Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
説明 | GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1. |
ターゲット&IC50 | mTOR:3.8 nM(Ki) |
In vitro | GDC-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. [1] |
In vivo | GDC-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 null) and 786-O (VHL mutant). [1] |
別名 | RG-7603 |
分子量 | 452.55 |
分子式 | C24H32N6O3 |
CAS No. | 1207360-89-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 6 mg/mL (13.25 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 84 mg/mL (185.6 mM)
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GDC-0349 1207360-89-1 Autophagy PI3K/Akt/mTOR signaling mTOR PI3K Mammalian target of Rapamycin RG-7603 inhibit RG 7603 GDC0349 RG7603 GDC 0349 Inhibitor inhibitor