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CCT129202, a derivative of the piperazinyl imidazo[4,5-b] pyridine scaffold, is a novel and potent inhibitor of Aurora kinase that ATP-competitively inhibits Aurora A, Aurora B and Aurora C with values of 50% inhibition concentration IC50 of 0.042, 0.198 and 0.227 μmol/L respectively. CCT129202 exhibits anti-cancer activity against multiple human tumor cell lines through inhibiting proliferation, inducing apoptosis and delaying mitosis, abrogation of nocodazole-induced mitotic arrest and spindle defects. Recent study results have shown that CCT129202 inhibits the growth of HCT116 xenografts in nude mice and induces the production of a cyclin-dependent kinase inhibitor, p21, in HCT116 cells consequently leading to Rb hypophosphorylation.

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