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VS-II-173

Chemical Structure : VS-II-173

CAS No.: 1627962-21-3

VS-II-173 (Pim1/Pim3 inhibitor)

Catalog No.: PC-36029Not For Human Use, Lab Use Only.

VS-II-173 is a highly potent Pim1 and Pim3 inhibitor with IC50 of 70 and 20 nM respectively, and a potent and selective inducer of AML cell death (IC50=5.5 uM, Molm-13 cell).

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    Biological Activity

    VS-II-173 is a highly potent Pim1 and Pim3 inhibitor with IC50 of 70 and 20 nM respectively, and a potent and selective inducer of AML cell death (IC50=5.5 uM, Molm-13 cell).
    VS-II-173 acts synergistically with the anthracycline daunorubicin, and additively with a number of other anti-cancer drugs.
    VS-II-173 attenuates phosphorylation of Pim kinase substrates, shows towards cell lines harboring the FLT3-ITD mutation (Molm-13, FLT3-ITD heterozygous and MV4-11 FLT3-ITD homozygous) with EC50 of 2-3 uM.
    VS-II-173 also induces cell death also in AML patient blasts, including blast carrying high-risk FLT3-ITD mutation.

    Physicochemical Properties

    M.Wt 264.244
    Formula C14H8N4O2
    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

    5-nitro-3H-pyrazolo[4,3-a]phenanthridine

    References

    1. Suchaud V, et al. Bioorg Med Chem. 2014 Sep 1;22(17):4704-10.

    2. Bjørnstad R, et al. Mol Cancer Ther. 2019 Jan 24. pii: molcanther.1234.2017. doi: 10.1158/1535-7163.MCT-17-1234.

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