JBJ-09-063 TFA

JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S mutations. It effectively reduces phosphorylation of EGFR, Akt, and ERK1/2, demonstrating efficacy in models both sensitive and resistant to EGFR tyrosine kinase inhibitors (TKI) . JBJ-09-063 TFA holds potential for research in EGFR-mutant lung cancer [1].