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M3258

Chemical Structure : M3258

CAS No.: 2285330-15-4

M3258 (M 3258)

Catalog No.: PC-72402Not For Human Use, Lab Use Only.

M3258 (M 3258) is a potent, reversible, highly selective and orally acitve LMP7 inhibitor with cellular IC50 of 4.1 nM.

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    Biological Activity

    M3258 (M 3258) is a potent, reversible, highly selective and orally acitve LMP7 inhibitor with cellular IC50 of 4.1 nM.
    M3258 does not inhibit other constitutive proteasome and immunoproteasome subunits (IC50>2.5 uM).
    M3258 demonstrated strong antitumor efficacy in multiple myeloma xenograft models.
    M3258 treatment led to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells both in vitro and in vivo.
    M3258 showed superior antitumor efficacy in selected multiple myeloma and mantle cell lymphoma xenograft models compared with the approved nonselective proteasome inhibitors bortezomib and ixazomib.

    Physicochemical Properties

    M.Wt 329.159
    Formula C17H20BNO5
    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

    ((R)-2-(benzofuran-3-yl)-1-((1S,2R,4R)-7-oxabicyclo[2.2.1]heptane-2-carboxamido)ethyl)boronic acid

    References

    1. Sanderson MP, et al. Mol Cancer Ther. 2021 Aug;20(8):1378-1387.

    2. Klein M, et al. J Med Chem. 2021 Jul 22;64(14):10230-10245.

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