Description
InformationBAY1251152 is a potentPTEFb/CDK9inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.TargetsCDK9 (Cell-free assay) 3 nMIn vitroBAY 1251152 (compound 2) significantly inhibits CDK9 and CDK2 with IC50 of 3 nM and 360 nM, respectively. BAY 1251152 (compound 2) shows cellular potency in MOLM13 with IC50 of 29 nM.In vivoBAY 1251152 demonstrates excellent efficacy upon i.v. treatment in xenograft models (e.g. MOLM13) in mice and rats. BAY 1251152 is currently being evaluated in Phase I studies to determine the safety, tolerability, pharmacokinetics and initial pharmacodynamic biomarker response in patients with advanced cancer.Cell Research(from reference)Cell lines：HeLa, NCI-H460, A2780, DU 145, HeLa-MaTu-ADR, Caco-2, B16F10, MOLM-13 Concentrations：0.001 µM - 10 µM Incubation Time：4 days