Notably, we observed that 4 gefitinib-resistant NSCLC cell lines, which have different resistance mechanisms (including c-Met amplification in HCC827/GR6, KRAS mutation in A549 or HCC827/GR6, and EGFR T790M/L858R mutation in H1975), were effectively inhibited by the combination treatment with GCJ-490A and gefitinib in vitro and in vivo. Here, EGFR is linked to non-small cell lung carcinoma.