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Avitinib maleate

Chemical Structure : Avitinib maleate

CAS No.: 1557268-88-8

Avitinib maleate (AC-0010MA;AC0010 maleate)

Catalog No.: PC-61450Not For Human Use, Lab Use Only.

Avitinib maleate (AC-0010MA, AC0010 maleate) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M.

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

    Biological Activity

    Avitinib maleate (AC-0010MA, AC0010 maleate) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M; displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM); selectively inhibits mutant EGFR phosphorylation (IC50 =7.3 nM and 2.8 nM) in NCI-H1975 and NIH/3T3_TC32T8 cells, 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431; overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.

    Lung Cancer

    Phase 2 Clinical

    Physicochemical Properties

    M.Wt 603.611
    Formula C30H30FN7O6
    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-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate

    References

    1. Xu X, et al. Mol Cancer Ther. 2016 Nov;15(11):2586-2597.

    2. Wang W, et al. J Pharm Biomed Anal. 2017 May 30;139:205-214.

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