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M-525

Chemical Structure : M-525

CAS No.: 2173582-08-4

M-525 (M525)

Catalog No.: PC-62486Not For Human Use, Lab Use Only.

M-525 is a first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction with binding IC50 of 3.3 nM in FP assays.

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    Biological Activity

    M-525 is a first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction with binding IC50 of 3.3 nM in FP assays.
    M-525 inhibits MV4;11 (MLL fusion) and HL60 (No MLL fusion) cell growth with IC50 of 2.7 and 2,000 nM, respectively.
    M-525 significantly down-regulates the expression of MEIS1, HOXA9 and HOXA11 genes in a dosedependent anner at ow nanomolar concentrations.
    M-525 also effectively suppresses the expression of MEIS1 and HOX genes in the MOLM-13 cell line at 3 nM.

    Physicochemical Properties

    M.Wt 734.932
    Formula C39H51FN6O5S
    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

    methyl ((1S,2R)-2-((S)-cyano(1-((1-(4-((1-((E)-4-(dimethylamino)but-2-enoyl)azetidin-3-yl)sulfonyl)phenyl)azetidin-3-yl)methyl)piperidin-4-yl)(3-fluorophenyl)methyl)cyclopentyl)carbamate

    References

    1. Xu S, et al. Angew Chem Int Ed Engl. 2018 Feb 5;57(6):1601-1605.

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