PeptideDB

Samuraciclib hydrochloride

CAS: 1805789-54-1 F: C22H31ClN6O W: 430.97

Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibit
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Bioactivity Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects[1][2].
Invitro Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].Samuraciclib (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].Samuraciclib (ICEC0942; 0-10 µM; 0-24 hours; HCT116 cells) treatment inhibits the phosphorylation of PolII CTD in a dose and time dependent manner in HCT116 colon cancer cells. ICEC0942 also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].Samuraciclib (ICEC0942) inhibits the growth of MCF7, T47D, MDA-MB-231, HS578T, MDA-MB-468, MCF10A and HMEC cells with GI50 values of 0.18 µM, 0.32 µM, 0. 33 µM, 0.21 µM, 0.22 µM, 0.67 µM and 1.25 µM, respectively[1]. Apoptosis Analysis[1] Cell Line:
Name Samuraciclib hydrochloride
CAS 1805789-54-1
Formula C22H31ClN6O
Molar Mass 430.97
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)