Extended Data Fig. 3: Resistance and tumor cell data.

(a) N-ethyl-N-nitrosourea (ENU) resistance screen in Ba/F3 cells dependent on HER2^YVMA. Compounds and concentrations as x-fold IC₅₀ are indicated. Bar-plot indicates absolute count for number of times the resistance allele was observed. n = 2 for BI-4142, BI-1622, Afatinib and Poziotinib. (b) Left table: Cell proliferation assay in Ba/F3 cells (parental, or dependent on HER2^YVMA or HER2^YVMA,T862A) with indicated compounds. Right table: Cell proliferation assay in Ba/F3 cells (dependent on HER2^YVMA or HER2^YVMA,L800F) with indicated compounds. All results are quoted as the geometric mean ± SEM, pIC₅₀ = -log IC₅₀ (M). The number of repeats, n, and the IC₅₀ are described in parentheses. (c) Confirmation of EGFR knockout and overexpression of exogenous EGFR variants by Western Blot in PC-9 cells. Representative image of two independent experiments. (d) Selectivity Index plot for proliferation assay in human tumor cells dependent on different oncogenic EGFR and HER2 variants in reference to EGFR^WT dependent A431 cells. Number of n repeats is described in panel e of Extended Data Fig. 3. (e) Table summarizing the cell proliferation experiments in various tumor cell lines with indicated compounds. All results are quoted as the geometric mean ± SEM, pIC₅₀ = -log IC₅₀ (M). The number of repeats, n, and the IC₅₀ are described in parentheses.

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