RGB-286147,784211-09-2

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RGB-286147

CAS No. : 784211-09-2

MCE 国际站：RGB-286147

产品活性：RGB-286147 是一种选择性和 ATP 竞争性 CDK 和 CDK 相关激酶 (CRK) 抑制剂，IC₅₀ 值范围为 9-839 nM。RGB-286147 对其他非 CDK/CRK 激酶的活性较低。RGB-286147 诱导细胞凋亡 (apoptosis)，并具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：CDK  |  Apoptosis

In Vitro: RGB-286147 (50-100 nM; 24-48 hr) induces cell cycle arrest in the G1 phase, causes a marked inhibition of DNA replication, and induces apoptosis in HCT116 cells.
RGB-286147 (100 nM; 48 hr) results in proteolytic cleavage of PARP in HCT116 cells.
RGB-286147 (24-72 hr) shows potent and irreversible cell killing activity in HCT116 cells. The IC₅₀ value for inhibition of colony formation by RGB-286147 is 57 nM.
RGB-286147 (48 hr) exhibits broad anti-tumor activity with an average GI₅₀ value of <10 nM for 60 tumorigenic cell lines. And also inhibits growth of non-cycling HCT116 cells with an IC₅₀ value of 40 nM.

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