CCT129202

CCT129202 is an Aurora kinase inhibitor that inhibits Aurora A and B by 82 and 60%, respectively, when used at a concentration of 1 µM in cell-free assays. It is selective for Aurora A and B over a panel of 13 kinases at 1 µM. CCT129202 inhibits growth of COLO 205, SW620, HCT116, HT-29, KW12, HeLa, A2780, OVCAR-8, MDA-MB-157, and MB4-11 cancer cells (GI50s = 0.08-1.2 µM). It induces DNA accumulation and cell cycle arrest at the G2/M phase, as well as apoptosis in HCT116 cells. CCT129202 increases the accumulation of doxorubicin and rhodamine 123 in multidrug-resistant (MDR) KBv200 and MCF-7/adr cells and increases the susceptibility of MDR KBv200, MCF-7/adr, S1-M1-80, and HL60/adr cells to cisplatin (Cay-13119) and doxorubicin (Cay-15007). In vivo, CCT129202 (100 mg/kg) reduces tumor growth in an HCT116 mouse xenograft model. It also potentiates the antitumor effects of vincristine (Cay-11764) in a KBv200 mouse xenograft model.Formal Name: 4-[6-chloro-2-[4-(dimethylamino)phenyl]-3H-imidazo[4,5-b]pyridin-7-yl]-N-2-thiazolyl-1-piperazineacetamide. CAS Number: 942947-93-5. Molecular Formula: C23H25ClN8OS. Formula Weight: 497.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 3 mg/ml. lambdamax: 267, 348, 404 nm. SMILES: CN(C)C(C=C1)=CC=C1C2=NC3=NC=C(Cl)C(N4CCN(CC(NC5=NC=CS5)=O)CC4)=C3N2. InChi Code: InChI=1S/C23H25ClN8OS/c1-30(2)16-5-3-15(4-6-16)21-28-19-20(17(24)13-26-22(19)29-21)32-10-8-31(9-11-32)14-18(33)27-23-25-7-12-34-23/h3-7,12-13H,8-11,14H2,1-2H3,(H,25,27,33)(H,26,28,29). InChi Key: QYKHWEFPFAGNEV-UHFFFAOYSA-N.