Cayman EAI045

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 EGFR^L858R, EGFR^T790M, EGFR^L858R/T790M, and wild-type EGFR, respectively). 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 EGFR^L858R/T790M and EGFR^{L858R/T790M/I941R}. In vivo, EAI045 induces tumor regression and reduces EGFR signaling in mice bearing EGFR^L858R/T790M, EGFR^{Exon19del/T790M}, and EGFR^{L858R/T790M/C797S} tumors when administered at a dose of 60 mg/kg per day in combination with cetuximab.

WARNING This product is not for human or veterinary use.