2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. AGI-5198

AGI-5198  (Synonyms: IDH-C35)

目录号: HY-18082 纯度: 98.19%
COA 产品使用指南

摩尔计算器

AGI-5198 (IDH-C35) 是有效和选择性的突变体 IDH1R132H 抑制剂，IC50 为 0.07 μM。

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AGI-5198 Chemical Structure

AGI-5198 Chemical Structure

CAS No. : 1355326-35-0

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3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥375
In-stock
10 mg ￥600
In-stock
50 mg ￥900
In-stock
100 mg ￥1500
In-stock
200 mg ￥2500
In-stock
500 mg ￥5500
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

AGI-5198 相关抗体

Top Publications Citing Use of Products

    AGI-5198 purchased from MCE. Usage Cited in: Cancer Res. 2018 Nov 15;78(22):6386-6398.  [Abstract]

    IDH1R132H-mediated epigenetic silencing of TSGs is inhibited by cyclin F.

    AGI-5198 purchased from MCE. Usage Cited in: FASEB J. 2018 Jun 7:fj201800547R.  [Abstract]

    Representative photomicrographs of cells that are plated on glass coverslips in the presence or absence of 1μM AGI-5198, treated with 5 or 10μM Cisplatin for 1 h, and fixed after 30 min. γ-H2AX is stained immunocytochemically (red) to demonstrate DNA DSBs and with DAPI (blue) to demonstrate DNA nucleus content.

    AGI-5198 purchased from MCE. Usage Cited in: J Neurooncol. 2018 Jun;138(2):241-250.  [Abstract]

    LN18 IDH1 R132H cells are either treated with vehicle (DMSO) or 1 μM AG-5198 for the indicated number of days. Cells are harvested and Fn14, PAR-4 and GAPDH levels are evaluated by Western blot analysis.

    查看 Isocitrate Dehydrogenase (IDH) 亚型特异性产品:

    查看所有亚型
    IDH1 IDH2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AGI-5198 (IDH-C35) is a potent and selective mutant IDH1R132H inhibitor with an IC50 of 0.07 μM.

    IC50 & Target

    IDH1

     

    体外研究
    (In Vitro)

    TS603 神经胶质瘤细胞沉淀中 R-2HG 浓度的测量表明，AGI-5198 对突变体 IDH1 酶的抑制具有剂量依赖性。AGI-5198 不会损害仅表达野生型 IDH1 等位基因 (TS676 和 TS516) 的两种源自患者的神经胶质瘤细胞系的集落形成[1]。IDH1 (R132H) 突变杂合的癌细胞表现出较少的 IDH 介导的 NADPH 产生，因此在暴露于电离辐射 (IR) 后，与IDH1野生型细胞相比，有更高水平的活性氧、DNA双链断裂和细胞死亡。IDH1 (R132H) 抑制剂 AGI-5198 可逆转这些作用[2]。

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

    AGI-5198 相关抗体:
    体内研究
    (In Vivo)

    AGI-5198 (450 mg/kg，po) 对人神经胶质瘤异种移植物的肿瘤生长产生 50% 至 60% 的生长抑制。来自 AGI-5198 处理的小鼠的肿瘤显示出用针对 Ki-67 蛋白的抗体染色减少。AGI-5198 不影响 IDH1 野生型神经胶质瘤异种移植物的生长[1]。

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

    462.56

    Formula

    C27H31FN4O2
    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: 

    DMF 中的溶解度 : ≥ 50 mg/mL (108.09 mM)

    DMSO 中的溶解度 : 20.83 mg/mL (45.03 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)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1619 mL 10.8094 mL 21.6188 mL
    5 mM 0.4324 mL 2.1619 mL 4.3238 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: ≥ 2.08 mg/mL (4.50 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 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% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.50 mM); 悬浊液; 超声助溶

      此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    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

    只
    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: 99.65%

    COA (197 KB) HNMR (206 KB) LCMS (241 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    Inhibitory potency against the IDH2 R140Q and IDH2 R172K enzymes is determined in an endpoint assay in which the amount of NADPH remaining at the end of the reaction is measured by the addition of a large excess of diaphorase and resazurin. IDH2 R140Q is diluted to 0.25 μg/mL in 40 μL 1X Assay Buffer (150 mM NaCl, 50 mM potassium phosphate pH 7.5, 10 mM MgCl2, 10% glycerol, 2 mM B-ME, 0.03% BSA) and incubated for 16 hours at 25°C in the presence of 1 μL of compound in DMSO. The reaction is started with the addition of 10 μL of Substrate Mix (20 μM NADPH, 8 μM alpha-ketoglutarate, in 1X Assay Buffer) and incubated for 1 hour at 25°C. Then, remaining NADPH is measured by the addition of 25 μL of Detection Mix (36 μg/mL diaphorase, 18 μM resazurin in 1X Assay buffer), incubated for 5 minutes at 25°C, and read as described above. IDH2 R172K is assayed as for IDH2 R140Q with the following modifications: 1.25 μg/mL of protein is used, the Substrate Mix contained 50 μM NADPH and 6.4 μM alpha-ketoglutarate, and the compound is incubated for 1 hour before starting the reaction.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    TS603 cells are grown in medium containing either AGI-5198 (1.5μM) or DMSO vehicle control. One week prior to harvest cells are ransferred to differentiation medium (DMEM F12; 15 mM HEPES; 0.06% glucose; B27 without vitamin A; N2; Insulin/transferrin; 1% FBS) containing freshly added retinoic acid (1μM). ChIP of non-crosslinked cells is then carried out using established ChIP methods. 350 μg of lysate is immunoprecipitated-using anti-H3K9Me3, H3K27me3 or Rabbit Control IgG. After washing, ChIP DNA is eluted from protein G beads and analyzed by RT-PCR using SYBR green. Relative occupancy is calculated using the standard curve method and fold enrichment versus IgG. Enrichment in AGI- 5198-treated cells is normalized to vehicle control. Means and standard deviation are calculated from 4 technical replicates.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    SCID mice are injected subcutaneously with 106 glioma cells, which are suspended in 100 μL of a 50:50 mixture of growth media and Matrigel. Once tumors have reached a measurable size, mice are randomized into the indicated treatment groups.

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

    AGI-5198 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 / DMF 1 mM 2.1619 mL 10.8094 mL 21.6188 mL 54.0470 mL
    5 mM 0.4324 mL 2.1619 mL 4.3238 mL 10.8094 mL
    10 mM 0.2162 mL 1.0809 mL 2.1619 mL 5.4047 mL
    15 mM 0.1441 mL 0.7206 mL 1.4413 mL 3.6031 mL
    20 mM 0.1081 mL 0.5405 mL 1.0809 mL 2.7024 mL
    25 mM 0.0865 mL 0.4324 mL 0.8648 mL 2.1619 mL
    30 mM 0.0721 mL 0.3603 mL 0.7206 mL 1.8016 mL
    40 mM 0.0540 mL 0.2702 mL 0.5405 mL 1.3512 mL
    DMF 50 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0809 mL
    60 mM 0.0360 mL 0.1802 mL 0.3603 mL 0.9008 mL
    80 mM 0.0270 mL 0.1351 mL 0.2702 mL 0.6756 mL
    100 mM 0.0216 mL 0.1081 mL 0.2162 mL 0.5405 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      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.

    Keywords:

    AGI-51981355326-35-0IDH-C35AGI5198AGI 5198Isocitrate Dehydrogenase (IDH)Inhibitorinhibitorinhibit

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