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. 2020 Dec 13;14(2):100961. doi: 10.1016/j.tranon.2020.100961

Fig. 2.

Fig. 2

BEBT-109 selectively suppresses EGFR TKI-sensitive mutants in vitro.A-D, In comparison with osimertinib, BEBT-109 exhibited greater potency in reducing the viability of cells harboring TKI-sensitive mutants(Del19, G719A and L861Q) (A and B) (n = 3), while having less activity against EGFR wild-type H460 cells and EGFR-deficiency Ba/F3 cells (C and D) (n = 2), as assessed by use of CellTiter-GLO assay after 3 days of treatment. E, IC50 values of BEBT-109 and osimertinib for EGFR wild-type cells (n = 2), EGFR-deficient Ba/F3 cells (n = 2) and mutant EGFR-expressing cells (n = 3). F, PC-9 cells (Del19) and Ba/F3 cells expressing EGFR G719A were treated with the indicated concentrations of BEBT-109 and osimertinib for 6 h. Phosphorylation of EGFR and its downstream signaling substrates were evaluated by western blotting with the indicated antibodies.