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MI-1481

Chemical Structure : MI-1481

CAS No.: 1887178-64-4

MI-1481 (MI1481)

Catalog No.: PC-35104Not For Human Use, Lab Use Only.

MI-1481 (MI1481) is a highly potent inhibitor of the menin-MLL1 interaction with IC50 of 3.6 nM, 10-fold increase in inhibitory activity over MI-463 and MI-503.

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    Biological Activity

    MI-1481 (MI1481) is a highly potent inhibitor of the menin-MLL1 interaction with IC50 of 3.6 nM, 10-fold increase in inhibitory activity over MI-463 and MI-503.
    MI-1481 markedly reduces cell growth of murine bone marrow cells transformed with MLL-AF9 with GI50 of 34 nM.
    MI-1481 demonstrates potent on target activity in MLL leukemia cells with GI50 values of 36 nM in MV4;11 (harboring MLL-AF4 fusion protein) and 61 nM in MOLM13 (harboring MLL-AF9).
    MI-1481 downregulates the MLL fusion protein target genes, HOXA9 and MEIS1, at 100 nMin MV4;11 human MLL leukemia cells.
    MI-1481 strongly inhibits leukemia progression in vivo.

    Physicochemical Properties

    M.Wt 597.661
    Formula C29H30F3N7O2S
    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)-4methyl-1-((5-oxomorpholin-2-yl)methyl)-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile

    References

    1. Borkin D, et al. J Med Chem. 2018 May 23. doi: 10.1021/acs.jmedchem.8b00071.

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