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

AGI-5198  (Synonyms: IDH-C35)

目錄號: HY-18082 純度: 98.57%
COA 產(chǎn)品使用指南

AGI-5198 (IDH-C35) 是有效和選擇性的突變體 IDH1R132H 抑制劑，IC50 為 0.07 μM。

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AGI-5198 Chemical Structure

AGI-5198 Chemical Structure

CAS No. : 1355326-35-0

1.  客戶無需承擔相應(yīng)的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)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   詢價  
5 g   詢價  

* Please select Quantity before adding items.

Customer Review

    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) 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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

     

    體外研究
    (In Vitro)

    TS603 神經(jīng)膠質(zhì)瘤細胞沉淀中 R-2HG 濃度的測量表明，AGI-5198 對突變體 IDH1 酶的抑制具有劑量依賴性。AGI-5198 不會損害僅表達野生型 IDH1 等位基因 (TS676 和 TS516) 的兩種源自患者的神經(jīng)膠質(zhì)瘤細胞系的集落形成[1]。IDH1 (R132H) 突變雜合的癌細胞表現(xiàn)出較少的 IDH 介導(dǎo)的 NADPH 產(chǎn)生，因此在暴露于電離輻射 (IR) 后，與IDH1野生型細胞相比，有更高水平的活性氧、DNA雙鏈斷裂和細胞死亡。IDH1 (R132H) 抑制劑 AGI-5198 可逆轉(zhuǎn)這些作用[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    AGI-5198 (450 mg/kg，po) 對人神經(jīng)膠質(zhì)瘤異種移植物的腫瘤生長產(chǎn)生 50% 至 60% 的生長抑制。來自 AGI-5198 處理的小鼠的腫瘤顯示出用針對 Ki-67 蛋白的抗體染色減少。AGI-5198 不影響 IDH1 野生型神經(jīng)膠質(zhì)瘤異種移植物的生長[1]。

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

    462.56

    Formula

    C27H31FN4O2
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗： 

    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; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.50 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.50 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      20% SBE-β-CD in Saline 的配制（4°C，儲存一周）：2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.65%

    參考文獻
    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.
    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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.

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    產(chǎn)品名稱：
    AGI-5198
    目錄號：
    HY-18082
    需求量：