PI3K/mTOR-IN-22 

PI3K/mTOR-IN-22 is an orally active PI3K/mTOR kinase dual inhibitor with IC₅₀ values of 400.5 nM and 8.2 nM. PI3K/mTOR-IN-22 downregulates phosphorylation of the AKT and mTOR, upregulates pro-apoptotic proteins Bax and caspase-3 and downregulates anti-apoptotic protein Bcl-2. PI3K/mTOR-IN-22 exhibits antiproliferative activity against cancer cells, induces apoptosis and ROS production, and reduces mitochondrial membrane potential. PI3K/mTOR-IN-22 exhibits antitumor activity in breast cancer mice models^[1].

PI3K/mTOR-IN-22 (Compound J-33) is a selective dual inhibitor of PI3K and mTOR kinases, with an IC₅₀ of 400.5 nM for PI3Kα and 8.2 nM for mTOR, and forms stable binding interactions with both kinases^[1].
PI3K/mTOR-IN-22 potently inhibits proliferation of MCF-7 human breast cancer cells with an IC₅₀ of 1.5 μM, and also inhibits proliferation of H1975, H460, PC-9 cells with IC₅₀ values of 10.7, 2.3 and 13.5 μM^[1].
PI3K/mTOR-IN-22 (256 μg/mL) exhibits low hemolytic toxicity in sheep erythrocytes, with a hemolysis rate of 2.60%^[1].
PI3K/mTOR-IN-22 (0.75-1.50 μM; 6-12 h) induces concentration-dependent apoptosis in MCF-7 human breast cancer cells, reduces mitochondrial membrane potential and increases intracellular ROS levels^[1].
PI3K/mTOR-IN-22 (0.75-1.50 μM; 24 h) dose-dependently inhibits migration of MCF-7 human breast cancer cells in vitro, as shown by the wound healing assay^[1].
PI3K/mTOR-IN-22 (0.19-3.00 μM; 14 days) dose-dependently inhibits clonogenicity of MCF-7 human breast cancer cells^[1].
PI3K/mTOR-IN-22 (0.75-6.00 μM) dose-dependently downregulates phosphorylation of AKT and mTOR in MCF-7 human breast cancer cells, inhibiting the PI3K-AKT-mTOR signaling pathway^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PI3K/mTOR-IN-22 (Compound J-33) (75 mg/kg; p.o.; every other day; 23 days) exhibits potent in vivo antitumor activity in BALB/c nude mice bearing MCF-7 xenografts, achieving a 44.9% tumor inhibition rate^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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• [1]. Cheng Z, et al. Discovery of novel bis-aryl urea-linked triazine derivatives as dual PI3K/mTOR inhibitors via scaffold hopping strategy and biological activity evaluations. Eur J Med Chem. 2026;311:118856.