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  • K 858

    • K858;K-858
    货号: abs810098
    CAS号: 72926-24-0
    分子式: C13H15N3O2S
    分子量: 277.34
    产品说明书
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    货号-规格 货期 价格 数量
    abs810098-10mg 1-2周 ¥800.00
    - +
    abs810098-50mg 1-2周 ¥2600.00
    - +
    大包装询价
    产品描述
    描述
    K 858 is an ATP-uncompetitive mitotic kinesin Eg5 inhibitor, which does not effect microtubule dynamics.
    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
    K858;K-858
    外观
    white to off-white powder
    可溶性/溶解性
    DMSO : 100 mg/mL (360.57 mM; Need ultrasonic)
    生物活性
    靶点
    Kinesin
    In vitro(体外研究)
    K858 Racemic is an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM. K858 does not inhibit the ATPase activity of the mitotic kinesins CENP-E and MKLP1, or the conventional kinesin heavy chain even at 200 μM. K858 induces mitotic arrest and growth inhibition via the activation of the Mad2-mediated spindle checkpoint. K858 (5 μM) induces mitotic cell death in cancer cells but not in normal cells. K858 (1, 10, 100 μM) inhibits the MCF7, BT474 and SKBR3 cell lines, and only at 10 and 100 μM suppresses MDA-MB231 cell line after treatment for 24 h. K858 incereases Bax/Bcl2 RNA ratio and survivin in the four cell lines. Furthermore, the up-regulation of survivin is totally reversed by wortmannin (phosphoinositide 3-kinase AKT) in MCF7 cells.
    In vivo(体内研究)
    K858 (50, 150 mg/kg, p.o.) shows antitumor activity in an A2780 ovarian cancer xenograft model, also inhibits tumor grwoth in a HCT116 colon cancer xenograft model via 100 mg/kg twice a day orally for 5 days. K858 (100 mg/kg, p.o., qd ×5) displays no neurotoxic side effects in mice.
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