Uses
CCT129202 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.
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%.
IC 50
Aurora A: 42 nM (IC
50); Aurora B: 198 nM (IC
50); Aurora C: 227 nM (IC
50)
References
[1] Chan F, et al. Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57. DOI:
10.1158/1535-7163.MCT-07-2156
