We first assessed antiproliferative activity of MTI-31 in a panel of six NSCLC cell lines, which included representative lines with oncogenic EGFR (HCC827, PC9, and H1975), c-Met (H1993), EML4-ALK (H2228), or KRAS (A549)...MTI-31 inhibited proliferation of all six NSCLC cell lines with IC50 values 0.247 ± 0.03, 0.31 ± 0.004, 0.477 ± 0.073, 0.424 ± 0.041, 0.505 ± 0.032, 0.707 ± 0.024 μmol/L, respectively...orally administrated MTI-31 strongly inhibited mTOR biomarker in vivo (Supplementary Fig. S1) and demonstrated a dose proportional antitumor efficacy in NSCLC tumors with diverse cancer-driver mutations...