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Samuraciclib hydrochloride hydrate

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MCE 站：Samuraciclib hydrochloride hydrate

产品活性：Samuraciclib (CT7001) hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 以 GI₅₀ 值为 0.2-0.3 ?M 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 hydrochloride hydrate (ICEC0942; 0-10 ?M; 24 hours; HCT116 cells) treatment promotes cell apoptosis.
Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 ?M; 24 hours; HCT116 cells) treatment induces cell cycle arrest.
Samuraciclib hydrochloride hydrate (ICEC0942; 0-10 ?M; 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 (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 ?M, 0.32 ?M, 0. 33 ?M, 0.21 ?M, 0.22 ?M, 0.67 ?M and 1.25 ?M, respectively.

In Vivo: Samuraciclib (ICEC0942; 100 mg/kg; oral gavage; daily; for 14 days; female nu/nu-BALB/c athymic nude mice) hydrochloride hydrate 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) hydrochloride hydrate and ICI 47699 treatment shows complete growth arrest of estrogen receptor (ER)-positive tumor xenografts.

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