GDC-0349 (C007B-173128)

InformationGDC-0349 GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with K i of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.In vitroGDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes.In vivoGDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN ) and 786-O (VHL mutant).Cell Datacell lines：Concentrations：Incubation Time：Powder Purity:≥99%.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C24H32N6O3

Molecular Weight: 452.55