GDC-0349
作者：齐岳
发布时间：2023-09-14
09:04:25
点击数：
产品名称：GDC-0349
产品描述：
| 产品描述 | GDC-0349 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. |
| 靶点活性 | mTOR:3.8 nM(Ki) |
| 体外活性 | 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] |
| 体内活性 | 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] |
| 别名 | RG-7603 |
| 分子量 | 452.55 |
| 分子式 | C24H32N6O3 |
| CAS No. | 1207360-89-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 6 mg/mL (13.25 mM)
H2O: <1 mg/mL
DMSO: 84 mg/mL (185.6 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
