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].