5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology

Phosphoinositide 3-kinase (PI3K) is deregulated in a wide variety of human tumors and triggers activation of protein kinase B (PKB/Akt) and mammalian target of rapamycin (mTOR). Here we describe the preclinical characterization of compound 1 (PQR309, bimiralisib), a potent 4,6-dimorpholino-1,3,5-tri...

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Vydáno v:J Med Chem
Hlavní autoři: Beaufils, Florent, Cmiljanovic, Natasa, Cmiljanovic, Vladimir, Bohnacker, Thomas, Melone, Anna, Marone, Romina, Jackson, Eileen, Zhang, Xuxiao, Sele, Alexander, Borsari, Chiara, Mestan, Jürgen, Hebeisen, Paul, Hillmann, Petra, Giese, Bernd, Zvelebil, Marketa, Fabbro, Doriano, Williams, Roger L., Rageot, Denise, Wymann, Matthias P.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2017
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Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC5656176/
https://ncbi.nlm.nih.gov/pubmed/28829592
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b00930
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