Drug intelligence / Profile preview

torin2

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

**Torin2** is a potent, selective, second-generation small molecule inhibitor of mammalian target of rapamycin (mTOR), functioning as an ATP-competitive antagonist with higher efficacy and selectivity compared to earlier mTOR inhibitors like Torin1. It is also a potent inhibitor of the phosphatidylinositol 3-kinase-related kinase (PIKK) family members including ATM (ataxia telangiectasia mutated), ATR (ataxia telangiectasia and Rad3-related protein), and DNA-PK (DNA-dependent protein kinase), with subnanomolar to low nanomolar activity. Preclinically, Torin2 inhibits cancer cell proliferation, induces autophagy and apoptosis in multiple tumor types including lung cancer, and demonstrates anti-angiogenic effects. The compound is used mainly for research purposes, and has been tested in models of EGFR-TKI-resistant non-small cell lung cancer, various solid tumors, and is studied for radiosensitization via DNA damage repair inhibition. Torin2 is a pyridoquinoline and an organofluorine compound[1][2][3][4][5].

Other names
1223001-51-19-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-oneDTXSID00679917DTXSID-00679917DTXSID 00679917DTXCID20630666DTXCID-20630666DTXCID 20630666
02

Targets

DNA-PK (DNA-dependent protein kinase)PIK3CA (Phosphoinositide 3-kinase alpha)mTOR (Mammalian target of rapamycin kinase)ATM (Ataxia telangiectasia mutated protein)

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