Atuveciclib (BAY-1143572) is a potent, highly selective, orally bioavailable CDK9/P-TEFb inhibitor with IC50 of 6 nM for CDK9/CyclinT1.
Atuveciclib displays >150-fold selectivity over CDK1/2/3/5/6/7 (IC50>800 nM), also shows submicromolar inhibitory activity against GSK3α (IC50=45 nM), GSK3β (IC50=87 nM).
Atuveciclib demonstrates antiproliferative activity against HeLa cells (IC50=920 nM) and MOLM‐13 cells (IC50=310 nM).
Atuveciclib exhibits anticancer activity in human AML models.
