EGFR-IN-1 TFA

EGFR-IN-1 TFA is an orally active and irreversible L858R T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR . EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity [1] .

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].

MS9427 TFA is a potent PROTAC-based EGFR degrader, exhibiting dissociation constants (Kd) of 7.1 nM for wild-type EGFR and 4.3 nM for the L858R EGFR mutation. It preferentially degrades the mutant EGFR, sparing the wild-type form, utilizing both the ubiquitin proteasome system (UPS) and the autophagy lysosome pathways. Its efficacy extends to the significant inhibition of non-small cell lung cancer (NSCLC) cell proliferation, indicating its potential utility in anticancer research [1].