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**PI-103** is a synthetic small molecule inhibitor of class I phosphatidylinositol 3‑kinase (PI3K), particularly the p110α isoform, and also inhibits mammalian target of rapamycin (mTOR) and DNA-dependent protein kinase (DNA-PK). It acts as a dual kinase inhibitor with potent anti-cancer properties. The compound is cell-permeable and ATP‑competitive. It has been shown to block the proliferation and survival of cancer cells in vitro and in vivo by inhibiting the PI3K/Akt/mTOR signaling pathway. While it demonstrates strong preclinical efficacy against various tumor models—including glioma and oral squamous cell carcinoma—its rapid metabolism in vivo has limited its clinical development to date. Instead, it is widely used as a research tool for studying kinase signaling pathways relevant to cancer biology[1][2][9].
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