSO	Inhibition of VEGFR1 phosphorylation in growth factor-stimulated HUVEC	23583911
A549	Cytotoxic Assay		72 h	DMSO	IC50=2.44 μM	23602441
HCT116	Cytotoxic Assay		72 h	DMSO	IC50=4.71 μM	23602441
MCF7	Cytotoxic Assay		72 h	DMSO	IC50=6.29 μM	23602441
BGC	Growth Inhibition Assay		72 h	DMSO	IC50=4.78 μM	23999040
BxPC3	Growth Inhibition Assay		72 h	DMSO	IC50=3.63 μM	23999040
HT-29	Growth Inhibition Assay		72 h	DMSO	IC50=1.47 μM	23999040
T24	Growth Inhibition Assay		72 h	DMSO	IC50=2.44 μM	23999040
4T1	Cytotoxic Assay		72 h	DMSO	IC50=0.016 μM	24890652
MCF7	Cytotoxic Assay		72 h	DMSO	IC50=0.0271 μM	24890652
MCF7	Cytotoxic Assay		72 h	DMSO	IC50=0.0293 μM	24890652
MDA-MB-231	Cytotoxic Assay		72 h	DMSO	IC50=0.0223 μM	24890652
MDA-MB-435	Cytotoxic Assay		72 h	DMSO	IC50=0.0097 μM	24890652
MDA-MB-468	Cytotoxic Assay		72 h	DMSO	IC50=0.0061 μM	24890652
A431	Kinase Assay	10 μM	1 h	DMSO	Inhibition of EGFR with IC50 of 0.1721 μM	24890652
SH-SY5Y	Kinase Assay	10 μM	1 h	DMSO	Inhibition of PDGFRbeta with IC50 of 0.0831 μM	24890652
U251	Kinase Assay	10 μM	1 h	DMSO	Inhibition of VEGFR2 with IC50 of 0.0189 μM	24890652
Bel7402	Growth Inhibition Assay		72 h	DMSO	IC50=2.67 μM	24904961
HK2	Growth Inhibition Assay		72 h	DMSO	IC50=5.85 μM	24904961
LO2	Growth Inhibition Assay		72 h	DMSO	IC50=19.93 μM	24904961
MV4-11	Growth Inhibition Assay		48 h	DMSO	IC50=0.003 μM	24904961
NCI-H3122	Growth Inhibition Assay		72 h	DMSO	IC50=0.83 μM	24904961
NCI-H460	Growth Inhibition Assay		72 h	DMSO	IC50=4.31 μM	24904961
NCI-H526	Growth Inhibition Assay		72 h	DMSO	IC50=1.01 μM	24904961
TT	Growth Inhibition Assay		72 h	DMSO	IC50=0.04 μM	24904961
3T3	Antiproliferative assay		72 hrs		Antiproliferative activity against mouse 3T3 cells expressing human CSF1R after 72 hrs by Celltiter assay, Activity = 0.09 μM.	18694641
MV4-11	Antiproliferative assay		72 hrs		Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay, IC50 = 0.0043 μM.	19754199
HEK293	Function assay				Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay, Kd = 0.00047 μM.	19754199
FDC-P1	Function assay		48 hrs		Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay, IC50 = 0.155 μM.	20156689
primary leukemia cells	Cytotoxicity assay		72 hrs		Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.03 μM.	22221201
primary leukemia cells	Cytotoxicity assay		72 hrs		Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.03 μM.	22221201
primary leukemia cells	Cytotoxicity assay		72 hrs		Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 1.1 μM.	22221201
endothelial precursor cells	Function assay				Inhibition of endothelial cord area formation in endothelial precursor cells by CD31 cord area detection based phenotypic drug discovery based assay, IC50 = 0.0096 μM.	22409666
endothelial precursor cells	Function assay				Inhibition of cell migration in endothelial precursor cells by Oris cell migration kit based phenotypic drug discovery based assay, IC50 = 13.6 μM.	22409666
U251	Function assay		60 mins		Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA, IC50 = 18.9 μM.	22739090
U251	Function assay		60 mins		Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis, IC50 = 18.9 μM.	23375090
U251	Function assay		60 mins		Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA, IC50 = 18.9 μM.	23434139
CHO	Function assay				Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50 = 33.4 μM.	23812503
U251	Function assay				Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA, IC50 = 0.0189 μM.	24900865
MCF7	Antiproliferative assay		48 hrs		Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 10.5 μM.	25064347
HepG2	Antiproliferative assay		48 hrs		Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 13.6 μM.	25064347
CHO	Function assay				Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform, IC50 = 7.94328 μM.	25087753
CHO K1	Function assay				Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform, IC50 = 10 μM.	25087753
CHO K1	Function assay				Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50 = 15.8489 μM.	25087753
HEK293	Function assay				Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50 = 39.8107 μM.	25087753
MOLM13	Cytotoxicity assay		48 hrs		Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0177 μM.	25089810
MV4-11	Cytotoxicity assay		48 hrs		Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0243 μM.	25089810
HL60	Cytotoxicity assay		48 hrs		Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0368 μM.	25089810
THP1	Cytotoxicity assay		48 hrs		Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0457 μM.	25089810
ACHN	Cytotoxicity assay		72 hrs		Cytotoxicity against human ACHN cells after 72 hrs by MTT assay, IC50 = 2 μM.	25124114
