In the present study, we aimed to to investigate the mechanism of action of AZD3759 and to compare its antitumor efficacy with that of osimertinib in order to provide more non-clinical evidence for the application of AZD3759 for the treatment of NSCLC patients with brain metastases and EGFR-TKI sensitive mutations in the clinic. This evidence concerns the gene EGFR and non-small cell lung carcinoma.