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M-808

Chemical Structure : M-808

CAS No.: 2377335-74-3

M-808 (M808)

Catalog No.: PC-20564Not For Human Use, Lab Use Only.

M-808 (M808) is a highly potent, selective and covalent inhibitor of menin-MLL interaction with binding IC50 of 2.6 nM, forms a covalent bond with Cys329 in menin.

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    Biological Activity

    M-808 (M808) is a highly potent, selective and covalent inhibitor of menin-MLL interaction with binding IC50 of 2.6 nM, forms a covalent bond with Cys329 in menin.
    M-808 effectively inhibits leukemia cell growth of MV4;11 and MOLM13 cell lines carrying MLL fusion with IC50 of 1 and 4 nM, respectively.
    M-808 (25 mg/kg, i.v. qD) exhibits partial tumor regression in the MV4;11 leukemia xenograft tumor model in mice, suppresses expression of HOXA9 and MEIS1 genes in MV4;11 xenograft tumors.

    Physicochemical Properties

    M.Wt 819.09
    Formula C45H63FN6O5S
    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)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-(1-((1-(4-((1-((E)-4-(piperidin-1-yl)but-2-enoyl)azetidin-3-yl)sulfonyl)phenyl)azetidin-3-yl)methyl)piperidin-4-yl)ethyl)cyclopentyl)carbamate

    References

    1. Xu S, et al. J Med Chem. 2020 May 14;63(9):4997-5010.

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