U251	Function assay		60 min		Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0189 μM.	25882519
U251	Function assay		60 min		Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0831 μM.	25882519
A431	Function assay		60 min		Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.1721 μM.	25882519
HT-29	Cytotoxicity assay		48 hrs		Cytotoxicity against human HT-29 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 4.7 μM.	26009164
A549	Cytotoxicity assay		48 hrs		Cytotoxicity against human A549 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 7.93 μM.	26009164
SKOV3	Cytotoxicity assay		48 hrs		Cytotoxicity against human SKOV3 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 9.21 μM.	26009164
PANC1	Cytotoxicity assay		48 hrs		Cytotoxicity against human PANC1 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 14.94 μM.	26009164
HepG2	Cytotoxicity assay		48 hrs		Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 16.06 μM.	26009164
MCF7	Cytotoxicity assay		48 hrs		Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 25.41 μM.	26009164
Bel7402	Photocytotoxicity assay		5 hrs		Photocytotoxicity against human Bel7402 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay, EC50 = 11 μM.	26584085
PANC1	Photocytotoxicity assay		5 hrs		Photocytotoxicity against human PANC1 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay, EC50 = 13 μM.	26584085
SVEC4-10	Cytotoxicity assay		24 hrs		Cytotoxicity against mouse SVEC4-10 cells assessed as cell viability after 24 hrs by MTS assay, IC50 = 8 μM.	26912111
HUVEC	Antiangiogenic assay	10 uM	5 hrs		Antiangiogenic activity in human HUVEC cells assessed as angiogenesis rate at 10 uM after 5 hrs by endothelial tube formation assay relative to control	26912111
HT-29	Cytotoxicity assay				Cytotoxicity against human HT-29 cells by MTT assay, IC50 = 1.7 μM.	26920800
A549	Cytotoxicity assay				Cytotoxicity against human A549 cells by MTT assay, IC50 = 9.1 μM.	26920800
MDA-MB-435	Cytotoxicity assay				Cytotoxicity against human MDA-MB-435 cells by MTT assay, IC50 = 9.3 μM.	26920800
MV4-11	Antiproliferative assay		72 hrs		Antiproliferative activity against FLT3-ITD dependent human MV4-11 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.001 μM.	27077705
HL60	Antiproliferative assay		72 hrs		Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.001 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.002 μM.	27077705
MOLM14	Antiproliferative assay		72 hrs		Antiproliferative activity against FLT3-ITD dependent human MOLM14 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.005 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.006 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.009 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.02 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.023 μM.	27077705
GISTT1	Antiproliferative assay		72 hrs		Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.041 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.053 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.078 μM.	27077705
GIST882	Antiproliferative assay		72 hrs		Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.11 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.51 μM.	27077705
Rec1	Antiproliferative assay		72 hrs		Antiproliferative activity against human Rec1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.87 μM.	27077705
K562	Antiproliferative assay		72 hrs		Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1 μM.	27077705
KU812	Antiproliferative assay		72 hrs		Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.1 μM.	27077705
BCR-ABL dependent MEG01	Antiproliferative assay		72 hrs		Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.2 μM.	27077705
BAF3	Function assay		72 hrs		Inhibition of Tel-fused cKIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.38 μM.	27077705
U937	Antiproliferative assay		72 hrs		Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.7 μM.	27077705
GIST48B	Antiproliferative assay		72 hrs		Antiproliferative activity against human GIST48B cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.01 μM.	27077705
CHO	Antiproliferative assay		72 hrs		Antiproliferative activity against CHO cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.03 μM.	27077705
CHL	Antiproliferative assay		72 hrs		Antiproliferative activity against CHL cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.48 μM.	27077705
BAF3	Antiproliferative assay				Antiproliferative activity against mouse BAF3 cells, GI50 = 2.78 μM.	27077705
MDA-MB-231	Cytotoxicity assay		48 hrs		Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 7.4 μM.	27128173
