CHIR-124

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抑制剂描述：

产品名称：CHIR-124

产品别名：见爱必信官网

英文别名：CHIR-124

靶点：Chk

CAS：405168-58-3

纯度：99%

外观：见爱必信官网

保存方法：﹣20 ℃冷藏长期储存。冰袋运输

描述：

CHIR-124是高活性的Chk1抑制剂，IC50为0.3 nM，比对Chk2，CDK2/4和Cdc2的抑制性高2000倍，500倍和5000倍

溶解性：DMSO:7 mg/mL
Water:<1 mg/mL
Ethanol:<1 mg/mL

体外研究：

CHIR-124 is a quinolone-based small molecule that is structurally unrelated to other known inhibitors of Chk1. CHIR-124 interacts synergistically with topoisomerase poisons (e.g., Camptothecin or SN-38) in causing growth inhibition in a variety of cancer cell lines, including breast carcinoma (MDA-MB-231 and MDA-MB-435) and colon carcinoma (SW-620 and Colo205), all of which contains the mutant p53 gene. CHIR-124 abrogates the SN-38-induced S and G2-M checkpoints and potentiates apoptosis in MDA-MD-435 breast cancer cells. The abrogation of the G2-Mcheckpoint and induction of apoptosis by CHIR-124 are enhanced by the loss of p53. CHIR-124 also potently targets other kinases such as PDGFR and Flt3 with IC50 of 6.6 nM and 5.8 nM, respectively.

体内研究：CHIR-124 potentiates the growth inhibitory effects of Irinotecan by abrogating the G2-M checkpoint and increasing tumor apoptosis in an orthotopic breast cancer xenograft model.

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