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Samuraciclib trihydrochloride

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MCE 站：Samuraciclib trihydrochloride

产品活性：Samuraciclib (CT7001) trihydrochloride 是一种有效的，具有选择性，ATP 竞争性和口服活性的 CDK7 抑制剂，IC₅₀ 为 41 nM。Samuraciclib trihydrochloride 对 CDK7 的选择性分别是 CDK1，CDK2 (IC₅₀ 为 578 nM)，CDK5 和 CDK9 的 45 倍，15 倍，230 倍和 30 倍。Samuraciclib trihydrochloride 以 GI₅₀ 值为 0.2-0.3 µM 来抑制乳腺癌细胞系的生长，具有有效的抗肿瘤作用。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：CDK  |  Apoptosis

In Vitro: Samuraciclib trihydrochloride (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment promotes cell apoptosis.
Samuraciclib trihydrochloride (ICEC0942; 0-10 µM; 24 hours; HCT116 cells) treatment induces cell cycle arrest.
Samuraciclib trihydrochloride (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.
Samuraciclib trihydrochloride (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.

In Vivo: Samuraciclib trihydrochloride (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 trihydrochloride (ICEC0942) ａnd ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts.

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