Biological Activity
CCT129202 is an ATP-competitive pan-Aurora inhibitor with IC50s of 0.042 μM, 0.198 μM and 0.227 μM for Aurora A, Aurora B and Aurora C, respectively, and has a weaker effect on FGFR3, GSK3β, PDGFRβ, etc.
in vivo
CCT129202 at a dose of 100 mg/kg subcutaneously injected HCT116 colon xenografts in athymic mice, after 30 minutes, caused a ~50% decrease in histone H3 phosphorylation, and after 9 days of treatment, significantly inhibited tumor growth, compared with the control group , inhibited by 57.7%.
