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Synonyms | RG-7603 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H32N6O3 |
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分子量 | 452.55 | CAS No. | 1207360-89-1 | |
Solubility (25°C)* | 体外 | DMSO | 91 mg/mL (201.08 mM) | |
Ethanol | 6 mg/mL (13.25 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | 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. |
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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] |
動物実験 | 動物モデル | MCF7-neo/Her2 tumor xenograft |
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投薬量 | 10, 20, 30, 40,50, 60, 70, 80 mg/kg | |
投与方法 | orally |
Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 477(2):174-80.]
Phosphorylation of REPS1 at Ser709 by RSK attenuates the recycling of transferrin receptor [ BMB Rep, 2021, 54(5):272-277] | PubMed: 33407999 |
Deubiquitinase OTUD5 is a positive regulator of mTORC1 and mTORC2 signaling pathways [ Cell Death Differ, 2020, 10.1038/s41418-020-00649-z] | PubMed: 33110214 |
Autophagy induction contributes to GDC-0349 resistance in head and neck squamous cell carcinoma (HNSCC) cells [Zhou Y, et al. Biochem Biophys Res Commun, 2016, 477(2):174-80] | PubMed: 27291151 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。