BT549	Cytotoxicity assay		48 hrs		Cytotoxicity against human BT549 cells after 48 hrs by MTT assay, IC50 = 15.5 μM.	27128173
DU145	Cytotoxicity assay		48 hrs		Cytotoxicity against human DU145 cells after 48 hrs by MTT assay, IC50 = 16.4 μM.	27128173
PC3	Cytotoxicity assay		48 hrs		Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 19.6 μM.	27128173
RWPE1	Cytotoxicity assay		48 hrs		Cytotoxicity against human RWPE1 cells after 48 hrs by MTT assay, IC50 = 23 μM.	27128173
MCF7	Function assay	1 uM	24 hrs		Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated ERK1/2 at 1 uM incubated for 24 hrs by Western blot analysis	27176944
MCF7	Function assay	1 uM	24 hrs		Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated Raf1 at 1 uM incubated for 24 hrs by Western blot analysis	27176944
PA1	Cytotoxicity assay		48 hrs		Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 7.97 μM.	27210438
LNCAP	Cytotoxicity assay		48 hrs		Cytotoxicity against human LNCAP cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 12.61 μM.	27210438
RWPE1	Cytotoxicity assay		48 hrs		Cytotoxicity against human RWPE1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 23 μM.	27210438
MCF7	Cytotoxicity assay		48 hrs		Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 23.76 μM.	27210438
MDA-MB-231	Cytotoxicity assay		48 hrs		Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 7.44 μM.	27448916
A549	Cytotoxicity assay		48 hrs		Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 14.4 μM.	27448916
BT549	Cytotoxicity assay		48 hrs		Cytotoxicity against human BT549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 15.54 μM.	27448916
DU145	Cytotoxicity assay		48 hrs		Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 16.38 μM.	27448916
PC3	Cytotoxicity assay		48 hrs		Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 19.6 μM.	27448916
MCF7	Cytotoxicity assay		48 hrs		Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 23.8 μM.	27448916
MDA-MB-231	Cytotoxicity assay		48 hrs		Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 7.4 μM.	27639369
HeLa	Cytotoxicity assay		48 hrs		Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 10.4 μM.	27639369
PC3	Cytotoxicity assay		48 hrs		Cytotoxicity against human PC3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 12.6 μM.	27639369
A549	Cytotoxicity assay		48 hrs		Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 14.4 μM.	27639369
BT549	Cytotoxicity assay		48 hrs		Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 15.5 μM.	27639369
DU145	Cytotoxicity assay		48 hrs		Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 16.3 μM.	27639369
RWPE1	Cytotoxicity assay		48 hrs		Cytotoxicity against human RWPE1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 25.2 μM.	27639369
L02	Cytotoxicity assay		72 hrs		Cytotoxicity against human L02 cells after 72 hrs by CCK-8 assay, IC50 = 4.62 μM.	27643639
HL60	Cytotoxicity assay		72 hrs		Cytotoxicity against human HL60 cells after 72 hrs by CCK-8 assay, IC50 = 4.95 μM.	27643639
U251	Function assay		60 mins		Inhibition of VEGFR-2 in human U251 cells assessed as reduction in VEGF induced phosphorylation preincubated for 60 mins followed by VEGF addition measured after 10 mins by ELISA method, IC50 = 0.0189 μM.	27894589
SF539	Function assay		60 mins		Inhibition of PDGFR-beta in human SF539 cells assessed as reduction in PDGF-BB induced phosphorylation preincubated for 60 mins followed by PDGF-BB addition measured after 10 mins by ELISA method, IC50 = 0.0831 μM.	27894589
HuH7	Growth inhibition assay		48 hrs		Growth inhibition of human HuH7 cells after 48 hrs by MTT assay, IC50 = 3.03 μM.	27956344
HCT116	Growth inhibition assay		48 hrs		Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50 = 5.62 μM.	27956344
SW620	Growth inhibition assay		48 hrs		Growth inhibition of human SW620 cells after 48 hrs by MTT assay, IC50 = 6.25 μM.	27956344
MV4-11	Antiproliferative assay		72 hrs		Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant after 72 hrs by MTS assay, IC50 = 0.0385 μM.	28038328
CHO	Function assay				Inhibition of human ERG expressed in CHO cells by Qpatch assay, IC50 = 0.5 μM.	28038328
HepG2	Antiproliferative assay		48 hrs		Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 16.06 μM.	28057423
MCF7	Antiproliferative assay		48 hrs		Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 25.41 μM.	28057423
HEK293	Function assay		2 mins		Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay, IC50 = 6.1 μM.	28230985
RCC4	Anticancer assay		48 hrs		Anticancer activity against human RCC4 cells after 48 hrs by XTT assay, IC50 = 4 μM.	28325600
