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XMU-MP-5

Chemical Structure : XMU-MP-5

CAS No.:

XMU-MP-5

Catalog No.: PC-38244Not For Human Use, Lab Use Only.

XMU-MP-5 is a new-generation potent and selective ALK inhibitor (IC50=4.15 nM) to overcome crizotinib resistance mutations, including L1196M and G1202R.

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    Biological Activity

    XMU-MP-5 is a new-generation potent and selective ALK inhibitor (IC50=4.15 nM) to overcome crizotinib resistance mutations, including L1196M and G1202R.
    XMU-MP-5 significantly induced apoptosis in EML4-ALK Ba/F3 cells did not affect apoptosis in wild-type Ba/F3 cells.
    XMU-MP-5 shows highest binding affinities for ALK and its mutants ALK(C1156Y) and ALK(L1196M), with K d values of 0.57, 0.4, and 0.77 nM, respectively.
    XMU-MP-5 blocks ALK signaling pathways and inhibits the proliferation of cells harboring either wild-type or mutant EML4-ALK in vitro and suppresses tumor growth in xenograft mouse models in vivo.
    XMU-MP-5 induces significant regression of lung tumors in two genetically engineered mouse (GEM) models.

    Physicochemical Properties

    M.Wt 563.677
    Formula C28H33N7O4S
    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

    2-(dimethylamino)-1-(6-((4-((2-(isopropylsulfonyl)phenyl)amino)-5H-pyrrolo[3,2-d]pyrimidin-2-yl)amino)-5-methoxyindolin-1-yl)ethan-1-one

    References

    1. Yue Lu, et al. EMBO Mol Med. 2022 Jan 11;14(1):e14296.

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