2-(5-氟-2-羟基苯基)-2-(1-氧代异吲哚啉-2-基)-N-(噻唑-2-基)乙酰胺

• 英文名称：

• EAI-045

• CAS号：

• 1942114-09-1

• 分子式：

• C19H14FN3O3S

• 分子量：

• 383.4

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.