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  • ABT-199

    促销商品
    • 维奈妥拉,Venetoclax;GDC-0199
    货号: abs810559
    CAS号: 1257044-40-8
    分子式: C45H50ClN7O7S
    分子量: 868.44
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    货号-规格 货期 价格 数量
    abs810559-5mg 现货 ¥1005.00 ¥302.00
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    abs810559-50mg 1-2周 ¥3977.00 ¥1193.00
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    大包装询价
    产品描述
    描述

    ABT-199 is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.

    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
    维奈妥拉;Venetoclax;GDC-0199
    外观
    Yellow solid
    可溶性/溶解性
    DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic)
    生物活性
    靶点
    Bcl-2 Family
    In vitro(体外研究)
    ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with Ki of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5.12-Bcl-xL cells with EC50 of 261 nM. ABT-199 induces a rapid apoptosis in RS4;11 cells with cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA. Quantitative immunoblotting reveals that sensitivity to ABT-199 correlated strongly with the expression of Bcl-2, including NHL, DLBCL, MCL, AML and ALL cell lines. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM.
    In vivo(体内研究)
    ABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts. ABT-199 also inhibits xenograft growth (DoHH2, Granta-519) as a single agent or in combination with SDX-105 and other agents.
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