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Roscovitine (Seliciclib) CDK Inhibitor

Name: Roscovitine (Seliciclib)
Brand: Selleck Chemicals
SKU: S1153
Rating: 5 (129 reviews)

Cat.Nr.: S1153

Roscovitine is een krachtige en selectieve CDK-remmer voor Cdc2, CDK2 en CDK5 met een IC50 van 0,65 μM, 0,7 μM en 0,16 μM in celvrije assays. Het heeft weinig effect op CDK4/6. Fase 2.

Roscovitine (Seliciclib) CDK Inhibitor Chemical Structure

Chemische structuur

Moleculair gewicht: 354.45

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.85%

99.85

Gerelateerde doelwitten	HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Overige CDK Inhibitoren	AS2863619 Ro-3306 SEL120 (SEL120-34A) hydrochloride INX-315 Tagtociclib (PF-07104091) PF-07220060 (CDK4/6-IN-6) AZD4573 ON123300 Enitociclib (BAY 1251152) Samuraciclib (ICEC0942) hydrochloride

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

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
LB771-HNC	Growth Inhibition Assay			IC50=48.9212 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=48.6202 μM	SANGER
DU-4475	Growth Inhibition Assay			IC50=48.4937 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=47.0448 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=46.0115 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=44.9697 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=42.893 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=42.6671 μM	SANGER
DG-75	Growth Inhibition Assay			IC50=42.6546 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=42.2787 μM	SANGER
HT	Growth Inhibition Assay			IC50=42.0028 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=41.5705 μM	SANGER
NCI-H1882	Growth Inhibition Assay			IC50=40.5998 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=39.5842 μM	SANGER
NCI-H345	Growth Inhibition Assay			IC50=38.9106 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay			IC50=38.2477 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=37.7069 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=37.6712 μM	SANGER
OPM-2	Growth Inhibition Assay			IC50=37.2949 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=37.1856 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=37.012 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=36.3276 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=36.3246 μM	SANGER
TE-441-T	Growth Inhibition Assay			IC50=36.1148 μM	SANGER
IMR-5	Growth Inhibition Assay			IC50=35.3139 μM	SANGER
K5	Growth Inhibition Assay			IC50=35.0861 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=34.9422 μM	SANGER
NCI-H2141	Growth Inhibition Assay			IC50=34.6533 μM	SANGER
KGN	Growth Inhibition Assay			IC50=34.2524 μM	SANGER
LP-1	Growth Inhibition Assay			IC50=33.8908 μM	SANGER
NCI-H64	Growth Inhibition Assay			IC50=33.8597 μM	SANGER
RKO	Growth Inhibition Assay			IC50=33.5969 μM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=33.4936 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=32.9129 μM	SANGER
Calu-6	Growth Inhibition Assay			IC50=32.4745 μM	SANGER
LOUCY	Growth Inhibition Assay			IC50=32.1253 μM	SANGER
SK-N-FI	Growth Inhibition Assay			IC50=31.7535 μM	SANGER
SIG-M5	Growth Inhibition Assay			IC50=31.6833 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=31.1397 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay			IC50=31.1059 μM	SANGER
NCI-H82	Growth Inhibition Assay			IC50=31.0135 μM	SANGER
NCI-H510A	Growth Inhibition Assay			IC50=30.0329 μM	SANGER
ES3	Growth Inhibition Assay			IC50=29.9582 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=29.9483 μM	SANGER
KM12	Growth Inhibition Assay			IC50=29.6239 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=29.0113 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=28.9733 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=28.908 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=28.7969 μM	SANGER
HL-60	Growth Inhibition Assay			IC50=27.9869 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=27.9144 μM	SANGER
KARPAS-299	Growth Inhibition Assay			IC50=26.8646 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=26.8082 μM	SANGER
BL-41	Growth Inhibition Assay			IC50=25.9597 μM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=25.6529 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=25.4425 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=24.5343 μM	SANGER
HH	Growth Inhibition Assay			IC50=24.3819 μM	SANGER
LS-513	Growth Inhibition Assay			IC50=23.5179 μM	SANGER
EB-3	Growth Inhibition Assay			IC50=23.1831 μM	SANGER
ACN	Growth Inhibition Assay			IC50=21.3389 μM	SANGER
NOMO-1	Growth Inhibition Assay			IC50=21.2008 μM	SANGER
ES8	Growth Inhibition Assay			IC50=21.06 μM	SANGER
CESS	Growth Inhibition Assay			IC50=20.8549 μM	SANGER
BL-70	Growth Inhibition Assay			IC50=20.3274 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=20.0356 μM	SANGER
BC-1	Growth Inhibition Assay			IC50=19.1198 μM	SANGER
