Cdk4/6 Inhibitor IV

Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound acting as a reversible and ATP-competitive inhibitor of Cdk4/6 (IC₅₀ = 1.5 µM and 5.6 µM for Cdk4/D1 and Cdk6/D1, respectively) with selectivity over Cdk5/p35 (IC50 = 25 µM), v-abl, c-met, IGF-1R and IR (IC₅₀ > 10 µM), Cdk2/A, Cdk2/E, Cdk4/D2, Cdk6/D2 (IC50 > 50 µM) and Cdk1/B (IC₅₀ > 100 µM). Cdk4/6 Inhibitor IV exhibits blocking of pRb phosphorylation at Ser780 and Ser795, induce cell cycle arrest (G0/G1), and apoptosis in U2OS and MRC-5 cells at 5 - 10 µM. Further, suppresses tumor growth in Xenograft mouse model (30 mg/kg, i.p.).