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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Eukaryotic Initiation Factor (eIF)-eIF4A3-IN-1q
eIF4A3-IN-1q

Chemical Structure : eIF4A3-IN-1q

CAS No.: 2132392-89-1

eIF4A3-IN-1q

货号: PC-60161Not For Human Use, Lab Use Only.

eIF4A3-IN-1q is a potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM.

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

    生物&药学活性

    eIF4A3-IN-1q is a potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM.
    eIF4A3-IN-1q displays no activity against eIF4A1, eIF4A2, BRR2 and DHX29 (IC50>100 uM).
    eIF4A3-IN-1q upregulates SC35 1.6 kb mRNA expression by 8-fold at 3 uM and 20-fold at 10 uM, potently inhibit cell growth in HCT-116 cells (GI50=1.18 uM).
    eIF4A3-IN-1q shows antitumor efficacy and promising PK profiles in vivo, without severe body weight loss.

    物理化学性质&存储条件

    分子量 645.861
    分子式 C29H21BrClF3N4O3
    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

    (S)-5-(4-(5-bromopicolinoyl)-3-(4-chlorophenyl)piperazine-1-carbonyl)-1-phenyl-3-(trifluoromethyl)pyridin-2(1H)-one

    参考文献

    1. Mizojiri R, et al. ACS Med Chem Lett. 2017 Sep 8;8(10):1077-1082.

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