LC4-1	Growth Inhibition Assay			IC50=18.8734 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=18.7688 μM	SANGER
A101D	Growth Inhibition Assay			IC50=18.3208 μM	SANGER
BC-3	Growth Inhibition Assay			IC50=18.0305 μM	SANGER
TGW	Growth Inhibition Assay			IC50=17.8124 μM	SANGER
JAR	Growth Inhibition Assay			IC50=17.0152 μM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=16.8246 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=16.3601 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=15.8382 μM	SANGER
OCI-AML2	Growth Inhibition Assay			IC50=15.6482 μM	SANGER
HCC1599	Growth Inhibition Assay			IC50=14.5975 μM	SANGER
SCC-3	Growth Inhibition Assay			IC50=14.2956 μM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=13.9121 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=13.8379 μM	SANGER
Raji	Growth Inhibition Assay			IC50=13.7894 μM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=13.6262 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=12.8613 μM	SANGER
697	Growth Inhibition Assay			IC50=12.6007 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=12.3516 μM	SANGER
NB1	Growth Inhibition Assay			IC50=12.3308 μM	SANGER
COR-L279	Growth Inhibition Assay			IC50=12.2907 μM	SANGER
LB831-BLC	Growth Inhibition Assay			IC50=11.5624 μM	SANGER
ST486	Growth Inhibition Assay			IC50=10.351 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=10.35 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=9.97495 μM	SANGER
KARPAS-422	Growth Inhibition Assay			IC50=9.96336 μM	SANGER
Becker	Growth Inhibition Assay			IC50=9.46082 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=9.45785 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay			IC50=8.50264 μM	SANGER
NCCIT	Growth Inhibition Assay			IC50=7.55482 μM	SANGER
MRK-nu-1	Growth Inhibition Assay			IC50=7.12969 μM	SANGER
A3-KAW	Growth Inhibition Assay			IC50=5.76116 μM	SANGER
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	15958589
LP-1	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human LP-1 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry	15958589
LP-1	Cytotoxicity assay	20 to 30 uM	24 hrs	Cytotoxicity against human LP-1 cells assessed as reduction of cell viability at 20 to 30 uM treated for 24 hrs followed by washout measured after total 72 hrs growth period alamar blue assay relative to control	15958589
LP-1	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human LP-1 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting	15958589
LP-1	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human LP-1 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting	15958589
LP-1	Apoptosis assay	30 uM	3 to 5 hrs	Induction of apoptosis in human LP-1 cells assessed as increase in level of cleaved PARP at 30 uM after 3 to 5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as increase in level of cleaved PARP at 30 uM after 5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as fast slow migrating hyperphosphorylated RNA polymerase 2O form at 30 uM after 1.5 hrs by immunoblotting	15958589
RPM18226	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human RPM18226 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting	15958589
RPM18226	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human RPM18226 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting	15958589
RPM18226	Apoptosis assay	30 uM	3 to 5 hrs	Induction of apoptosis in human RPM18226 cells assessed as increase in level of cleaved PARP at 30 uM after 3 to 5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells assessed as changes in XIAP protein level at 30 uM after 3 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells assessed as changes in survivin protein level at 30 uM after 3 hrs by immunoblotting	15958589
RPM18226	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human RPM18226 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as reduction of RNA polymerase 2 phosphoserine 2 level at 30 uM after 1.5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as dephosphorylation of pRb at S249/T252 at 30 uM after 1.5 hrs by immunoblotting	15958589
NCI-H929	Cytotoxicity assay	20 to 30 uM	16 hrs	Cytotoxicity against human NCI-H929 cells assessed as reduction of cell viability at 20 to 30 uM treated for 16 hrs followed by washout measured after total 72 hrs growth period alamar blue assay relative to control	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells assessed as reduction of Mcl-1 protein level at 30 uM after 3 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells assessed as changes in Bcl-2 protein level at 30 uM after 3 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	3 hrs	Induction of apoptosis in human NCI-H929 cells at 30 uM after 3 hrs using TUNEL staining by flow cytometry	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as reduction of RNA polymerase 2 phosphoserine 5 level at 30 uM after 1.5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as reduction of Hdm2 level at 30 uM after 1.5 hrs by immunoblotting	15958589
