DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S ( IC 50 = 6.9 nM), Ba/F3-EGFR WT ( IC 50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M ( IC 50 = 5.5 nM), and Ba/F3-EML4-ALK ( IC 50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC 50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models.
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