Biological Activity
Atuveciclib (BAY-1143572) is a potent and highly selective PTEFb/CDK9 inhibitor with IC50 of 13 nM for CDK9/CycT. Its IC50 for CDK2 is about 100-fold higher than that for CDK9. In addition to CDK family members, it also inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β, respectively.
in vivo
BAY 1143572 has a low plasma clearance (CL b 1.1 L/h/kg) and a volume of distribution (Vss) of 1.0 L/kg in a rat pharmacokinetic study . Its oral bioavailability is 54% and the blood-plasma concentration ratio is 1. BAY 1143572 has no significant inhibitory effect on cytochrome P450 activity, IC50>20 μM. NOD/Shi-scid/IL-2Rγ in immunocompromised.
