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Skip Navigation LinksHome > Kinase Inhibitors > CDK (Cyclin-dependent Kinase) > BAY-1251152 (BAY 1251152)
BAY-1251152 (BAY 1251152)
BAY 1251152 (BAY-1251152) is the next-generation, potent and highly selective CDK9/P-TEFb inhibitor in clinical evaluation. 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 (ref 1). 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.　
Catalog NO: CT-BAY125
Synonym:
CAS NO: 1610358-53-6
Mol. Formula: C19H18F2N4O2S
MW: 404.4
** A snow-white crystalline powder (picture attached), >99% purity HPLC with clean H-NMR, and elemental analysis. Bulk stock! Same day shipping.
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