Drug intelligence / Profile preview

PI-103

Development stage
Preclinical
Lead developer
UT Southwestern Medical Center
Modality
Small Molecules
01

Overview

**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].

Other names
3-(4-morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenolPhenol, 3-(4-(4-morpholinyl)pyrido(3',2':4,5)furo(3,2-d)pyrimidin-2-yl)-YQX02F616FYQX-02F616FYQX 02F616FUNII-YQX02F616FUNII-YQX-02F616FUNII-YQX 02F616FmTOR Inhibitor VPI 3-K Inhibitor VPI3-K Inhibitor VPI-3-K Inhibitor V
02

Targets

ATM (Ataxia telangiectasia mutated protein)DNA-PK (DNA-dependent protein kinase)PIK3C2A (Phosphatidylinositol 4-phosphate 3-kinase catalytic subunit type 2 alpha)PIK3C2B (PI3K-C2β)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3C3 (PI3K class III)mTOR (Mammalian target of rapamycin kinase)PIK3CA (Phosphoinositide 3-kinase alpha)

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