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BS-181 hydrochloride

CAS No. : 1397219-81-6

MCE 站：BS-181 hydrochloride

产品活性：BS-181 hydrochloride 是一种高度选择性的 CDK7 抑制剂，IC₅₀ 值为 21 nM，对 CDK7 的选择性是对 CDK1，2，4，5，6 和 9 的 40 多倍。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC₅₀ values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser⁷⁹⁵ and Ser⁸²¹ with an apparent IC₅₀ of 15 μM, similar to the IC₅₀ obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells leads to G1 arrest at and apoptosis. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC₅₀) ranging from 17 to 22 μM and 6.5 μM, respectively. BS-181 significantly inhibits cell migration and invasion ability in a dose-dependent manner.

In Vivo: BS-181 (5 mg/kg, 10 mg/kg, i.p.) inhibits the growth of MCF-7 tumors in nude mice. Intravenous (i.v) and i.p administration of 10 mg/kg BS-181 shows rapid clearance. BS-181 (10 mg/kg/d or 20 mg/kg/d, i.p.) significantly inhibits the growth of tumor in a dose-dependent manner compared to the control group.

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