CCT 137690 is an
aurora kinase inhibitor with
IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.
IC50 & Target: IC50: 142 nM (Aurora A), 198 nM (Aurora B), 227 nM (Aurora C)
[1]Ki: 49.8 nM (Aurora A)[1]
In Vitro: CCT129202 causes the accumulation of human tumor cells with z4N DNA content, leading to apoptosis. CCT129202 is found to induce apoptosis with GI
50 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
[1].
In Vivo: 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
[1].