1207370-33-9Relevant articles and documents
Discovery and biological profiling of potent and selective mTOR inhibitor GDC-0349
Pei, Zhonghua,Blackwood, Elizabeth,Liu, Lichuan,Malek, Shiva,Belvin, Marcia,Koehler, Michael F. T.,Ortwine, Daniel F.,Chen, Huifen,Cohen, Frederick,Kenny, Jane R.,Bergeron, Philippe,Lau, Kevin,Ly, Cuong,Zhao, Xianrui,Estrada, Anthony A.,Truong, Tom,Epler, Jennifer A.,Nonomiya, Jim,Trinh, Lan,Sideris, Steve,Lesnick, John,Bao, Linda,Vijapurkar, Ulka,Mukadam, Sophie,Tay, Suzanne,Deshmukh, Gauri,Chen, Yung-Hsiang,Ding, Xiao,Friedman, Lori S.,Lyssikatos, Joseph P.
, p. 103 - 107 (2013/02/26)
Aberrant activation of the PI3K-Akt-mTOR signaling pathway has been observed in human tumors and tumor cell lines, indicating that these protein kinases may be attractive therapeutic targets for treating cancer. Optimization of advanced lead 1 culminated in the discovery of clinical development candidate 8h, GDC-0349, a potent and selective ATP-competitive inhibitor of mTOR. GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models.