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pan-PIM inhibitor 17

Chemical Structure : pan-PIM inhibitor 17

CAS No.: 1681021-52-2

pan-PIM inhibitor 17

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 374.869
    Formula C19H23ClN4O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

    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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