PI3K/mTOR-IN-17 is a dual inhibitor that targets both PI3K and mTOR, with IC50 values of 1.21 μM and 0.21 μM, respectively. It induces apoptosis mediated by caspases and arrests cell growth in the G1 phase. The compound elevates the levels of caspases-3, 7, 8, and 9, enhances p53 expression, and increases the Bax/Bcl-2 ratio. By inhibiting the PI3K/mTOR signaling pathway, PI3K/mTOR-IN-17 is applicable in cancer research, including studies on non-small cell lung cancer (NSCLC).

PI3K:1.21 μM

PI3K/mTOR-IN-17 (Compound 8) exhibits remarkable cytotoxicity, with an IC50 of 21.13 μM against lung fibroblasts WI-38 and 1.39 μM against A549 cells, yielding a selectivity index of 15.32. At 1.39 μM for 48 hours, PI3K/mTOR-IN-17 increases the levels of p53 and Bax while decreasing Bcl-2, EGFR, PI3K, and mTOR in A549 cells. It also enhances initiator caspase-8 and 9 levels, as well as executor caspase-3 and 7. Additionally, PI3K/mTOR-IN-17 effectively induces apoptosis by arresting A549 cell growth in the G1 phase.