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首页-小分子抑制剂&激动剂-Tyrosine Kinase-IGF-1R-GTX-134
GTX-134

Chemical Structure : GTX-134

CAS No.: 1356059-82-9

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GTX-134 (GTx-134, GTx134)

货号: PC-49759Not For Human Use, Lab Use Only.

GTx-134 (GTx 134) is a selective small-molecule inhibitor of IGF-1R and insulin receptor (IR) with biochemical IC50 of 97 nM and 187 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    GTx-134 (GTx 134) is a selective small-molecule inhibitor of IGF-1R and insulin receptor (IR) with biochemical IC50 of 97 nM and 187 nM, respectively.
    GTx-134 is selective for IGF-1R and closely related RTKs in a broad survey of the kinome.
    GTx-134 (1-5 uM) inhibited IGF-1 induced phosphorylation of IGF-1R and Akt in a dose-dependent manner in HMCL, MM1.S cells, equally inhibited signaling downstream of both IGF-1R and IR.
    GTx-134 inhibited the growth of genetically diverse human myeloma cell lines (HMCLs) at low micromolar level (IC50<5 uM), MM1.S, UTMC2, and H929 were most sensitive to the cytotoxic effects of GTx-134 (IC50 < 1.5 uM).
    GTx-134 showed in vitro synergies when combined with dexamethasone or lenalidomide.
    GTx-134 enhanced the activity of PD173074, a FGFR3 inhibitor, against t(4;14) myeloma cells.
    GTx-134 inhibited IGF-1R signaling and induces apoptosis of primary MM cells, GTx-134 (40 mg/kg/day, i.p.)effectively reduced tumor burden in a HMCL xenografts model.

    物理化学性质&存储条件

    分子量 648.78
    分子式 C33H40N6O6S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    2-(4-((3-(2,4-dimethylphenoxy)-2-hydroxypropyl)amino)-2-oxo-1,2-dihydropyridin-3-yl)-6-(1-(2-(methylsulfonyl)ethyl)piperidin-4-yl)-6,7-dihydroimidazo[4,5-f]isoindol-5(3H)-one

    参考文献

    1. Sheng-Ben Liang, et al. Clin Cancer Res. 2011 Jul 15;17(14):4693-704.

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