pi3kα/mtorin1

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/mTOR-IN-18 (Compound 12) is a highly selective dual inhibitor of PI3K/mTOR. It exerts antitumor effects through competitive binding to PI3Kα (Ki=0.130 nM) and mTOR (Ki=0.111 nM). By blocking the PI3K/AKT/mTOR pathway, PI3K/mTOR-IN-18 inhibits tumor cell proliferation (IC50=144 nM) and holds potential for research in solid tumors such as breast cancer and non-small cell lung cancer.

PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR, with an IC50 of 7 nM for PI3Kα in a cell assay and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα [in a cell-free assay], respectively.