EAI045
CAS号 | 1942114-09-1 | 货号 | BCP17698 |
中文名 | EAI045 | ||
英文名 | EAI045 | ||
中文别名 | |||
英文别名 | EAI-045;EAI 045; | ||
分子式 | C19H14FN3O3S | 分子量 | 383.4 |
生物活性 | EAI045 is an allosteric, non-ATP competitive inhibitor of mutant EGFR. In vitro studies proved that EAI045 is active and selective for T790M- harboring EGFR mutants that are in a monomer state. In vivo the combination of EAI045 and cetuximab caused a marked tumor shrinkage in a mouse model carrying the EGFR mutant with L858R/T790M/C797S. Therefore, EAI045 is the first allosteric inhibitor that targets T790M and C797S EGFR mutants but it is effective only in combination with cetuximab. | ||
信号通路 | Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway | ||
靶 点 | EGFR |
结构式
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