2922402-03-5

EGFR kinase inhibitor 3 (compound 2) is a bivalent ATP-allosteric EGFR kinase inhibitor with IC50s of <10 nM, 1.5 nM, 0.059 nM, 0.064 nM for WT EGFR, EGFR-activating mutations L858R, L858R/T790M and L858R/T790M/C797S, respectively. EGFR kinase inhibitor 3 is a C-linked inhibitor[1].

EGFR (WT): <10 nM (IC₅₀); EGFR L858R: 1.5 nM (IC₅₀); EGFR L858R/T790M: 0.059 nM (IC₅₀); EGFR L858R/T790M/C797S: 0.064 nM (IC₅₀)

[1] Florian Wittlinger, et al. Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors. Commun Chem. 2024 Feb 20;7(1):38. DOI:10.1038/s42004-024-01108-3