Crozbaciclib

CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively. IC50 & Target:IC50: 3 nM (CDK4), 1 nM (CDK6)^[1] In Vitro: CDK4/6/1 Inhibitor is a potent anti-proliferative agent that arrests U87MG cell line exclusively in G1 (IC₅₀=15.3 ± 2.9 nM in the anti-proliferation assay). U87MG cells exposed to varying concentrations of CDK4/6/1 Inhibitor for 24 hours show a dose-related increase in G1 arrest, and a significant increase in the percentage of cells in G1 is found in as little as 13.72 nM of CDK4/6/1 Inhibitor^[1]. In Vivo: CDK4/6/1 Inhibitor has tumor growth inhibition values ranging from 62% to 99% for doses ranging from 3.125 to 50 mg/kg in an orthotopic xenograft mouse model of glioblastoma multiforme, and no significant body weight loss is observed. The increase in life span based on the median survival time of vehicle-treated animals in mice administered a dose of 50 mg/kg is significant at 162%^[1].