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Atuveciclib Racemate

CAS No. : 1414943-88-6

MCE 国际站：Atuveciclib Racemate

产品活性：Atuveciclib Racemate (BAY-1143572 Racemate) 是 Atuveciclib 的外消旋混合物。 Atuveciclib 是一种有效且高选择性的口服 P-TEFb/CDK9 抑制剂，CDK9/CycT1 的IC₅₀ 为13 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: 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. 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) shows a favorable selectivity against a panel of non-CDK kinases. 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.

In Vivo: 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.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. The in vivo efficacy of Atuveciclib (BAY-1143572) is significantly enhanced in combination with several chemotherapeutics in different solid tumor models.

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