The results demonstrated that the combination of gefitinib and BYL719 significantly inhibited the phosphorylation of AKT, when compared with control group and gefitinib group in the EGFR mutant NSCLC cell lines with PI3K/AKT activation in 2D/3D culture and in PC-9-PIK3CA-M xenografts. Here, PIK3CB is linked to non-small cell lung carcinoma.