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Saracatinib (AZD0530) Src Remmer

Name: Saracatinib (AZD0530)
Brand: Selleck Chemicals
SKU: S1006
Rating: 5 (310 reviews)

Cat.Nr.: S1006

Saracatinib (AZD0530) is een potente Src-remmer met een IC50 van 2,7 nM in celvrije assays, en is potent tegen c-Yes, Fyn, Lyn, Blk, Fgr en Lck; minder actief voor Abl en EGFR (L858R en L861Q). Het induceert autophagy en bevindt zich in Fase 2/3.

Saracatinib (AZD0530) Src Remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 542.03

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	EGFR VEGFR JAK FGFR PDGFR HIF FLT3 FLT HER2 Bcr-Abl
Overige Src Inhibitoren	WH-4-023 PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 UM-164 Tolimidone (MLR-1023) 1-Naphthyl PP1(1-NA-PP1) RK 24466 eCF506

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
CTV-1	Growth Inhibition Assay			IC50=0.06143 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=0.1599 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=0.23688 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=0.265 μM	SANGER
TE-15	Growth Inhibition Assay			IC50=0.27412 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=0.28116 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=0.3268 μM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=0.44196 μM	SANGER
K-562	Growth Inhibition Assay			IC50=0.44967 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=0.50304 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=0.60529 μM	SANGER
EW-24	Growth Inhibition Assay			IC50=0.62693 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=0.65249 μM	SANGER
NCCIT	Growth Inhibition Assay			IC50=0.73218 μM	SANGER
NCI-H1436	Growth Inhibition Assay			IC50=0.79049 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=0.86203 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=0.87275 μM	SANGER
A704	Growth Inhibition Assay			IC50=0.8921 μM	SANGER
TK10	Growth Inhibition Assay			IC50=0.90669 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=1.19779 μM	SANGER
C2BBe1	Growth Inhibition Assay			IC50=1.20507 μM	SANGER
RXF393	Growth Inhibition Assay			IC50=1.2436 μM	SANGER
KGN	Growth Inhibition Assay			IC50=1.27687 μM	SANGER
NB69	Growth Inhibition Assay			IC50=1.37497 μM	SANGER
TE-11	Growth Inhibition Assay			IC50=1.43418 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=1.44105 μM	SANGER
ST486	Growth Inhibition Assay			IC50=1.45852 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=1.50246 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=1.55083 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=1.55453 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=1.66252 μM	SANGER
RL95-2	Growth Inhibition Assay			IC50=1.66902 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=1.71782 μM	SANGER
MFH-ino	Growth Inhibition Assay			IC50=1.7787 μM	SANGER
GB-1	Growth Inhibition Assay			IC50=1.79833 μM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=1.84688 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=1.88574 μM	SANGER
SW982	Growth Inhibition Assay			IC50=1.92093 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=1.98722 μM	SANGER
TGBC24TKB	Growth Inhibition Assay			IC50=2.05958 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=2.16084 μM	SANGER
SW962	Growth Inhibition Assay			IC50=2.17178 μM	SANGER
SW872	Growth Inhibition Assay			IC50=2.18507 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=2.25714 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=2.29356 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=2.35723 μM	SANGER
BL-70	Growth Inhibition Assay			IC50=2.47422 μM	SANGER
SW954	Growth Inhibition Assay			IC50=2.57408 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=2.68594 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=2.72379 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=2.87005 μM	SANGER
KU812	Growth Inhibition Assay			IC50=3.05299 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=3.12109 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=3.20767 μM	SANGER
SF126	Growth Inhibition Assay			IC50=3.31174 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=3.557 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=3.65 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=3.73433 μM	SANGER
PF-382	Growth Inhibition Assay			IC50=3.83698 μM	SANGER
SH-4	Growth Inhibition Assay			IC50=4.25259 μM	SANGER
KM12	Growth Inhibition Assay			IC50=4.32416 μM	SANGER
NB5	Growth Inhibition Assay			IC50=4.41864 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=4.65256 μM	SANGER
Becker	Growth Inhibition Assay			IC50=4.66416 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=4.81344 μM	SANGER
KINGS-1	Growth Inhibition Assay			IC50=4.82373 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=5.49684 μM	SANGER
SF268	Growth Inhibition Assay			IC50=5.61262 μM	SANGER
A388	Growth Inhibition Assay			IC50=5.63667 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=6.01811 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=6.02075 μM	SANGER
ES4	Growth Inhibition Assay			IC50=6.53074 μM	SANGER
SR	Growth Inhibition Assay			IC50=6.58807 μM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=6.73206 μM	SANGER
KLE	Growth Inhibition Assay			IC50=6.78377 μM	SANGER
HUTU-80	Growth Inhibition Assay			IC50=6.98466 μM	SANGER
SNU-C2B	Growth Inhibition Assay			IC50=7.82737 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=7.94904 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=8.42808 μM	SANGER
GDM-1	Growth Inhibition Assay			IC50=8.97292 μM	SANGER
