Atuveciclib Racemate 是 Atuveciclib 的外消旋混合物。 Atuveciclib 是口服有效的P-TEFb/CDK9高选择性抑制剂，CDK9/CycT1的IC50为13 nM。

Atuveciclib Racemate is the racemate mixture of Atuveciclib, which is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.

Atuveciclib (BAY-1143572) has potent and highly selective PTEFb-kinase inhibitory activity in the low nanomolar range against PTEFb/CDK9 and an at least 50-fold selectivity against other CDKs. Atuveciclib (BAY-1143572) inhibits the proliferation of 7 MLL-rearrangements positive and negative AML cell lines with a median IC50 of 385 nM (range 230-1100 nM) and induces apoptosis[1]. Atuveciclib (BAY-1143572) shows a favorable selectivity against a panel of non-CDK kinases and it shows broad antiproliferative activity against a panel of tumor cell lines with sub-micromolar IC50 values. The concentration-dependent inhibition of the phosphorylation of the RNA polymerase II and downstream reduction of MYC mRNA and protein levels is observed[2].

The in vivo efficacy of Atuveciclib (BAY-1143572) is significantly enhanced in combination with several chemotherapeutics in different solid tumor models[2]. The inhibition of MYC mRNA is also observed in blood cells of Atuveciclib (BAY-1143572)-treated rats indicating the potential clinical utility of MYC in blood cells as a pharmacodynamic marker in clinical development. Atuveciclib (BAY-1143572) exhibits single agent efficacy at tolerated doses in 4 out of 5 AML xenograft tumor models in mice and in 2 out of 2 AML xenograft tumor models in rats upon once daily oral administration. Partial or even complete remissions could be achieved in several models[1].

1414943-88-6

C18H18FN5O2S

387.43

BAY-1143572 Racemate;阿维西利;Atuveciclib Racemate

DMSO:100 mg/mL (285.11 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years