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IAM1363

Chemical Structure : IAM1363

CAS No.: 3031413-24-5

IAM1363 (IAM-1363, IAM-H1, ENT-H1)

Catalog No.: PC-26757Not For Human Use, Lab Use Only.

IAM1363 (IAM-1363, IAM-H1, ENT-H1) is a potent, irreversible and selective Type II inhibitor of HER2, prevents phosphorylation and activation of wild-type HER2 and variants with activating mutations in the tyrosine kinase domain.

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    Biological Activity

    IAM1363 (IAM-1363, IAM-H1, ENT-H1) is a potent, irreversible and selective Type II inhibitor of HER2, prevents phosphorylation and activation of wild-type HER2 and variants with activating mutations in the tyrosine kinase domain.
    IAM1363 exhibits >500-fold biochemical selectivity for HER2 over EGFR and >400-fold cellular selectivity in HER2- versus EGFR-driven cell lines.
    IAM1363 effectively inhibitsHER2-dependent cell growth and survival.
    IAM1363 inhibits both wildtype HER2 and oncogenic HER2 mutants, including the recalcitrant exon 20 mutations.

    Physicochemical Properties

    M.Wt 551.66
    Formula C30H33N9O2
    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

    (E)-1-(4-(4-((4-([1,2,4]Triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)amino)pyrrolo[2,1-f][1,2,4]triazin-5-yl)piperidin-1-yl)-4-(dimethylamino)but-2-en-1-one

    References

    1. Z.J. Huang, et al. Journal of Thoracic Oncology Volume 20, Issue 10, Supplement 1, October 2025, Page S441.

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