Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GDC-0349 (RG-7603) 是一种ATP 竞争性的选择性mTOR 抑制剂,Ki 值为 3.8 nM。它对 PI3Kα 和其他 266 种激酶的抑制作用是 790 倍,可抑制mTORC1和mTORC2复合体。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 392 | 现货 | ||
2 mg | ¥ 563 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,660 | 现货 | ||
25 mg | ¥ 3,590 | 现货 | ||
50 mg | ¥ 4,980 | 现货 | ||
100 mg | ¥ 6,950 | 现货 | ||
500 mg | ¥ 13,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 973 | 现货 |
产品描述 | 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. |
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 |
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)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.2097 mL | 11.0485 mL | 22.097 mL | 55.2425 mL |
5 mM | 0.4419 mL | 2.2097 mL | 4.4194 mL | 11.0485 mL | |
10 mM | 0.221 mL | 1.1049 mL | 2.2097 mL | 5.5243 mL | |
DMSO | 20 mM | 0.1105 mL | 0.5524 mL | 1.1049 mL | 2.7621 mL |
50 mM | 0.0442 mL | 0.221 mL | 0.4419 mL | 1.1049 mL | |
100 mM | 0.0221 mL | 0.1105 mL | 0.221 mL | 0.5524 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GDC-0349 1207360-89-1 Autophagy PI3K/Akt/mTOR signaling PI3K mTOR Mammalian target of Rapamycin RG-7603 inhibit RG 7603 GDC0349 RG7603 GDC 0349 Inhibitor inhibitor