BS-181,1092443-52-1

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BS-181

CAS No. : 1092443-52-1

MCE 国际站：BS-181

产品活性：BS-181 是一种有效的 CDK7 选择性抑制剂 (IC₅₀=21 nM)，与 Seliciclib (HY-30237) 相比。BS-181 抑制CDK2、CDK5 和 CDK9 的 IC₅₀ 值分别为 880 nM、3000 nM 和 4200 nM (不能阻断 CDK1、4 和 6)。BS-181 抑制一组癌细胞生长 (IC₅₀=11.5 μM-37.3 μM)，诱导细胞凋亡 (apoptosis)。BS-181 具有癌症研究相关研究的潜力。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：CDK  |  Apoptosis

In Vitro: BS-181 (0-40 μM; 72 hours) inhibits cancer cells growth, it is against Breast cancer cell lines growth with IC₅₀ values ranging from 15.1 μM to 20 μM, it is against Colorectal cancer cell lines growth with IC₅₀ values ranging from 11.5 μM to15.3 μM and is against lung, osteosarcoma, prostate and liver cancer cell lines with IC₅₀ values ranging from 11.5 μM to 37.3 μM, respectively.
BS-181 (0-50 μM; 4 hours) shows inhibition of phosphorylation of the RNA polymerase II C-terminal domain (CTD) at serine 5 (P-Ser5). It down-regulates CDK4 and cyclin D1 expression while does not effect other CDKs and cyclins.
BS-181 (0-50 μM; 24 hours) shows an increase in cells in G1, accompanied by a reduction in cell numbers in S and G2/M at low concentrations. At higher concentrations, however, cells accumulates in the sub-G1, indicative of apoptosis.

In Vivo: BS-181 (intraperitoneal injection; 5 mg/kg or 10 mg/kg twice daily; total daily doses of 10 mg/kg or 20 mg/kg; 14 days) inhibitstumor growth in a dose-dependent manner. Tumor growth exhibits 25% and 50% reduction compared with the control group, for 10 mg/kg/day and 20 mg/kg/day, respectively.

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