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MET inhibitor Compound 1

Chemical Structure : MET inhibitor Compound 1

CAS No.: 1208248-23-0

MET inhibitor Compound 1 (c-Met-IN-16)

Catalog No.: PC-60929Not For Human Use, Lab Use Only.

MET inhibitor Compound 1 is a potent, selective orally bioavailable MET tyrosine kinase inhibitor with IC50 of <1 nM and 12 nM for unphosphorylated and phosphorylaed MET, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    MET inhibitor Compound 1 is a potent, selective orally bioavailable MET tyrosine kinase inhibitor with IC50 of <1 nM and 12 nM for unphosphorylated and phosphorylaed MET, respectively.
    MET inhibitor Compound 1 demonstrates potent, broad spectrum activity against MET mutants (V1110I, H1112Y, L1195V, Y1235D, D1228H and M1250T) with IC50 of <1 nM-57 nM, and Y1230 mutants with moderate potency (IC50=25-280 nM).
    MET inhibitor Compound 1 displays >50-fold selectivity in a panel of 130 kinases with exception of Fms and TrkA/B/C.
    MET inhibitor Compound 1 inhibits MET-dependent tumor cell growth in vivo through decreasing phosphorylaed MET.

    Physicochemical Properties

    M.Wt 449.426
    Formula C21H17F2N9O
    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

    N-(6-(difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)methyl)imidazo[1,2-b]pyridazin-2-yl)cyclopropanecarboxamide

    References

    1. Farrell PJ, et al. Mol Cancer Ther. 2017 Jul;16(7):1269-1278.

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