LC4-1	Growth Inhibition Assay			IC50=9.00911 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=9.15006 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=9.30192 μM	SANGER
BOKU	Growth Inhibition Assay			IC50=9.96466 μM	SANGER
EVSA-T	Growth Inhibition Assay			IC50=10.6568 μM	SANGER
D-283MED	Growth Inhibition Assay			IC50=10.9176 μM	SANGER
NB1	Growth Inhibition Assay			IC50=11.0242 μM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=11.178 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=11.1806 μM	SANGER
NB7	Growth Inhibition Assay			IC50=11.3297 μM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=12.9567 μM	SANGER
697	Growth Inhibition Assay			IC50=13.2701 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=13.5948 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=13.9234 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=14.3915 μM	SANGER
SKM-1	Growth Inhibition Assay			IC50=14.4499 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=14.7591 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=14.7898 μM	SANGER
ECC4	Growth Inhibition Assay			IC50=17.0277 μM	SANGER
ES3	Growth Inhibition Assay			IC50=17.4655 μM	SANGER
LB647-SCLC	Growth Inhibition Assay			IC50=17.4949 μM	SANGER
NB10	Growth Inhibition Assay			IC50=18.5256 μM	SANGER
L-540	Growth Inhibition Assay			IC50=18.8109 μM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=19.51 μM	SANGER
HH	Growth Inhibition Assay			IC50=20.0099 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=23.2289 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=23.8658 μM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=23.9255 μM	SANGER
EC-GI-10	Growth Inhibition Assay			IC50=24.5989 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=26.0203 μM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=26.434 μM	SANGER
Daudi	Growth Inhibition Assay			IC50=27.0773 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=27.081 μM	SANGER
NB6	Growth Inhibition Assay			IC50=27.488 μM	SANGER
ES6	Growth Inhibition Assay			IC50=27.9123 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=28.0373 μM	SANGER
K5	Growth Inhibition Assay			IC50=28.1287 μM	SANGER
ES1	Growth Inhibition Assay			IC50=28.7773 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=29.7346 μM	SANGER
SCLC-21H	Growth Inhibition Assay			IC50=30.7317 μM	SANGER
SK-PN-DW	Growth Inhibition Assay			IC50=32.5598 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=32.9773 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=33.0362 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay			IC50=33.5048 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=33.7666 μM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=33.7928 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=35.144 μM	SANGER
A253	Growth Inhibition Assay			IC50=35.7429 μM	SANGER
HCC1599	Growth Inhibition Assay			IC50=36.7053 μM	SANGER
EB-3	Growth Inhibition Assay			IC50=36.9518 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=37.3224 μM	SANGER
SW684	Growth Inhibition Assay			IC50=41.8495 μM	SANGER
DEL	Growth Inhibition Assay			IC50=42.0522 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=42.1676 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=43.4596 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=44.3925 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=44.5034 μM	SANGER
RCC10RGB	Growth Inhibition Assay			IC50=44.7392 μM	SANGER
CP67-MEL	Growth Inhibition Assay			IC50=45.6241 μM	SANGER
NB17	Growth Inhibition Assay			IC50=45.6643 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=45.9464 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay			IC50=46.0119 μM	SANGER
HCE-4	Growth Inhibition Assay			IC50=46.5968 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=46.7682 μM	SANGER
KARPAS-422	Growth Inhibition Assay			IC50=47.0895 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=47.1622 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=47.6828 μM	SANGER
PSN1	Growth Inhibition Assay			IC50=47.7813 μM	SANGER
NIH3T3	Function assay			Inhibition of human c-Src in NIH3T3 cells, IC50 = 0.0027 μM.	17064066
HEK293	Function assay		1 hr	Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0398 μM.	29941193
HEK293	Function assay		1 hr	Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.418 μM.	29941193
Rh30	Antiproliferative assay		48 hrs	Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay, IC50 = 10.1 μM.	23787099
Huh7	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Huh7	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Vero	Antiviral assay		3 days	Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay	17360676
Vero	Antiviral assay	2.5 uM	5 days	Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control	17360676
Huh7	Antiviral assay	2.5 uM	4 days	Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control	17360676
C6/36	Antiviral assay	2.5 uM	6 days	Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control	17360676
HEK293	Function assay	0.1 to 1 uM	16 hrs	Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting	26191369
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
HEK293	Function assay	0.1 to 1 uM	16 hrs	Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting	26191369
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Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	542.03	Formule	C₂₇H₃₂ClN₅O₅	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	379231-04-6	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	N/A			Smiles	CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (184.49 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 100 mg/mL

