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Atuveciclib is an inhibitor of Cdk9/cyclin T1 (IC50 = 6 nM).1 It is selective for Cdk9/cyclin T1 over Cdk1/cyclin B, Cdk2/cyclin E, Cdk3/cyclin E, Cdk5/p35, Cdk6/cyclin D3, and Cdk7/cyclin H/Mat1 (IC50s = 1,100, 1,000, 890, 1,600, >10,000 and >10,000 nM, respectively). In vivo, atuveciclib (6.25 and 12.5 mg/kg) reduces tumor area in a MOLM-13 acute myeloid leukemia (AML) mouse xenograft model. It reduces skin thickness and scaling in a mouse model of psoriasis induced by imiquimod (Item No. 14956).2
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1. Identification of atuveciclib (BAY 1143572), the first highly selective, clinical PTEFb/CDK9 inhibitor for the treatment of cancer. ChemMedChem 12(21), 1776-1793 (2017).
2. Cyclin-