CCT129202

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CCT129202 是一种有效、选择性、ATP 竞争性泛 Aurora 激酶抑制剂，对 Aurora A、Aurora B 和 Aurora C 的 IC50 值分别为 42、198 和 227 nM。

CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively; displays high selectivity for the Aurora kinases over a broad range of 13 other kinases; inhibits proliferation in multiple cultured human tumor cell lines (GI50=0.08-1.7 uM), induces aberrant mitosis that leads to apoptosis; reduces phosphorylation of histone H3, stabilizes p53, and inhibits growth of HCT116 human colon cancer xenografts in athymic mice.

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-Dependent TK1 Down-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.

CCT-129202 | CCT 129202

Cell Cycle/DNA Damage

Aurora Kinase

Aurora A , Aurora B , Aurora C

Cancer

——

942947-93-5

497.0156

C23H25ClN8OS

>98% (HPLC)

10 mM in DMSO

O=C(NC1=NC=CS1)CN2CCN(C3=C4C(NC(C5=CC=C(N(C)C)C=C5)=N4)=NC=C3Cl)CC2

1-Piperazineacetamide, 4-[6-chloro-2-[4-(dimethylamino)phenyl]-3H-imidazo[4,5-b]pyridin-7-yl]-N-2-thiazolyl-

(-20℃)

With Ice Pack

≥ 2 years