BAY-1251152 is the next-generation, potent and highly selective CDK9/P-TEFb inhibitor. In comparison to BAY-1143572 (the first oral CDK9/P-TEFb inhibitor), BAY-1251152 shows significantly increased biochemical (IC50 CDK9 = 3 nM) and cellular potency (IC50 MOLM13 = 29 nM), and an increased selectivity against CDK2 as well as high permeability and no efflux. The significantly reduced therapeutic dosage and high solubility of BAY-1251152 enable the desired i.v. application. It demonstrated excellent in vivo efficacy upon i.v. treatment in xenograft models (e.g. MOLM13) in mice and rats. Cyclin-dependent kinase 9 (CDK9), a subunit of the positive transcription elongation factor b (P-TEFb) complex, regulates gene transcription elongation by phosphorylating the carboxy-terminal domain (CTD) of RNA polymerase II (RNAPII). The deregulation of CDK9/P-TEFb has implicated in many cancer types.

KEYWORDS: BAY-1251152 | Supplier | CDK9 inhibitor | Enitociclib | VIP-152 | BAY1251152 | BAY 1251152 | CT-BAY125 | CAS [1610358-53-6] | DNA-RNA | CDK9 | Inhibitor | Enzymes