MDA-MB-231	Anticancer assay		48 hrs		Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay, IC50 = 6 μM.	28325600
COLO205	Cytotoxicity assay		24 hrs		Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay, IC50 = 8 μM.	28756024
K562	Cytotoxicity assay		24 hrs		Cytotoxicity against human K562 cells after 24 hrs by MTT assay, IC50 = 14 μM.	28756024
MDA-MB-231	Cytotoxicity assay		24 hrs		Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 32 μM.	28756024
MDA-MB-231	Cytotoxicity assay		24 hrs		Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay, IC50 = 6.98 μM.	28760313
MCF7	Function assay	4 uM	24 hrs		Inhibition of VEGFR2 phosphorylation in human MCF7 cells at 4 uM incubated for 24 hrs by Western blot method	28942113
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.04 μM.	28991465
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.09 μM.	28991465
GIST430	Cytotoxicity assay		72 hrs		Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.098 μM.	28991465
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 5.88 μM.	28991465
HuH7	Antiproliferative assay		48 hrs		Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 4.707 μM.	29057042
A498	Antiproliferative assay		48 hrs		Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 7.981 μM.	29057042
NCI-H727	Antiproliferative assay		48 hrs		Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay, IC50 = 10.12 μM.	29057042
MV4-11	Antiproliferative assay		72 hrs		Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50 = 0.01 μM.	29935772
HuH7	Antiproliferative assay				Antiproliferative activity against human HuH7 cells by MTT assay, IC50 = 3.03 μM.	30059803
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 5.62 μM.	30059803
SW620	Antiproliferative assay				Antiproliferative activity against human SW620 cells by MTT assay, IC50 = 6.25 μM.	30059803
HepG2	Antiproliferative assay				Antiproliferative activity against human HepG2 cells by MTT assay, IC50 = 7.78 μM.	30059803
U251	Function assay		60 mins		Inhibition of VEGF-induced VEGFR2 activation in human U251 cells pretreated for 60 mins followed by VEGF addition and measured after 10 mins by ELISA, IC50 = 0.0189 μM.	30098869
SH-SY5Y	Function assay		60 mins		Inhibition of PDGF-BB-induced PDGFRbeta activation in human SH-SY5Y cells pretreated for 60 mins followed by PDGF-BB addition and measured after 10 mins by ELISA, IC50 = 0.0831 μM.	30098869
A431	Function assay		60 mins		Inhibition of EGF-induced EGFR activation in human A431 cells pretreated for 60 mins followed by EGF addition and measured after 10 mins by ELISA, IC50 = 0.1721 μM.	30098869
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.004 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.005 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.006 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.007 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.007 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.012 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.024 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.027 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.03 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.214 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.271 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.398 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.43 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.584 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.631 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.638 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.696 μM.	30204441
BA/F3	Function assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.782 μM.	30204441
BA/F3	Cytotoxicity assay		72 hrs		Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 4.789 μM.	30204441
Sf21	Function assay		60 mins		Inhibition of recombinant human N-terminal His6-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells after 60 mins by ELISA, IC50 = 0.0047 μM.	30241010
EoL-1-cell	Growth Inhibition Assay				IC50=1.64 pM	SANGER
MV-4-11	Growth Inhibition Assay				IC50=272 pM	SANGER
NOS-1	Growth Inhibition Assay				IC50=15.3 nM	SANGER
CGTH-W-1	Growth Inhibition Assay				IC50=30.94 nM	SANGER
MONO-MAC-6	Growth Inhibition Assay				IC50=33.8 nM	SANGER
ALL-PO	Growth Inhibition Assay				IC50=79.89 nM	SANGER
NKM-1	Growth Inhibition Assay				IC50=98.52 nM	SANGER
KM12	Growth Inhibition Assay				IC50=350.14 nM	SANGER
TE-15	Growth Inhibition Assay				IC50=507.61 nM	SANGER
697	Growth Inhibition Assay				IC50=614.25 nM	SANGER
MOLT-16	Growth Inhibition Assay				IC50=631.32 nM	SANGER
GB-1	Growth Inhibition Assay				IC50=710.23 nM	SANGER
