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  • GSK-923295

    • GSK-923295,GSK923295
    货号: abs810313
    CAS号: 1088965-37-0
    分子式: C32H38ClN5O4
    分子量: 592.13
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810313-5mg 1-2周 ¥1274.00
    - +
    abs810313-10mg 1-2周 ¥1996.00
    - +
    abs810313-50mg 1-2周 ¥7047.00
    - +
    abs810313-100mg 1-2周 ¥13340.00
    - +
    大包装询价
    产品描述
    描述
    GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. Phase 1.
    纯度
    >98%
    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
    别名
    GSK-923295,GSK923295
    外观
    Powder
    可溶性/溶解性

    DMSO 100 mg/mL (168.88 mM)

    Ethanol 100 mg/mL (168.88 mM)




    生物活性
    靶点
    CENP-E
    In vitro(体外研究)
    GSK923295 is the first potent and selective inhibitor of the mitotic kinesin centromere-associated protein-E (CENP-E). GSK923295 is uncompetitive with both ATP and microtubules (MT), inhibiting CENP-E MT-stimulated ATPase activity with a Ki of 3.2 nM, highly selective over other kinesins. GSK923295 inhibits release of inorganic phosphate and stabilizes CENP-E motor domain interaction with microtubules, reduces the rate of ATP-promoted dissociation of CENP-E from MT (koff, MT) by more than 50-fold. GSK923295 causes failure of metaphase chromosome alignment and induces mitotic arrest. GSK923295 is a potent inhibitor of tumor cell growth, with an average GI50 of 253 nM and a median GI50 of 32 nM for 237 tumor cell lines. GSK923295 inhibits tumor cell growth more effectively when mitogen-activated protein kinase (MEK/ERK) signaling is also inhibited.
    In vivo(体内研究)
    GSK923295 produces clear increases in the abundance of mitotic figures and scattered apoptotic bodies in tumors. GSK923295 causes a dose-dependent increase in the ratio of 4n to 2n nuclei. GSK923295 exhibits robust, dose-dependent antitumor activity against Colo205 xenografts, including partial and complete regressions at the 125 mg/kg dose. GSK923295 demonstrates significant antitumor activity against solid tumor models, inducing CRs in Ewing sarcoma, rhabdoid, and rhabdomyosarcoma xenografts, may be a valuable therapeutic target in pediatric cancer.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
    • 实验方法 实验条件
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