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  • CHIR-124

    货号: abs817968
    CAS号: 405168-58-3
    分子式: C23H22ClN5O
    分子量: 419.91
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    货号-规格 货期 价格 数量
    abs817968-10mg 1-2周 ¥1658.00
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    abs817968-25mg 1-2周 ¥3068.00
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    大包装询价
    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.
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