TE-12	Growth Inhibition Assay				IC50=804.55 nM	SANGER
ES6	Growth Inhibition Assay				IC50=981.06 nM	SANGER
LC-2-ad	Growth Inhibition Assay				IC50=1.11407 μM	SANGER
BL-70	Growth Inhibition Assay				IC50=1.11846 μM	SANGER
ETK-1	Growth Inhibition Assay				IC50=1.2858 μM	SANGER
A4-Fuk	Growth Inhibition Assay				IC50=1.34141 μM	SANGER
OCI-AML2	Growth Inhibition Assay				IC50=1.36851 μM	SANGER
SIG-M5	Growth Inhibition Assay				IC50=1.37009 μM	SANGER
NCI-SNU-16	Growth Inhibition Assay				IC50=1.46486 μM	SANGER
PSN1	Growth Inhibition Assay				IC50=1.50676 μM	SANGER
SR	Growth Inhibition Assay				IC50=1.54572 μM	SANGER
A3-KAW	Growth Inhibition Assay				IC50=1.62546 μM	SANGER
KS-1	Growth Inhibition Assay				IC50=1.69247 μM	SANGER
CTV-1	Growth Inhibition Assay				IC50=1.72751 μM	SANGER
LB1047-RCC	Growth Inhibition Assay				IC50=1.81624 μM	SANGER
EMG-01	Growth Inhibition Assay				IC50=1.83563 μM	SANGER
TE-11	Growth Inhibition Assay				IC50=1.83985 μM	SANGER
CMK	Growth Inhibition Assay				IC50=1.95517 μM	SANGER
NB1	Growth Inhibition Assay				IC50=1.96117 μM	SANGER
HAL-01	Growth Inhibition Assay				IC50=2.05946 μM	SANGER
DEL	Growth Inhibition Assay				IC50=2.08482 μM	SANGER
RL95-2	Growth Inhibition Assay				IC50=2.11137 μM	SANGER
KARPAS-299	Growth Inhibition Assay				IC50=2.11313 μM	SANGER
EW-16	Growth Inhibition Assay				IC50=2.13508 μM	SANGER
RS4-11	Growth Inhibition Assay				IC50=2.17924 μM	SANGER
BB30-HNC	Growth Inhibition Assay				IC50=2.22375 μM	SANGER
DOHH-2	Growth Inhibition Assay				IC50=2.33431 μM	SANGER
RPMI-8402	Growth Inhibition Assay				IC50=2.33618 μM	SANGER
BV-173	Growth Inhibition Assay				IC50=2.3366 μM	SANGER
TE-10	Growth Inhibition Assay				IC50=2.34384 μM	SANGER
TE-8	Growth Inhibition Assay				IC50=2.37038 μM	SANGER
K052	Growth Inhibition Assay				IC50=2.40202 μM	SANGER
KARPAS-45	Growth Inhibition Assay				IC50=2.49446 μM	SANGER
SK-NEP-1	Growth Inhibition Assay				IC50=2.60237 μM	SANGER
KGN	Growth Inhibition Assay				IC50=2.60339 μM	SANGER
ML-2	Growth Inhibition Assay				IC50=2.63512 μM	SANGER
LAMA-84	Growth Inhibition Assay				IC50=2.69545 μM	SANGER
LXF-289	Growth Inhibition Assay				IC50=2.72989 μM	SANGER
A101D	Growth Inhibition Assay				IC50=2.78304 μM	SANGER
KY821	Growth Inhibition Assay				IC50=2.79758 μM	SANGER
ES4	Growth Inhibition Assay				IC50=2.80628 μM	SANGER
SCC-3	Growth Inhibition Assay				IC50=2.82891 μM	SANGER
NALM-6	Growth Inhibition Assay				IC50=2.90473 μM	SANGER
BL-41	Growth Inhibition Assay				IC50=2.91222 μM	SANGER
OPM-2	Growth Inhibition Assay				IC50=3.05954 μM	SANGER
SF126	Growth Inhibition Assay				IC50=3.06198 μM	SANGER
BE-13	Growth Inhibition Assay				IC50=3.23111 μM	SANGER
SF268	Growth Inhibition Assay				IC50=3.32869 μM	SANGER
MOLT-4	Growth Inhibition Assay				IC50=3.39838 μM	SANGER
PF-382	Growth Inhibition Assay				IC50=3.4457 μM	SANGER
HEL	Growth Inhibition Assay				IC50=3.48005 μM	SANGER
RPMI-6666	Growth Inhibition Assay				IC50=3.54171 μM	SANGER
QIMR-WIL	Growth Inhibition Assay				IC50=3.63391 μM	SANGER
ATN-1	Growth Inhibition Assay				IC50=3.67114 μM	SANGER
BB49-HNC	Growth Inhibition Assay				IC50=3.70508 μM	SANGER
HCE-4	Growth Inhibition Assay				IC50=3.78642 μM	SANGER
SK-LMS-1	Growth Inhibition Assay				IC50=3.83338 μM	SANGER
MS-1	Growth Inhibition Assay				IC50=3.83778 μM	SANGER
JAR	Growth Inhibition Assay				IC50=3.98832 μM	SANGER
KE-37	Growth Inhibition Assay				IC50=4.06158 μM	SANGER
LB996-RCC	Growth Inhibition Assay				IC50=4.12168 μM	SANGER
HH	Growth Inhibition Assay				IC50=4.20914 μM	SANGER
HL-60	Growth Inhibition Assay				IC50=4.21065 μM	SANGER
HOP-62	Growth Inhibition Assay				IC50=4.3352 μM	SANGER
NOMO-1	Growth Inhibition Assay				IC50=4.33699 μM	SANGER
DU-4475	Growth Inhibition Assay				IC50=4.36729 μM	SANGER
LC4-1	Growth Inhibition Assay				IC50=4.3807 μM	SANGER
MC116	Growth Inhibition Assay				IC50=4.43081 μM	SANGER
SW982	Growth Inhibition Assay				IC50=4.55307 μM	SANGER
SK-N-DZ	Growth Inhibition Assay				IC50=4.67099 μM	SANGER
EW-1	Growth Inhibition Assay				IC50=4.67911 μM	SANGER
SU-DHL-1	Growth Inhibition Assay				IC50=4.80174 μM	SANGER
L-363	Growth Inhibition Assay				IC50=4.80621 μM	SANGER
OS-RC-2	Growth Inhibition Assay				IC50=4.8731 μM	SANGER
HD-MY-Z	Growth Inhibition Assay				IC50=5.17301 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay				IC50=5.32312 μM	SANGER
HC-1	Growth Inhibition Assay				IC50=5.43291 μM	SANGER
SK-MM-2	Growth Inhibition Assay				IC50=5.4782 μM	SANGER
SH-4	Growth Inhibition Assay				IC50=5.4837 μM	SANGER
MHH-CALL-2	Growth Inhibition Assay				IC50=5.76719 μM	SANGER
KG-1	Growth Inhibition Assay				IC50=6.02878 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay				IC50=6.07909 μM	SANGER
