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EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively[1].

EGFR^L858R/T790M: 42 ± 2 nM (IC₅₀); EGFR^{L858R/T790M/C797S}: 137 ± 6 nM (IC₅₀); EGFR (WT): 743 ± 20 nM (IC₅₀)

[1] Ding S, et al. Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors. Eur J Med Chem. 2022 Aug 5;238:114492. DOI:10.1016/j.ejmech.2022.114492