NCI-H929	Apoptosis assay	30 uM	1.5 hrs	Induction of apoptosis in human NCI-H929 cells assessed as increase of p53 accumulation at 30 uM after 1.5 hrs by immunoblotting	15958589
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	21080703
HCT116	Function assay	30 to 40 umol/L	24 hrs	Inhibition of cyclin A in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis	21080703
HCT116	Function assay	30 to 40 umol/L	24 hrs	Inhibition of cyclin B in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis	21080703
HCT116	Function assay	30 to 40 umol/L	24 hrs	Inhibition of cyclin D1 in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis	21080703
HCT116	Function assay	30 to 40 umol/L	24 hrs	Inhibition of CDK2 in human HCT116 cells assessed as decrease in protein level at 30 to 40 umol/L after 24 hrs by immunoblotting analysis	21080703
HT-29	Function assay	2.5 to 40 uM	24 hrs	Inhibition of retinoblastoma protein in human HT-29 cells assessed as reduction of cyclin A level at 2.5 to 40 uM after 24 hrs by immunoblotting	21417417
MCF7	Cell cycle assay		24 hrs	Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
RPMI8226	Cell cycle assay		24 hrs	Cell cycle arrest in human RPMI8226 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
MCF7	Cell cycle assay		24 hrs	Cell cycle arrest in human MCF7 cells assessed as decrease in S phase cell population after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
MCF7	Cell cycle assay		24 hrs	Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
RPMI8226	Cell cycle assay		24 hrs	Cell cycle arrest in human RPMI8226 cells assessed as accumulation at sub-G1 phase after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
MCF7	Cell cycle assay	80 uM	24 hrs	Cell cycle arrest in human MCF7 cells assessed as reduction of actively replicating DNA level at 80 uM after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
MCF7	Function assay	20 uM	24 hrs	Induction of p53-dependent transcriptional activity in human MCF7 cells assessed as increase of p21 WAF1 level at 20 uM after 24 hrs by immunofluorescence assay	21417417
RPMI8226	Cell cycle assay		24 hrs	Cell cycle arrest in human RPMI8226 cells assessed as decrease in S phase cell population after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
RPMI8226	Cell cycle assay	80 uM	24 hrs	Cell cycle arrest in human RPMI8226 cells assessed as reduction of actively replicating DNA level at 80 uM after 24 hrs using propidium iodide and BrdU staining by flow cytometry	21417417
A549	Apoptosis assay	2 uM	48 hrs	Induction of apoptosis in human A549 cells assessed as DNA fragmentation at 2 uM after 48 hrs by agarose gel electrophoresis	23623491
Sf9	Function assay		10 mins	Inhibition of His-6-tagged recombinant human CDK2/cyclinE expressed in baculovirus-infected sf9 cells using histone H1 as substrate after 10 mins by liquid scintillation counting in presence of [gamma-32P]ATP, IC50 = 0.1 μM.	24417566
BJ	Function assay	10 uM	10 days	Suppression of senescence in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay	24681986
BJ	Function assay	10 uM	10 days	Inhibition of ataxia telangiectasia-mutated in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay	24681986
MCF7	Function assay	10 uM	10 mins	Sensitization of infrared-induced DNA damage in human MCF7 cells assessed as reduction in colony formation at 10 uM pretreated for 10 mins followed by irradiation for 4 hrs measured after 10 days by crystal violet staining analysis	26851505
Caco2	Cell cycle assay			Cell cycle arrest in human Caco2 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
HaCaT	Cell cycle assay			Cell cycle arrest in human HaCaT cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
HuH7	Cell cycle assay			Cell cycle arrest in human HuH7 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
PC3	Cell cycle assay			Cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase by Hoechst staining based fluorescence assay	28214231
MDA-MB-231	Cell cycle assay			Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
HCT116	Cell cycle assay			Cell cycle arrest in human HCT116 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
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	28557430
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
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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
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	30199702
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	354.45	Formule	C₁₉H₂₆N₆O	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	186692-46-6	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	CYC202, Seliciclib, R-roscovitine			Smiles	CCC(CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CC=CC=C3