Water : 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 40%PEG300 2 5%Tween80 3 50%ddH2O 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 (9.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.650mg/ml (3.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 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.
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 (Mechanism of Action)

Kenmerken	The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
Targets/IC₅₀/Ki	c-Src (Cell-free assay) 2.7 nM LCK (Cell-free assay) <4 nM c-YES (Cell-free assay) 4 nM EGFR (L861Q) (Cell-free assay) 4 nM Lyn (Cell-free assay) 5 nM EGFR (L858R) (Cell-free assay) 5 nM Fyn (Cell-free assay) 10 nM FGR (Cell-free assay) 10 nM BLK (Cell-free assay) 11 nM v-Abl (Cell-free assay) 30 nM EGFR (Cell-free assay) 66 nM c-Kit (Cell-free assay) 200 nM EphA2 (Cell-free assay) 236 nM
In vitro	Saracatinib (AZD0530) remt ook potent andere leden van de Src-tyrosinekinasefamilie, waaronder c-Yes, Fyn, Lyn, Blk, Fgr en Lck met IC50 van 4-10 nM. Het remt gevoelig Src Y530F NIH 3T3 met IC50 van 80 nM. Deze verbinding vermindert significant de invasie van HT1080-cellen door een 3-dimensionale collageenmatrix en remt volledig EGF-geïnduceerde celverstrooiing in NBT-II blaaskankercellen. Het remt potent Src-activering in DU145- en PC3-cellen, door remming van Y419-fosforylering. Het remt de groei van prostaatkanker, waaronder PC3, DU145, CWR22Rv1 en LNCaP, terwijl het een lage activiteit vertoont in LAPC-4, PZ-HPV7 en RWPE-1-cellen. Het induceert celcyclusarrestatie bij G1/S, maar geen caspase 3-splitsingen. Het remt ook significant de migratie van DU145 en PC3 in de Boyden-kamer. Het geeft een potente en aanhoudende blokkering van AKT en verhoogt de gevoeligheid voor bestraling in A549- en Calu-6-cellen. Het remt osteoclasten in activiteit, resorptie en vorming. Het voorkomt ook omkeerbaar de migratie van osteoclastvoorlopercellen.
Kinase Assay	Kinase Assay
Kinase Assay	IC50 van tyrosinekinaseactiviteit wordt gemeten door een enzym-gekoppelde immunosorbentassay (ELISA) met recombinante katalytische domeinen van een panel van receptor- en niet-receptor-tyrosinekinasen (in sommige gevallen wordt slechts een deel van het katalytische domein gebruikt). Dit verbinding dosisbereik is van 0,001-10 mM. Specificiteitsassays tegen een panel van serine/threoninekinasen worden uitgevoerd met behulp van een filtervangstassay met ³²P. Kortom, multidrop 384-platen die 0,5 μL Saracatinib (AZD0530) of controles (alleen DMSO of pH 3.0 buffercontroles) bevatten, worden gedurende 5 minuten geïncubeerd met 15 μL enzym plus peptide/proteïne substraat voordat de reactie wordt geïnitieerd door de toevoeging van 10 μL van 20 mM Mg-ATP. Voor alle enzymen wordt de uiteindelijke concentratie benaderd tot de Michaelis-constante (K_m). Assays worden gedurende 30 minuten bij kamertemperatuur uitgevoerd voordat ze worden beëindigd door de toevoeging van 5 μL orthofosforzuur. Na het mengen wordt de inhoud van de putjes verzameld op een P81 Uniﬁlter-plaat, met orthofosforzuur als wasbuffer. Daarna wordt de IC50 berekend.
