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CCT129202 is an aurora kinase inhibitor with IC₅₀s of 42, 198, and 227 nM for aurora A, B and C, respectively.

CCT129202 causes the accumulation of human tumor cells with z4N DNA content, leading to apoptosis. CCT129202 is found to induce apoptosis with GI₅₀ values that ranges between 0.08 and 1.7 μM. CCT120202-treated human tumor cells shows a delay in mitosis, abrogation of nocodazole-induced mitotic arrest, and spindle defects. CCT129202 Causes p21Up-regulation, Rb Hypophosphorylation, and H2F-DependentTK1Down-regulation.

Growth of HCT116 xenografts in nude mice is inhibited after i.p. administration of CCT129202. p21, the cyclin-dependent kinase inhibitor, is induced by CCT129202. Up-regulation of p21 by CCT129202 in HCT116 cells led to Rb hypophosphorylation and E2F inhibition, contributing to a decrease in thymidine kinase 1 transcription.

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