PHA-680632

PHA-680632 is an inhibitor of Aurora A, B, and C kinases (IC50s = 27, 135, and 120 nM, respectively). It has greater than 15-fold selectivity for Aurora A kinase in a panel of 31 kinases. PHA-680632 inhibits phosphorylation of serine 10 on histone H3 in U2OS cells (IC50 = 0.39 µM). It inhibits proliferation of U2OS, HeLa, A549, HCT116, U937, and HL-60 cells (IC50s = 1.6, 0.4, 0.6, 0.1, 0.1, and 0.1 µM, respectively). PHA-680632 reduces the size of established tumors in transgenic v-Ha-ras mice and in an HL-60 human leukemia mouse xenograft model when administered at a dose of 45 mg/kg.Formal Name: N-(2,6-diethylphenyl)-4,6-dihydro-3-[[4-(4-methyl-1-piperazinyl)benzoyl]amino]-pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide. CAS Number: 398493-79-3. Molecular Formula: C28H35N7O2. Formula Weight: 501.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 310 nm. SMILES: O=C(NC1=C(CC)C=CC=C1CC)N(C2)CC3=C2NN=C3NC(C4=CC=C(N5CCN(C)CC5)C=C4)=O. InChi Code: InChI=1S/C28H35N7O2/c1-4-19-7-6-8-20(5-2)25(19)29-28(37)35-17-23-24(18-35)31-32-26(23)30-27(36)21-9-11-22(12-10-21)34-15-13-33(3)14-16-34/h6-12H,4-5,13-18H2,1-3H3,(H,29,37)(H2,30,31,32,36). InChi Key: OBWNXGOQPLDDPS-UHFFFAOYSA-N.