CCT-129202

• CAT Number: I005607
• CAS Number: 942947-93-5
• Molecular Formula: C₂₃H₂₅ClN₈OS
• Molecular Weight: 497.02
• Purity: ≥95%
• Target: Aurora Kinase
• Solubility: 10 mM in DMSO
• Storage: 3 years -20℃ powder
• IC50: IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C
• IUPAC Name: 2-[4-[6-chloro-2-[4-(dimethylamino)phenyl]-1H-imidazo[4,5-b]pyridin-7-yl]piperazin-1-yl]-N-(1,3-thiazol-2-yl)acetamide
• InChI: InChI=1S/C23H25ClN8OS/c1-30(2)16-5-3-15(4-6-16)21-28-19-20(17(24)13-26-22(19)29-21)32-10-8-31(9-11-32)14-18(33)27-23-25-7-12-34-23/h3-7,12-13H,8-11,14H2,1-2H3,(H,25,27,33)(H,26,28,29)
• InChIKey: QYKHWEFPFAGNEV-UHFFFAOYSA-N
• SMILES: CN(C)C1=CC=C(C=C1)C2=NC3=NC=C(C(=C3N2)N4CCN(CC4)CC(=O)NC5=NC=CS5)Cl

CCT-129202 (Cat.No:I005607) is an ATP-competitive pan-Aurora inhibitor with IC50 values of 0.042μM, 0.198μM, and 0.227μM for AuroraA, AuroraB, and AuroraC, respectively. It has a slight effect on FGFR3, GSK3β, PDGFRβ, and other targets. In vitro studies show that CCT-129202 is highly selective for AuroraA and AuroraB, inhibiting them by 92% and 60%, respectively. It also induces apoptosis in HCT116 cells containing ≥4N DNA, and inhibits tumor growth in vivo.

Reference

1:Protein kinase C modulates Aurora-kinase inhibition induced by CCT129202 in HMC-1⁵⁶⁰,⁸¹⁶ cell line. Tobío A, Alfonso A, Fernández-Araujo A, Alonso E, Botana LM.Antiinflamm Antiallergy Agents Med Chem. 2013;12(3):265-76. PMID: 23701310 2:Enhancing chemosensitivity in ABCB1- and ABCG2-overexpressing cells and cancer stem-like cells by an Aurora kinase inhibitor CCT129202. Cheng C, Liu ZG, Zhang H, Xie JD, Chen XG, Zhao XQ, Wang F, Liang YJ, Chen LK, Singh S, Chen JJ, Talele TT, Chen ZS, Zhong FT, Fu LW.Mol Pharm. 2012 Jul 2;9(7):1971-82. doi: 10.1021/mp2006714. Epub 2012 Jun 13. PMID: 22632055 3:Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity. Chan F, Sun C, Perumal M, Nguyen QD, Bavetsias V, McDonald E, Martins V, Wilsher NE, Raynaud FI, Valenti M, Eccles S, Te Poele R, Workman P, Aboagye EO, Linardopoulos S.Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57. PMID: 18089709 Free Article