1. Metabolic Enzyme/Protease
  2. NAMPT
  3. GNE-617

GNE-617是新型特异的Nampt抑制剂,在A549细胞中IC50为18.9nM。

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GNE-617 Chemical Structure

GNE-617 Chemical Structure

CAS No. : 1362154-70-8

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10 mM * 1 mL in DMSO ¥920
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2 mg ¥550
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5 mg ¥900
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Other Forms of GNE-617:

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Top Publications Citing Use of Products

    GNE-617 purchased from MCE. Usage Cited in: Oncotarget. 2018 Mar 27;9(23):16451-16461.  [Abstract]

    Drug sensitivities of HCT116RFK866 and HCT116 in the colony formation assay. HCT116RFK866 and HCT116 cells are treated with 100 nM each of FK866, CHS-828, GNE-617, STF-118804, and incubated for 10 days.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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.

    IC50 & Target

    IC50: 5 nM (NAMPT)[1]

    体外研究
    (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]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (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]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    427.42

    Formula

    C21H15F2N3O3S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 16.67 mg/mL (39.00 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.3396 mL 11.6981 mL 23.3962 mL
    5 mM 0.4679 mL 2.3396 mL 4.6792 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (3.91 mM); 澄清溶液

      此方案可获得 ≥ 1.67 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 1.67 mg/mL (3.91 mM); 澄清溶液

      此方案可获得 ≥ 1.67 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.69%

    参考文献
    Kinase Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Rats[2]
    Male naïve 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    GNE-617 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3396 mL 11.6981 mL 23.3962 mL 58.4905 mL
    5 mM 0.4679 mL 2.3396 mL 4.6792 mL 11.6981 mL
    10 mM 0.2340 mL 1.1698 mL 2.3396 mL 5.8490 mL
    15 mM 0.1560 mL 0.7799 mL 1.5597 mL 3.8994 mL
    20 mM 0.1170 mL 0.5849 mL 1.1698 mL 2.9245 mL
    25 mM 0.0936 mL 0.4679 mL 0.9358 mL 2.3396 mL
    30 mM 0.0780 mL 0.3899 mL 0.7799 mL 1.9497 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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