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  • FK866

    • 达珀利奈;Daporinad; APO866; FK-866; FK 866; APO 866; APO-866
    货号: abs812157
    CAS号: 658084-64-1
    分子式: C24H29N3O2
    分子量: 391.51
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    货号-规格 货期 价格 数量
    abs812157-10mg 现货 ¥1150.00
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    abs812157-50mg 1-2周 ¥3950.00
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    大包装询价
    产品描述
    描述

    FK866 (APO866, Daporinad)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase),无细胞试验中IC50为0.09 nM。

    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
    达珀利奈;Daporinad; APO866; FK-866; FK 866; APO 866; APO-866
    外观
    White to yellow solid
    可溶性/溶解性
    Ethanol:78 mg/mL (199.22 mM)
    生物活性
    靶点
    NMPRTase
    In vitro(体外研究)
    APO866 at low concentrations ranging from 0.09-27 nM induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia , acute lymphoblastic leukemia , mantle cell lymphoma , chronic lymphocytic leukemia , and T-cell lymphoma. APO866 at low concentrations ranging from 0-10 nM induces cell death, this effect is independent of caspase activation but is associated with depolarization of mitochondrial membrane. APO866 at concentrations ranging from 0-10 nM dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells.
    In vivo(体内研究)
    APO866 administered intraperitoneally at dose of 20 mg/kg twice a day for 4 days, repeat weekly over 3 weeks, prevents and abrogats tumor growth in C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA.
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    参考文献
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    • 实验方法 实验条件
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