MMAC-SF	Growth Inhibition Assay				IC50=6.10949 μM	SANGER
IST-SL2	Growth Inhibition Assay				IC50=6.12519 μM	SANGER
SW954	Growth Inhibition Assay				IC50=6.27517 μM	SANGER
HDLM-2	Growth Inhibition Assay				IC50=6.32109 μM	SANGER
ST486	Growth Inhibition Assay				IC50=6.3471 μM	SANGER
DG-75	Growth Inhibition Assay				IC50=6.43069 μM	SANGER
EW-3	Growth Inhibition Assay				IC50=6.43207 μM	SANGER
8-MG-BA	Growth Inhibition Assay				IC50=6.51507 μM	SANGER
GT3TKB	Growth Inhibition Assay				IC50=6.60763 μM	SANGER
KU812	Growth Inhibition Assay				IC50=6.6942 μM	SANGER
CESS	Growth Inhibition Assay				IC50=7.10438 μM	SANGER
BC-1	Growth Inhibition Assay				IC50=7.24812 μM	SANGER
MZ1-PC	Growth Inhibition Assay				IC50=7.30389 μM	SANGER
NCI-H82	Growth Inhibition Assay				IC50=7.3785 μM	SANGER
NCI-H1355	Growth Inhibition Assay				IC50=7.45804 μM	SANGER
RPMI-8226	Growth Inhibition Assay				IC50=7.50739 μM	SANGER
ARH-77	Growth Inhibition Assay				IC50=7.53597 μM	SANGER
MN-60	Growth Inhibition Assay				IC50=7.54088 μM	SANGER
IMR-5	Growth Inhibition Assay				IC50=7054876 μM	SANGER
KARPAS-422	Growth Inhibition Assay				IC50=7.57206 μM	SANGER
CA46	Growth Inhibition Assay				IC50=7.58012 μM	SANGER
SJSA-1	Growth Inhibition Assay				IC50=7.66061 μM	SANGER
no-11	Growth Inhibition Assay				IC50=7.77557 μM	SANGER
IST-SL1	Growth Inhibition Assay				IC50=8.02417 μM	SANGER
NCI-H209	Growth Inhibition Assay				IC50=8.11652 μM	SANGER
TALL-1	Growth Inhibition Assay				IC50=8.18384 μM	SANGER
KMOE-2	Growth Inhibition Assay				IC50=8.1942 μM	SANGER
HCC1599	Growth Inhibition Assay				IC50=8.19987 μM	SANGER
CI-1	Growth Inhibition Assay				IC50=8.20411 μM	SANGER
NCI-H1304	Growth Inhibition Assay				IC50=8.20661 μM	SANGER
Daudi	Growth Inhibition Assay				IC50=8.23546 μM	SANGER
CPC-N	Growth Inhibition Assay				IC50=8.29199 μM	SANGER
MC-CAR	Growth Inhibition Assay				IC50=8.3358 μM	SANGER
SW872	Growth Inhibition Assay				IC50=8.34758 μM	SANGER
OVCAR-4	Growth Inhibition Assay				IC50=8.50351 μM	SANGER
OCUB-M	Growth Inhibition Assay				IC50=8.56508 μM	SANGER
SK-PN-DW	Growth Inhibition Assay				IC50=8.60985 μM	SANGER
NCCIT	Growth Inhibition Assay				IC50=8.71745 μM	SANGER
NCI-H1648	Growth Inhibition Assay				IC50=9.13834 μM	SANGER
COR-L279	Growth Inhibition Assay				IC50=9.3909 μM	SANGER
LS-123	Growth Inhibition Assay				IC50=9.68161 μM	SANGER
LP-1	Growth Inhibition Assay				IC50=9.78083 μM	SANGER
NB13	Growth Inhibition Assay				IC50=9.79994 μM	SANGER
ONS-76	Growth Inhibition Assay				IC50=9.81016 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay				IC50=9.99933 μM	SANGER
GR-ST	Growth Inhibition Assay				IC50=10.2207 μM	SANGER
ES1	Growth Inhibition Assay				IC50=10.2984 μM	SANGER
NB14	Growth Inhibition Assay				IC50=10.9277 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay				IC50=11.265 μM	SANGER
RXF393	Growth Inhibition Assay				IC50=11.4834 μM	SANGER
NCI-H2107	Growth Inhibition Assay				IC50=11.5984 μM	SANGER
K562	Growth Inhibition Assay				IC50=11.8702 μM	SANGER
LOUCY	Growth Inhibition Assay				IC50=11.9875 μM	SANGER
TGBC1TKB	Growth Inhibition Assay				IC50=12.002 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay				IC50=12.1565 μM	SANGER
K5	Growth Inhibition Assay				IC50=12.2985 μM	SANGER
BC-3	Growth Inhibition Assay				IC50=12.4651 μM	SANGER
REH	Growth Inhibition Assay				IC50=12.6498 μM	SANGER
NEC8	Growth Inhibition Assay				IC50=12.6887 μM	SANGER
IST-MEL1	Growth Inhibition Assay				IC50=12.8694 μM	SANGER
NCI-H128	Growth Inhibition Assay				IC50=13.0723 μM	SANGER
NCI-H1694	Growth Inhibition Assay				IC50=13.1144 μM	SANGER
TGW	Growth Inhibition Assay				IC50=13.3276 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay				IC50=13.345 μM	SANGER
IST-MES1	Growth Inhibition Assay				IC50=13.6729 μM	SANGER
CTB-1	Growth Inhibition Assay				IC50=13.7294 μM	SANGER
HUTU-80	Growth Inhibition Assay				IC50=13.7573 μM	SANGER
LAN-6	Growth Inhibition Assay				IC50=14.2457 μM	SANGER
KP-N-YS	Growth Inhibition Assay				IC50=14.2894 μM	SANGER
CCRF-CEM	Growth Inhibition Assay				IC50=14.4169 μM	SANGER
NCI-H1770	Growth Inhibition Assay				IC50=14.5369 μM	SANGER
MZ2-MEL	Growth Inhibition Assay				IC50=15.2251 μM	SANGER
COR-L88	Growth Inhibition Assay				IC50=16.0012 μM	SANGER
LOXIMVI	Growth Inhibition Assay				IC50=16.256 μM	SANGER
KALS-1	Growth Inhibition Assay				IC50=16.5931 μM	SANGER
D-283MED	Growth Inhibition Assay				IC50=16.8489 μM	SANGER
NCI-H719	Growth Inhibition Assay				IC50=16.9161 μM	SANGER
MLMA	Growth Inhibition Assay				IC50=16.9907 μM	SANGER
EVSA-T	Growth Inhibition Assay				IC50=17.0485 μM	SANGER
