LY2857785

LY2857785 is an inhibitor of cyclin-dependent kinase 9 (Cdk9, IC50 = 0.011 µM). It also inhibits Cdk8 and Cdk7 (IC50s = 0.016 and 0.246 µM, respectively), as well as five kinases in a panel of 114 kinases (IC50s = 50 values of 0.22 and 0.197 µM, respectively. It inhibits phosphorylation of DNA-dependent RNA polymerase II (RNAP II) in peripheral blood mononuclear cells (PBMCs) isolated from patients with acute myeloid leukemia (AML) or chronic lymphocytic leukemia (CLL, IC50s = 0.044 and 0.145 µM, respectively). LY2857785 (3, 6, and 9 mg/kg) reduces tumor growth in an MV4-11 rat xenograft model.Formal Name: trans-N1-[4-[2-methyl-3-(1-methylethyl)-2H-indazol-5-yl]-2-pyrimidinyl]-N4-(tetrahydro-2H-pyran-4-yl)-1,4-cyclohexanediamine. CAS Number: 1619903-54-6. Molecular Formula: C26H36N6O. Formula Weight: 448.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 227, 258, 264, 342 nm. SMILES: CC(C1=C2C(C=CC(C3=NC(N[C@H]4CC[C@@H](CC4)NC5CCOCC5)=NC=C3)=C2)=NN1C)C. InChi Code: InChI=1S/C26H36N6O/c1-17(2)25-22-16-18(4-9-24(22)31-32(25)3)23-10-13-27-26(30-23)29-20-7-5-19(6-8-20)28-21-11-14-33-15-12-21/h4,9-10,13,16-17,19-21,28H,5-8,11-12,14-15H2,1-3H3,(H,27,29,30)/t19-,20-. InChi Key: LHIUZPIDLZYPRL-MXVIHJGJSA-N.