JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. It effectively reduces EGFR, Akt and ERK1/2 phosphorylation and is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer.
- Effectively inhibits cell growth and increases apoptosis, even in gefitinib-resistant H3255GR cells with an EGFR T790M mutation.
- Shows efficacy in H1975 cells expressing osimertinib-resistant mutations.
- Exhibits IC50s of 50 nM and 6 nM in Ba/F3 cell when used alone or in combination.
- Has favorable pharmacokinetic properties and good efficacy upon oral dosing.