RGB-286147

RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC₅₀ values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity^[1]. 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^[1].
RGB-286147 (100 nM; 48 hr) results in proteolytic cleavage of PARP in HCT116 cells^[1].
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^[1].
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^[1].