GSK1070916

GSK1070916 is a potent and ATP-competitive inhibitor of Aurora kinases B and C (Kis = 0.38 and 1.5 nM, respectively). It is >250-fold selective for Aurora B and C over Aurora A. GSK1070916 inhibits proliferation of A549 lung cancer cells in vitro (EC50 = 7 nM). It also inhibits proliferation in a panel of 100 tumor cell lines (EC50s = via induction of polyploidy and apoptosis. In vivo, GSK1070916 inhibits histone H3 phosphorylation in a COLO 205 mouse xenograft model and induces tumor regression in an HL-60 mouse xenograft model. It also reduces tumor growth in 10 mouse xenograft models, including models of breast, colon, and lung carcinomas as well as leukemias.Formal Name: N'-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-1H-pyrazol-3-yl]phenyl]-N,N-dimethyl-urea. CAS Number: 942918-07-2. Molecular Formula: C30H33N7O. Formula Weight: 507.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 3 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.2 mg/ml. lambdamax: 252, 334 nm. SMILES: CN(C)CC1=CC=CC(C2=CC3=C(C4=CN(CC)N=C4C5=CC=C(NC(N(C)C)=O)C=C5)C=CN=C3N2)=C1. InChi Code: InChI=1S/C30H33N7O/c1-6-37-19-26(28(34-37)21-10-12-23(13-11-21)32-30(38)36(4)5)24-14-15-31-29-25(24)17-27(33-29)22-9-7-8-20(16-22)18-35(2)3/h7-17,19H,6,18H2,1-5H3,(H,31,33)(H,32,38). InChi Key: QTBWCSQGBMPECM-UHFFFAOYSA-N.