Enitociclib ((±)-BAY-1251152) is a potent, highly specific P-TEFb/CDK9 inhibitor with IC50 of 3 nM.
BAY-1251152 exhibits ex vivo potency (MOLM-13 cells, IC50=29 nM) and enhanced selectivity against CDK2, permeability, solubility, and no efflux.
BAY-1251152 has demonstrated IC50 of 19.06, 16.57 and 74.64 nM against HeLa, SiHa and OVCAR-3 cells, respectively.
BAY-1251152 is the only selective CDK9 inhibitor currently undergoing clinical trialsagainst advanced malignancies (NHL and solid tumors; NCT02635672).
1. Ulrich T. Luecking, et al. Abstract 984: Identification of potent and highly selective PTEFb inhibitor BAY 1251152 for the treatment of cancer: from p.o. to i.v. application via scaffold hops. DOI: 10.1158/1538-7445.
