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  • SGI-1776

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    • SGI 1776;SGI1776
    货号: abs812211
    CAS号: 1025065-69-3
    分子式: C20H22F3N5O
    分子量: 405.42
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs812211-5mg 现货 ¥1158.00 ¥347.00
    - +
    abs812211-10mg 现货 ¥2062.00 ¥619.00
    - +
    abs812211-50mg 现货 ¥5348.00 ¥1604.00
    - +
    大包装询价
    产品描述
    描述

    SGI-1776  is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. 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
    SGI 1776;SGI1776
    外观
    White to yellow powder
    可溶性/溶解性
    DMSO : 75 mg/mL (185 mM)

    Ethanol : 75 mg/mL (185 mM)
    生物活性
    靶点
    Pim1;FLT3;Pim3;Pim2
    In vitro(体外研究)
    In addition to Pim, SGI-1776 also potently targets FLT3 (IC50 = 44nM). Treatment of AML cells with SGI-1776 results in a concentration-dependent induction of apoptosis. Importantly, SGI-1776 is also cytotoxic in AML primary cells, irrespective of FLT3 mutation status and results in Mcl-1 protein decline. Treatment of CLL cells with SGI-1776 results in a concentration-dependent induction of apoptosis. SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction. Apoptosis induction coupled with the inhibition of RNA synthesis is observed in CLL cells treated with SGI-1776. SGI-1776 exhibites cytotoxic activity in vitro with a median relative IC50 of 3.1 mM. SGI-1776 induces tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induces complete responses of subcutaneous MV4;11.
    In vivo(体内研究)
    Consistent with cell line data, xenograft model studies with mice bearing MV-4-11 tumors shows efficacy with SGI-1776. SGI-1776 has shown preclinical activity against leukemia and solid tumor cell line models with IC50 values of 0.005–11.68 mM. SGI-1776 induces significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts.
    参考文献
    参考文献
    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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