| Bioactivity | Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects[1][2]. |
| Invitro | Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis[1].Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest[1].Samuraciclib hydrochloride hydrate (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. Samuraciclib trihydrochloride also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma[1].Samuraciclib (ICEC0942) hydrochloride hydrate 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 hydrate |
| Formula | C22H30N6O.(2.5HCl).(2H2O) |
| Molar Mass | 521.70 |
| 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) |
Samuraciclib hydrochloride hydrate
CAS: F: C22H30N6O.(2.5HCl).(2H2O) W: 521.70
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, wi
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