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

Chemical Structure : IAM1363

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	551.66
分子式	C30H33N9O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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