Description
Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb / CDK9 inhibitor. Atuveciclib (BAY-1143572) inhibits CDK9 / CycT1 with an IC 50 of 13 nM.Appearance:SolidIC50& Target:CDK9/CycT1 13 nM (IC 50 ) CDK9/CycT1(h) 6 nM (IC 50 ) CDK3/CycE(h) 890 nM (IC 50 ) CDK2/CycE(h) 1000 nM (IC 50 ) CDK1/CycB(h) 1100 nM (IC 50 ) CDK5/p35(h) 1600 nM (IC 50 )In Vitro:Positive transcription elongation factor b (PTEFb) is a heterodimer of CDK9 and one of four cyclin partners, cyclin T1, cyclin K, cyclin T2a or cyclin T2b. Atuveciclib (BAY-1143572) demonstrates potent antiproliferative activity against HeLa cells (IC 50In Vivo:In vivo efficacy studies in the MOLM-13 xenograft model in mice, Atuveciclib (BAY-1143572) demonstrates great potency and high antitumor efficacy. Daily administration of Atuveciclib (BAY-1143572) at 6.25 or 12.5mg/kg results in a dose-dependent antitumoBiological Activity:Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb / CDK9 inhibitor. Atuveciclib (BAY-1143572) inhibits CDK9 / CycT1 with an IC 50 of 13 nM