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pan-PIM inhibitor 17

Chemical Structure : pan-PIM inhibitor 17

CAS No.: 1681021-52-2

pan-PIM inhibitor 17

货号: PC-35943Not For Human Use, Lab Use Only.

pan-PIM inhibitor 17 is a potent, selective, orally available inhibitor of Pim kinase with IC50 of 0.8, 5.1 and 1.8 nM for Pim1, 2 and 3, respectively.

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

    生物&药学活性

    pan-PIM inhibitor 17 is a potent, selective, orally available inhibitor of Pim kinase with IC50 of 0.8, 5.1 and 1.8 nM for Pim1, 2 and 3, respectively.
    pan-PIM inhibitor 17 disaplays broad selectivity in an internal panel of 192 kinases, only eight kinases were inhibited above 50% at 1 uM.
     demonstrates cellular biomarker pS6 inhibition with EC50 of 27 nM, shows tumor growth inhibition in a KG1 tumor-bearing mouse model.

    物理化学性质&存储条件

    分子量 374.869
    分子式 C19H23ClN4O2
    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)-4-chloro-2-(4-methoxybut-1-yn-1-yl)-3-methyl-1-(piperidin-3-yl)-1H-pyrrolo[2,3-b]pyridine-6-carboxamide

    参考文献

    1. Barberis C, et al. Bioorg Med Chem Lett. 2018 Dec 10. pii: S0960-894X(18)30949-1.

    2. Barberis C, et al. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4735-4740.

    3. Guo Z, et al. Blood. 2014 Sep 11;124(11):1777-89.

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