SK-N-FI	Growth Inhibition Assay				IC50=17.6913 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay				IC50=17.8572 μM	SANGER
NCI-H1882	Growth Inhibition Assay				IC50=17.9834 μM	SANGER
A704	Growth Inhibition Assay				IC50=17.9904 μM	SANGER
L-428	Growth Inhibition Assay				IC50=18.0151 μM	SANGER
HCC1187	Growth Inhibition Assay				IC50=18.0187 μM	SANGER
NCI-H1581	Growth Inhibition Assay				IC50=18.0866 μM	SANGER
BB65-RCC	Growth Inhibition Assay				IC50=18.4162 μM	SANGER
EM-2	Growth Inhibition Assay				IC50=18.5672 μM	SANGER
Raji	Growth Inhibition Assay				IC50=19.9565 μM	SANGER
TE-1	Growth Inhibition Assay				IC50=20.4104 μM	SANGER
SW962	Growth Inhibition Assay				IC50=20.4293 μM	SANGER
MHH-NB-11	Growth Inhibition Assay				IC50=20.5521 μM	SANGER
no-10	Growth Inhibition Assay				IC50=21.0264 μM	SANGER
GDM-1	Growth Inhibition Assay				IC50=21.9414 μM	SANGER
KMS-12-PE	Growth Inhibition Assay				IC50=22.274 μM	SANGER
NCI-H510A	Growth Inhibition Assay				IC50=24.1278 μM	SANGER
ES5	Growth Inhibition Assay				IC50=24.7349 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay				IC50=26.2742 μM	SANGER
NMC-G1	Growth Inhibition Assay				IC50=27.1822 μM	SANGER
NCI-H446	Growth Inhibition Assay				IC50=27.4946 μM	SANGER
NB7	Growth Inhibition Assay				IC50=27.9229 μM	SANGER
A388	Growth Inhibition Assay				IC50=28.0074 μM	SANGER
JVM-2	Growth Inhibition Assay				IC50=28.2898 μM	SANGER
HT-144	Growth Inhibition Assay				IC50=28.69 μM	SANGER
NCI-H747	Growth Inhibition Assay				IC50=28.9195 μM	SANGER
NCI-H1650	Growth Inhibition Assay				IC50=29.0176 μM	SANGER
EB-3	Growth Inhibition Assay				IC50=29.5309 μM	SANGER
KLE	Growth Inhibition Assay				IC50=29.619 μM	SANGER
TK10	Growth Inhibition Assay				IC50=30.126 μM	SANGER
COLO-668	Growth Inhibition Assay				IC50=30.792 μM	SANGER
NCI-H23	Growth Inhibition Assay				IC50=31.1063 μM	SANGER
GOTO	Growth Inhibition Assay				IC50=31.6085 μM	SANGER
MSTO-211H	Growth Inhibition Assay				IC50=31.8678 μM	SANGER
LB831-BLC	Growth Inhibition Assay				IC50=32.3843 μM	SANGER
SCH	Growth Inhibition Assay				IC50=32.8485 μM	SANGER
EHEB	Growth Inhibition Assay				IC50=34.1193 μM	SANGER
U-266	Growth Inhibition Assay				IC50=34.2781 μM	SANGER
EW-11	Growth Inhibition Assay				IC50=34.4725 μM	SANGER
TE-9	Growth Inhibition Assay				IC50=37.0401 μM	SANGER
ES3	Growth Inhibition Assay				IC50=37.5004 μM	SANGER
NCI-H2141	Growth Inhibition Assay				IC50=38.0843 μM	SANGER
MPP-89	Growth Inhibition Assay				IC50=42.0586 μM	SANGER
SK-MEL-2	Growth Inhibition Assay				IC50=42.6405 μM	SANGER
LC-1F	Growth Inhibition Assay				IC50=43.3682 μM	SANGER
NH-12	Growth Inhibition Assay				IC50=43.9359 μM	SANGER
RKO	Growth Inhibition Assay				IC50=44.1252 μM	SANGER
KM-H2	Growth Inhibition Assay				IC50=44.9577 μM	SANGER
SK-UT-1	Growth Inhibition Assay				IC50=49.8825 μM	SANGER
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	532.56	Formule	C₂₂H₂₇FN₄O₂.C₄H₆O₅	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	341031-54-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	SU11248 malate			Smiles	CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C.C(C(C(=O)O)O)C(=O)O

Oplosbaarheid

In vitro
Batch:

DMSO : 70 mg/mL (131.44 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	5.000mg/ml (9.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 30%PEG300 2 66%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.000mg/ml (3.76mM)	Taking the 1 mL working solution as an example, add 40 μL of 50 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	IRE1α Kit (Cell-free assay) FLT3 (Cell-free assay) PDGFRβ (Cell-free assay) 2 nM VEGFR2 (Cell-free assay) 80 nM
In vitro	Sunitinib remt ook krachtig Kit en FLT-3. Sunitinib is een krachtige ATP-competitieve remmer van VEGFR2 (Flk1) en PDGFRβ met K_i van respectievelijk 9 nM en 8 nM, en vertoont een >10-voudig hogere selectiviteit voor VEGFR2 en PDGFR dan FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl en src. In serumarme NIH-3T3-cellen die VEGFR2 of PDGFRβ tot expressie brengen, remt Sunitinib VEGF-afhankelijke VEGFR2-fosforylering en PDGF-afhankelijke PDGFRβ-fosforylering met respectievelijk IC50 van 10 nM en 10 nM. Sunitinib remt VEGF-geïnduceerde proliferatie van serumarme HUVEC's met IC50 van 40 nM, en remt PDGF-geïnduceerde proliferatie van NIH-3T3-cellen die PDGFRβ of PDGFRα overexpressen met respectievelijk IC50 van 39 nM en 69 nM. Sunitinib remt de fosforylering van wild-type FLT3, FLT3-ITD en FLT3-Asp835 met respectievelijk IC50 van 250 nM, 50 nM en 30 nM. Sunitinib remt de proliferatie van MV4;11- en OC1-AML5-cellen met respectievelijk IC50 van 8 nM en 14 nM, en induceert apoptose op een dosisafhankelijke manier.
