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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 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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