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 71 mg/mL (200.31 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 71 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.
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.
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.	10.000mg/ml (28.21mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 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 make it clear; 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.

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)

Targets/IC₅₀/Ki	CDK5/p35 (Cell-free assay) 0.16 μM Cdc2/CyclinB (Cell-free assay) 0.65 μM CDK2/CyclinA (Cell-free assay) 0.7 μM CDK2/CyclinE (Cell-free assay) 0.7 μM ERK2 (Cell-free assay) 14 μM
In vitro	Roscovitine vertoont een hoge efficiëntie en hoge selectiviteit ten opzichte van sommige cycline-afhankelijke kinasen met een IC50 van respectievelijk 0,65, 0,7, 0,7 en 0,16 μM voor cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E en cdk5/p53. Deze verbinding remt omkeerbaar de profase/metafase-overgang in het micromolaire bereik van zeester-oöcyten en zee-egel-embryo's, remt in vitro de M-fase-bevorderende factoractiviteit en in vitro de DNA-synthese in Xenopus-eiextracten, en onderdrukt de proliferatie van zoogdiercellijnen met een gemiddelde IC50 van 16 μM. In mesangiale cellen resulteert het in een dosisafhankelijke vermindering van CDK2-activiteit, waarbij bij concentraties van 7,5, 12,5 en 25 mM deze chemische stof een respectievelijk 25, 50% en 100% afname van de CDK2-activiteit veroorzaakt. Een recente studie toont aan dat deze verbinding de cdk5-kinaseactiviteit, celproliferatie, multicellulaire ontwikkeling en cdk5-nucleaire translocatie in Dictyostelium discoideum remt, zonder de expressie van cdk5-eiwit tijdens axenische groei te beïnvloeden.
Kinase Assay	Enzymen
Kinase Assay	Roscovitine (Seliciclib) is een krachtige en selectieve CDK-remmer voor Cdc2, CDK2 en CDK5 met IC50 van 0,65 μM, 0,7 μM en 0,16 μM in celvrije assays. Het heeft weinig effect op CDK4/6.
In vivo	Roscovitine, in een dosis van 50 mg/kg, remt de groei van xenografts van de Ewing-sarcoomfamilie (ESFT) significant. Deze verbinding verhoogt het antitumorale effect van doxorubicine zonder verhoogde toxiciteit met een mechanisme dat celcyclusarrest omvat in plaats van apoptose in naakte muizen met gevestigde MCF7-xenografts.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/9030781/ [2] https://pubmed.ncbi.nlm.nih.gov/9366565/ [3] https://pubmed.ncbi.nlm.nih.gov/22234985/ [4] https://pubmed.ncbi.nlm.nih.gov/16230394/ [5] https://pubmed.ncbi.nlm.nih.gov/19003963/

Toepassingen (Applications)

Methoden	Biomarkers	PMID
Western blot	p-Rb / p-CDK2 / CDK2 / Cyclin D1 / Cyclin A2 / ERα / ERβ/ AIB1 / PELP1 pT231-tau / pS202-tau / tau	21834972
Immunofluorescence	E2F1 / FASN / Bmi1 / Cyclin D2 / CDK2 / CDK4 CDK1 / Smek2 / FUBP1 / Cdc20	20890301
Growth inhibition assay	Cell viability	29996940

Informatie klinische proef (Clinical Trial Information)

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

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT02649751	Terminated	Cystic Fibrosis	University Hospital Brest\|ManRos Therapeutics\|Cyclacel Pharmaceuticals Inc.	February 22 2016	Phase 2

Veelgestelde vragen (Frequently Asked Questions)

Vraag 1:
How can I reconstitute it for in vivo studies?

Antwoord:
It in 1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+PEG 400 is a clear solution which is okay for injection. And this compound in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30mg/ml is a suspension, which is fine for oral gavage.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):