Kinase Assay	Biochemische Tyrosinekinase-assays
Kinase Assay	IC50-waarden voor Sunitinib tegen VEGFR2 (Flk-1) en PDGFRβ worden bepaald met behulp van glutathion S-transferasefusie-eiwitten die het complete cytoplasmatische domein van de RTK bevatten. Biochemische tyrosinekinase-assays om de trans-fosforyleringsactiviteit van VEGFR2 (Flk-1) en PDGFRβ te kwantificeren, worden uitgevoerd in 96-well microtiterplaten die vooraf zijn gecoat (20 μg/well in PBS; overnacht geïncubeerd bij 4 °C) met het peptidesubstraat poly-Glu,Tyr (4:1). Overtollige eiwitbindingsplaatsen worden geblokkeerd door toevoeging van 1-5% (w/v) BSA in PBS. Gezuiverde GST-fusie-eiwitten worden geproduceerd in baculovirus-geïnfecteerde insectencellen. GST-VEGFR2 en GST-PDGFRβ worden vervolgens toegevoegd aan de microtiterwells in een 2 × concentratie kinase-verdunningsbuffer bestaande uit 100 mM HEPES, 50 mM NaCl, 40 μM NaVO₄ en 0,02% (w/v) BSA. De uiteindelijke enzymconcentratie voor GST-VEGFR2 of GST-PDGFRβ is 50 ng/mL. Vijfentwintig μL verdunde Sunitinib worden vervolgens aan elk reactievat toegevoegd om een reeks remmerconcentraties te produceren die geschikt zijn voor elk enzym. De kinasereactie wordt geïnitieerd door de toevoeging van verschillende concentraties ATP in een oplossing van MnCl₂, zodat de uiteindelijke ATP-concentraties de Km voor het enzym overspannen, en de uiteindelijke concentratie van MnCl₂ 10 mM is. De platen worden 5-15 minuten bij kamertemperatuur geïncubeerd voordat de reactie wordt gestopt door toevoeging van EDTA. De platen worden vervolgens driemaal gewassen met TBST. Konijnen polyklonale anti-fosfotyrosine-antisera worden in de wells toegevoegd in een 1:10.000 verdunning in TBST dat 0,5% (w/v) BSA, 0,025% (w/v) magere melkpoeder en 100 μM NaVO₄ bevat en 1 uur bij 37 °C geïncubeerd. De platen worden vervolgens driemaal gewassen met TBST, gevolgd door toevoeging van geit anti-konijn antisera geconjugeerd met mierikswortelperoxidase (1:10.000 verdunning in TBST). De platen worden 1 uur bij 37 °C geïncubeerd en vervolgens driemaal gewassen met TBST. De hoeveelheid fosfotyrosine in elke well wordt gekwantificeerd na toevoeging van 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] als substraat.
In vivo	In overeenstemming met de substantiële en selectieve remming van VEGFR2- of PDGFR-fosforylering en -signalering in vivo, vertoont Sunitinib (20-80 mg/kg/dag) een brede en potente dosisafhankelijke antitumoractiviteit tegen een verscheidenheid aan tumorxenograftmodellen, waaronder HT-29, A431, Colo205, H-460, SF763T, C6, A375 of MDA-MB-435. Dosis Sunitinib van 80 mg/kg/dag gedurende 21 dagen leidt tot volledige tumorregressie bij zes van de acht muizen, zonder tumorhergroei gedurende een observatieperiode van 110 dagen na het einde van de behandeling. Een tweede behandelingsronde met Sunitinib blijft effectief tegen tumoren die niet volledig zijn geregresseerd tijdens de eerste behandelingsronde. Sunitinib-behandeling resulteert in een significante afname van tumor-MVD, met ~40% reductie in SF763T-glioomtumoren. SU11248-behandeling resulteert in een volledige remming van aanvullende tumorgroei van luciferaset-expressende PC-3M-xenografts, ondanks geen afname van de tumorgrootte. Sunitinib-behandeling (20 mg/kg/dag) onderdrukt dramatisch de groei van subcutane MV4;11 (FLT3-ITD)-xenografts en verlengt de overleving in het FLT3-ITD-beenmergengraftmentmodel.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/12646019/ [2] https://pubmed.ncbi.nlm.nih.gov/12538485/ [3] https://pubmed.ncbi.nlm.nih.gov/12531805/ [4] https://pubmed.ncbi.nlm.nih.gov/14578466/ [5] https://pubmed.ncbi.nlm.nih.gov/15304385/ [6] https://pubmed.ncbi.nlm.nih.gov/17041096/ [7] https://pubmed.ncbi.nlm.nih.gov/21317875/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	p-AKT / AKT / p-ERK / ERK p-GSK3β / GSK3β / MYCN p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK		24759734
Growth inhibition assay	Cell viability		24369536

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT06222593	Not yet recruiting	Carcinoma Renal Cell	State University of New York at Buffalo	June 1 2024	Phase 1\|Phase 2
NCT06208748	Not yet recruiting	Gastrointestinal Stromal Tumors\|GIST	Sarcoma Alliance for Research through Collaboration\|Cogent Biosciences Inc.\|Dana-Farber Cancer Institute\|The Life Raft Group	March 2024	Phase 2
NCT05745142	Completed	Carcinoma Renal Cell\|Clear-cell Metastatic Renal Cell Carcinoma	Pfizer	February 23 2023	--
NCT05043090	Recruiting	Papillary Renal Cell Carcinoma	AstraZeneca	October 28 2021	Phase 3
NCT04669366	Completed	Kidney Neoplasms	Pfizer	January 20 2021	--

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

Als u nog andere vragen heeft, kunt u een bericht achterlaten.

Veelgestelde vragen

Vraag 1:
I was wondering whether it is in its cis or trans form?

Antwoord:
It is Z form.

Vraag 2:
What is the difference between it (S1042) and Sunitinib (S7781)?

Antwoord:
S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same, but their solubility in aqueous solvent differs.

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