Atuveciclib

Atuveciclib is an inhibitor of Cdk9/cyclin T1 (IC50 = 6 nM). 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. and 12. 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 (Cay-14956). InChI: InChI=1S/C18H18FN5O2S/c1-26-16-9-13(19)6-7-15(16)17-21-11-22-18(24-17)23-14-5-3-4-12(8-14)10-27(2,20)25/h3-9,11,20H,10H2,1-2H3,(H,21,22,23,24), InChIKey: ACWKGTGIJRCOOM-UHFFFAOYSA-N, SMILES: CS(CC1=CC=CC(NC2=NC(C3=C(OC)C=C(C=C3)F)=NC=N2)=C1)(=N)=O