GDC-0349

GDC-0349 is a potent and selective ATP-competitive small molecule inhibitor of the mammalian target of rapamycin (mTOR), with a Ki of 3.8 nM and high selectivity over PI3Kα and other kinases[1][5][8]. It inhibits both mTORC1 and mTORC2 complexes by binding to the kinase domain of mTOR. This inhibition leads to reduced phosphorylation of downstream targets such as Akt (Ser473) and 4EBP1, resulting in decreased tumor cell proliferation and increased apoptosis[8]. GDC-0349 has demonstrated dose-dependent antitumor efficacy in various xenograft cancer models. It has been investigated primarily for the treatment of solid tumors and Non-Hodgkin's lymphoma in early-phase clinical trials[2][3].

Other names

(S)-1-ethyl-3-(4-(4-(3-methylmorpholino)-7-(oxetan-3-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)phenyl)urea