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ETP-45658 is a small molecule, potent pan-class I phosphoinositide 3-kinase (PI3K) inhibitor that also exhibits significant activity against DNA-dependent protein kinase (DNA-PK) and the mammalian target of rapamycin (mTOR). Developed by the Experimental Therapeutics Programme at the Spanish National Cancer Research Centre (CNIO), the compound serves as a pharmacological research tool for investigating the PI3K/AKT/mTOR signaling axis. ETP-45658 demonstrates antiproliferative effects across multiple cancer cell lines, including breast and colon cancer, by inducing FOXO-dependent, p53-independent cell cycle arrest and oxidative stress. In preclinical models, it has been shown to effectively reduce Akt phosphorylation levels in vivo, though it is not currently in clinical development for human use.
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