产品描述:
EAI045 is a potent and selective inhibitor of mutant EGF receptors (EGFRs; IC50s = 0.076, 0.049, 0.002, and 1.6 μM for recombinant EGFRL858R, EGFRT790M, EGFRL858R/T790M, and wild-type EGFR, respectively).{31376} It inhibits phosphorylation of EGFR in a concentration-dependent manner in H1975 cells. EAI045 (0.01-10 μM) reduces proliferation of Ba/F3 cells expressing EGFRL858R/T790M and EGFRL858R/T790M/I941R. In vivo, EAI045 induces tumor regression and reduces EGFR signaling in mice bearing EGFRL858R/T790M, EGFRExon19del/T790M, and EGFRL858R/T790M/C797S tumors when administered at a dose of 60 mg/kg per day in combination with cetuximab.