产品描述:
Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine that reversibly blocks Cdk4/cyclin D1 and Cdk6/cyclin D1 activity with IC50 values of 1.5 and 5.6 μM, respectively.{29264} It demonstrates potent selectivity for Cdk4/6 over Cdk5/p35, v-abl, c-met, IGF-1R, insulin receptor, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D2, Cdk6/cyclin D2, and Cdk1/cyclin B (IC50s = > 10-100 µM).{29264} At 5-10 µM, this compound blocks retinoblastoma protein phosphorylation at Ser780 and Ser795, inducing cell cycle arrest in the G1 phase and apoptosis in asynchronous cell lines.{29264} In mice bearing human HCT116 colon carcinoma xenografts, 30 mg/kg, i.p. Cdk/6 inhibitor IV suppressed tumor growth after 29 days of treatment.{29264}