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- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
GNE-617
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1362154-70-8
- 规格：
2mg/5mg/10mg/50mg
| 规格： | 2mg | 产品价格： | ¥540.00 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ¥890.00 |
| 规格： | 10mg | 产品价格： | ¥1490.00 |
| 规格： | 50mg | 产品价格： | ¥4490.00 |
| CAS | 1362154-70-8 |
| 英文名称 | GNE-617 |
| 分子式 | C21H15F2N3O3S |
| 分子量 | 427.42 |
| 规格 | 2mg ; 5mg ; 10mg ; 50mg |
| 溶解性 | Soluble in DMSO ≥2mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| MDL | MFCD26960964 |
| SMILES | Fc1cc(F)cc(c1)S(=O)(=O)c1ccc(CNC(=O)c2ccc3nccn3c2)cc1 |
| 靶点 | Nampt |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | GNE-617是特异的Nampt抑制剂。 |
| 生物活性 | GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.[1-2] |
| IC50 | IC50: 5 nM (NAMPT)[1] |
| In Vitro | 在存在或不存在 10 μM Nicotinic Acid 的情况下，对一组 53 种非小细胞肺癌 (NSCLC) 细胞系评估了 GNE-617 盐酸盐的活性。 GNE-617 在 A549 细胞中抑制 NAMPT 的 IC50 为 18.9 nM。当通过 ATP 或总核酸的减少评估时，大多数细胞系对 GNE-617 表现出陡峭的剂量反应，并且通过同时添加 Nicotinic Acid 完全挽救细胞毒性。大多数测试的细胞系的 IC50 值低于 100 nM，大约一半的 IC50 值低于 10 nM[1]。 |
| In Vivo | 在大鼠中，与 GMX-1778 (BID 给药) 相比，GNE-617 (QD 给药) 和 GNE-875 (BID 给药) 在相似的暴露和给药持续时间下与更严重的视网膜毒性相关。使用 GNE-617、GNE-618 和 GMX-1778 进行的小鼠功效研究旨在评估功效，并适时用于评估小鼠的视网膜毒性。用 GNE-617 和 GMX-1778 观察到 NAMPTi 视网膜毒性；然而，GNE-617 和 GMX-1778 之间不同的研究持续时间不允许直接比较视网膜毒性[2]。 |
| 细胞实验 | Cells are grown in RPMI-1640 medium supplemented with 10% FBS and 2 mM glutamine and passaged not more than 20 times after thawing. To determine the IC50 values and nicotinic acid rescue status， cells are treated with nine point dose titrations of GNE-617 with or without 10 μM nicotinic acid. At 96 hours post-drug addition， the GNE-617-treated cells are evaluated using CyQUANT Direct Cell Proliferation Assay followed by CellTiter-Glo Luminescent Cell Viability Assay quantified with a Wallac EnVision 2104 Multilabel Reader. IC50 values are calculated using XLfit 5.1. To examine the protein level， cells are lysed in ice-cold radioimmunoprecipitation assay buffer， run on SDS-PAGE (4%-12% Bis-Tris)， and evaluated by Western blotting using antibodies directed against NAPRT1 and β-actin[1]. |
| 动物实验 | Rats[2] Male na?ve Sprague Dawley rats are administered once daily (QD) via oral gavage either (1) GNE-617 at 30?mg/kg for 2 consecutive days in combination with NA at 75?mg/kg twice daily (BID; 6?h apart); (2) GNE-618 at 30?mg/kg for 1 day; or (3) GMX-1778 at 30?mg/kg for 1 day. Dose selection for each compound is based on tolerability and toxicity findings from the safety studies and for nicotinic acid (NA) on the highest concentration of NA that could be administered to rats in a solution form. Formulating NA at higher concentration resulted in a suspension， and NA is determined to be unstable in a suspension form. GNE-617， GNE-618， and GMX-1778 are formulated as a solution in the vehicle of 60% polyethylene glycol (PEG 400)/10% ethanol/30% 5% dextrose in water (D5W) (vol/vol/vol)， and NA is formulated as a solution in water. At 1?h and 6.5?h post-dose (on Day 2 for GNE-617)， rats (3-4 rats per time point) are euthanized， and the blood， retina， and brain are collected. Blood samples are collected into K2EDTA Microtainer tubes. The tubes are chilled on wet ice until centrifugation within 30?min of collection. Plasma is collected and transferred to 1.2 mL cluster tubes. Tissues are rinsed with phosphate-buffered saline and blotted dry using gauze. All samples are stored at more than ?80°C until compound analysis. Results are expressed as an absolute concentration in retina， brain， or plasma and as a ratio of retina:plasma concentration. |
| 激酶实验 | For RNA interference (RNAi)， A549 cells are plated at 1，500 cells per well in 96-well plates， allowed to adhere for 24 hours， and transfected with 25 nM siRNA oligonucleotide using Dharmafect 4. Transfected cells are treated with the indicated concentrations of GNE-617 (0.1， 1 ， 10 ， 100 ， and 1000 nM) for 72 hours and viability is evaluated with CellTiter-Glo. Lysates for detection of NAPRT1 protein are collected 72 hours after transfection of 1 million A549 cells in 10 cm dishes. For NAPRT1 re-expression， RERF-LC-MS cells are transfected with pCMV6-AC.NAPRT1 and empty vector pCMV6-AC using Amaxa Nucleofector technology and selected with Geneticin[1]. |
| 数据来源文献 | [1]. Shames DS， et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23. [2]. Zabka TS， et al. Retinal toxicity， in vivo and in vitro， associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72. |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|2.3396mL|11.6981mL|23.3962mL|$$|5mM|0.4679mL|2.3396mL|4.6792mL|$$|10mM|0.234mL|1.1698mL|2.3396mL| |
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