CHIR-124
货号: abs817968
货号-规格 | 货期 | 价格 | 数量 |
abs817968-10mg | 1-2周 | ¥1658.00 | - + |
abs817968-25mg | 1-2周 | ¥3068.00 | - + |

产品描述 | ||
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 | |
纯度 | 99% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
可溶性/溶解性 | DMSO:7 mg/mL Water:<1 mg/mL Ethanol:<1 mg/mL | |
生物活性 | ||
靶点 | Chk1 ,FLT3 ,PDGFR ,GSK-3 | |
In vitro(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. | |
In vivo(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. | |
参考文献 | ||
参考文献 | [1] Tse AN, et al, Clin Cancer Res, 2007, 13(2 Pt 1), 591-602. | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
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