In vivo	Saracatinib (AZD0530) vertoont een grote tumorgoeiremming in Src3T3-allografts en een matige groeivertraging in Calu-6, MDA-MB-231, AsPc-1 en BT474C xenografts. Deze verbinding vertoont ook een grote antitumoractiviteit in orthotope DU145-xenograftmuizen bij een dosis van 25 mg/kg (oraal toegediend, dagelijks).
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/18679417/ [2] https://pubmed.ncbi.nlm.nih.gov/19393585/ [3] https://pubmed.ncbi.nlm.nih.gov/19240653/ [4] https://pubmed.ncbi.nlm.nih.gov/19372577/ [5] https://pubmed.ncbi.nlm.nih.gov/19216789/ [6] https://pubmed.ncbi.nlm.nih.gov/18493848/ [7] https://pubmed.ncbi.nlm.nih.gov/19451593/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	pY576-FAK / pY861-FAK / FAK pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα		20551056
Growth inhibition assay	Cell number		24349321

Informatie klinische proef (Clinical Trial Information)

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

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT04598919	Active not recruiting	Idiopathic Pulmonary Fibrosis (IPF)	National Jewish Health\|Yale University\|Icahn School of Medicine at Mount Sinai\|AstraZeneca\|National Center for Advancing Translational Sciences (NCATS)\|Baylor University\|International Center for Health Outcomes and Innovation Research	November 12 2020	Phase 1\|Phase 2
NCT04307953	Recruiting	Fibrodysplasia Ossificans Progressiva	Amsterdam UMC location VUmc\|Royal National Orthopaedic Hospital NHS Trust\|Klinikum Garmisch-Patenkirchen\|University of Oxford\|Brigham and Women''s Hospital\|AstraZeneca\|Innovative Medicines Initiative	August 5 2020	Phase 2
NCT02085603	Completed	Cancer	Sheffield Teaching Hospitals NHS Foundation Trust\|AstraZeneca	March 2014	Phase 2
NCT01864655	Completed	Alzheimer''s Disease	Stephen M. Strittmatter\|National Institute of Neurological Disorders and Stroke (NINDS)\|Yale University	July 2013	Phase 1
NCT01000896	Withdrawn	Cancer\|Non Small Cell Lung Cancer\|Epithelial Ovarian Cancer	AstraZeneca	January 2010	Phase 1

Veelgestelde vragen (Frequently Asked Questions)

Vraag 1:
What is its half-life?

Antwoord:
Based on the following paper, its half-life in vivo is around 40 hours and it reaches its peak level around 2–4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

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