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编 号：F621943
分子式：C22H30N6O
分子量：394.51
分子式：C22H30N6O
分子量：394.51
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CAS No: 1805833-75-3
产品详情
生物活性：
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects.
体内研究：
Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors.The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts.Animal Model:Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells.
Dosage:100 mg/kg
Administration:Oral gavage; daily; for 14 days
Result:At day 14, tumor growth was inhibited by 60%.
体外研究：
Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment promotes cell apoptosis.Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment induces cell cycle arrest.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. Samuraciclib also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma.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.
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects.
体内研究：
Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) treatment inhibits tumor growth by 60% at day 14, and is accompanied by highly significant reductions in PolII Ser2 and Ser5 phosphorylation in PBMCs and in tumors.The combination of Samuraciclib (ICEC0942) and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts.Animal Model:Female nu/nu-BALB/c athymic nude mice (7-week old) with MCF7 cells.
Dosage:100 mg/kg
Administration:Oral gavage; daily; for 14 days
Result:At day 14, tumor growth was inhibited by 60%.
体外研究：
Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment promotes cell apoptosis.Samuraciclib (ICEC0942; 0-10 μM; 24 hours; HCT116 cells) treatment induces cell cycle arrest.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. Samuraciclib also inhibits phosphorylation of CDK1, CDK2 and retinoblastoma.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.
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