图片.png For research use only

Product Infomation
Product NameCCT129202
CAS No.

942947-93-5

Molecular Weight

497.02

FormulaC₂₃H₂₅ClN₈OS
SMILES

CN(C1=CC=C(C2=NC3=C(C(Cl)=CN=C3N2)N4CCN(CC4)CC(NC5=NC=CS5)=O)C=C1)C

Stock statusGet quote



Online consultation: s_qq.png  s_email.png



Product description

Description

CCT129202 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.


IC50 & Target

________________________________________________________________________________________


Aurora A

42 nM (IC50)

In Vitro

_________________________________________________________________________________________

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-DependentTK1Down-regulation[1].

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].





Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month







Peferences:

[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.