Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNE-317 是一种可透过血脑屏障 (BBB)的 PI3K/mTOR 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 297 | 现货 | ||
2 mg | ¥ 422 | 现货 | ||
5 mg | ¥ 722 | 现货 | ||
10 mg | ¥ 1,130 | 现货 | ||
25 mg | ¥ 2,180 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,320 | 现货 | ||
200 mg | ¥ 6,120 | 现货 | ||
500 mg | ¥ 8,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 761 | 现货 |
产品描述 | GNE-317, a PI3K/mTOR inhibitor, can pass through the blood-brain barrier (BBB). |
体外活性 | GNE-317, an oxetane derivative synthesized by GDC-0980, is aimed at reducing substrate affinity for efflux transporters. In vitro, GDC-0980 demonstrate similar profiles with GNE-317 in MTS cytotoxicity experiments using the GL261 cell line. |
体内活性 | Mice, which are i.c. inoculation with GL261-GFP-Luc cells Seven days later,are treated once daily with the maximum tolerated dose of GDC-0980 (7.5 mg/kg), GNE-317 (30 mg/kg), or vehicle. Tumor growth is tracked in GL261 through bioluminescence imaging on a weekly basis. There are no significant differences in GL261 tumor growth among the 3 groups treated by GDC-0980, GNE-317 or vehicle. The data show that the drugs have limited efficacy in inducing cell death in the GL261 cell line. Although GNE-317 has greater delivery and enhanced therapeutic targeting efficacy, it is not effective in the treatment of the GL261 tumor. |
细胞实验 | Cellular viability assays are set up in a 96-well format with 2000 GL261-GFP-Luc cells plated per well in the culture conditions. GL261, an aggressive C57BL/6J-derived glioma line, is transfected with both green fluorescent protein (GFP) and luciferase (Luc) from separate plasmids.GL261-GFP-Luc cells are cultured in Dulbecco's modified Eagle's medium supplemented with 10% FBS and Penicillin/Streptomycin (100 U/mL) at 5% oxygen, and are selected by 4 mg/mL Puromycin and 4 mg/mL G418. Suspend GNE-317 in DMSO and then diluted with the medium.GL261-GFP-Luc cells are incubated in the presence of drug or vehicle for 48 hours, and viability was assessed by MTS assay. Results were detected using a Synergy Mx automated plate reader,which are set up absorbance at 490 nm and used to determine viability and at 650 nm to account for the background. Numerical values from drug-treated wells are normalized to the values of vehicle-treated wells to yield percent survival. |
动物实验 | 7-week-old C57BL/6J mice are implanted GL261-GFP-Luc cells. When tumors reach 5e7 photons/s/cm2/sr (radiance), mice are orally administered the maximum tolerated the dose,which is defined as <10% drop in mice bodyweight dose, GDC-0980 for 7.5 mg/kg, GNE-317 for 30 mg/kg or vehicle once daily for 3 days. At 1 or 6 hours after the third dose, mice are euthanized with carbon dioxide and perfused with 30 mL PBS. |
别名 | GNE317 |
分子量 | 414.48 |
分子式 | C19H22N6O3S |
CAS No. | 1394076-92-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12.5 mg/mL (30.16 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4127 mL | 12.0633 mL | 24.1266 mL | 60.3165 mL |
5 mM | 0.4825 mL | 2.4127 mL | 4.8253 mL | 12.0633 mL | |
10 mM | 0.2413 mL | 1.2063 mL | 2.4127 mL | 6.0317 mL | |
20 mM | 0.1206 mL | 0.6032 mL | 1.2063 mL | 3.0158 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。
GNE-317 1394076-92-6 PI3K/Akt/mTOR signaling PI3K mTOR inhibit Inhibitor Phosphoinositide 3-kinase Mammalian target of Rapamycin GNE 317 GNE317 inhibitor