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 EGFRL858R, EGFRT790M, EGFRL858R/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 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.Formal Name: alpha-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-isoindole-2-acetamide. CAS Number: 1942114-09-1. Molecular Formula: C19H14FN3O3S. Formula Weight: 383.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): 0.1 mg/ml. lambdamax: 203, 270 nm. SMILES: FC1=CC=C(C(C(N2CC(C=CC=C3)=C3C2=O)C(NC4=NC=CS4)=O)=C1)O. InChi Code: InChI=1S/C19H14FN3O3S/c20-12-5-6-15(24)14(9-12)16(17(25)22-19-21-7-8-27-19)23-10-11-3-1-2-4-13(11)18(23)26/h1-9,16,24H,10H2,(H,21,22,25). InChi Key: YTUFHOKUFOQRDF-UHFFFAOYSA-N.