Drug intelligence / Profile preview

ETP-45658

Development stage
Discontinued
Lead developer
Spanish National Cancer Centre
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

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.

Other names
CAS 1198357-79-7CAS1198357-79-7CAS-1198357-79-7
02

Targets

PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)DNA-PK (DNA-dependent protein kinase)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)mTOR (Mammalian target of rapamycin kinase)

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