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  1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. Didox

Didox  (Synonyms: NSC-324360)

目錄號: HY-19387 純度: 98.24%
COA 產(chǎn)品使用指南

Didox (NSC-324360) 是一種合成的核糖核苷酸還原酶 (ribonucleotide reductase, RR) 抑制劑。

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Didox Chemical Structure

Didox Chemical Structure

CAS No. : 69839-83-4

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Customer Review

    Didox purchased from MCE. Usage Cited in: J Ethnopharmacol. 2018 Dec 5;227:166-175.  [Abstract]

    The hepa 1c1c7 cells are treated with indicated doses of extracts along with LPS (1 μg/mL) for 24 h, and then the accumulation of nitrite from the supernatants is evaluated by Griess reagent. Didox (DI) is used as a positive control, and possessed an inhibitory rate of about 70% at 100 μM.

    Didox purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2018 Mar 20;2018:7616852.  [Abstract]

    MPP inhibits the NF-κB-dependent luciferase activity. After being cotransfected with NF-κB firefly luciferase and TK-Renilla luciferase, cells are pretreated with MPP (25?μM) or Didox (100?μM) for 1?h and cotreated with LPS (1?μg/mL) for 16?h.
    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Didox (NSC-324360) is a synthetic ribonucleotide reductase (RR) inhibitor.

    IC50 & Target

    Ribonucleotide reductase[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    RAW264.7 EC50
    82.4 μM
    Compound: Didox
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production measured after 24 hrs by Griess assay
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production measured after 24 hrs by Griess assay
    [PMID: 29517238]
    體外研究
    (In Vitro)

    Didox (NSC-324360) suppresses LPS-induced mRNA levels of iNOS, IL-6, IL-1, TNF-α, NF-κβ (p65), and p38-α, after 24 h of treatment. Treatment with Didox also suppresses the secretion of nitric oxide (NO), IL-6, and IL-10. Using mitochondrial dehydrogenase activity as a measure of cytotoxicity, the effects of Didox on cellular respiration in RAW264.7 are examined over a range of concentrations for 24 h. Cells exposures to 200 μM and below Didox, with and without LPS, do not exhibit significant cellular toxicity[1]. Didox (NSC-324360) is active against all human and murine acute myeloid leukemia (AML) lines tested with IC50 values in the low micromolar range (mean IC50 37 μM [range 25.89-52.70 μM])[2].

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

    體內(nèi)研究
    (In Vivo)

    Once engraftment is established by bioluminescent imaging, the animals receive daily administrations of Didox at 425 mg/kg via IP injection over 5 days. Didox (NSC-324360) treatment significantly reduces leukemic burden compared to vehicle treated controls (p=0.0026 and p=0.0342). More importantly, Didox (NSC-324360) provides a significant survival benefit (p<0.0001 and p=0.0094)[2].

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

    分子量

    169.13

    Formula

    C7H7NO4

    CAS 號
    性狀

    固體

    顏色

    Light yellow to khaki

    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 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實驗: 

    DMSO 中的溶解度 : 100 mg/mL (591.26 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)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 5.9126 mL 29.5631 mL 59.1261 mL
    5 mM 1.1825 mL 5.9126 mL 11.8252 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, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(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(dāng)?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(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)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: ≥ 2.75 mg/mL (16.26 mM); 澄清溶液

      此方案可獲得 ≥ 2.75 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 27.5 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: ≥ 2.75 mg/mL (16.26 mM); 澄清溶液

      此方案可獲得 ≥ 2.75 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 27.5 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。

      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

    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(jǐn)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
    參考文獻(xiàn)
    Cell Assay
    [1]

    RAW264.7 macrophages are treated with Didox alone, with 0.1 μg/mL LPS, or the two in combination. Cellular respiration, as an indication of cytotoxicity, is measured by the MTT assay, which quantifies mitochondrial dehydrogenase activity. Macrophages are plated into 96 well Costar plates at 105 cells per well in 100 μL of DMEM media. After 4 h of incubation at 37°C for adherence, compounds and DMSO carrier control (0.01% final) are added in triplicate over serial dilutions beginning with 200 μM per well in a total volume of 200 μL, and the plates incubated for 24 h. Four h before termination of the assay, each well receives 20 μL of a 5 mg/mL MTT solution in un-supplemented DMEM. After centrifugation, the supernatant for each well is discarded and cells containing reduced MTT are solubilized with 100 μL of acidified isopropanol (4 mM HCl, 0.1% NP-40 in isopropanol). Following a brief period of shaking, the optical density (O.D.) for each well is recorded at 550 nm. Each experiment is repeated three times and the data averaged from each triplicate, then expressed as percentage of the control O.D. values for each experiment[1].

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

    Animal Administration
    [2]

    Mice[2]
    Luciferase-tagged leukemia cells are transplanted into 8- week old, sublethally irradiated (4.5 Gy) C57Bl/6 mice by tail vein injection of 1.0×106 cells per mouse. Mice are injected with 150 mg/kg D-Luciferin, anesthetised with Isoflurane, and imaged using the IVIS 100 imaging system. Mice begin treatment with Didox upon detection of clear signal. The animals are treated with daily administrations of Didox (NSC-324360) at 425 mg/kg Didox by intraperitoneal injection (IP) for 5 days. Control animals receive 5% dextrose water by IP injection. Repeat imaging is performed on the day following the final treatment[2].

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

    參考文獻(xiàn)

    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, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(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 1 mM 5.9126 mL 29.5631 mL 59.1261 mL 147.8153 mL
    5 mM 1.1825 mL 5.9126 mL 11.8252 mL 29.5631 mL
    10 mM 0.5913 mL 2.9563 mL 5.9126 mL 14.7815 mL
    15 mM 0.3942 mL 1.9709 mL 3.9417 mL 9.8544 mL
    20 mM 0.2956 mL 1.4782 mL 2.9563 mL 7.3908 mL
    25 mM 0.2365 mL 1.1825 mL 2.3650 mL 5.9126 mL
    30 mM 0.1971 mL 0.9854 mL 1.9709 mL 4.9272 mL
    40 mM 0.1478 mL 0.7391 mL 1.4782 mL 3.6954 mL
    50 mM 0.1183 mL 0.5913 mL 1.1825 mL 2.9563 mL
    60 mM 0.0985 mL 0.4927 mL 0.9854 mL 2.4636 mL
    80 mM 0.0739 mL 0.3695 mL 0.7391 mL 1.8477 mL
    100 mM 0.0591 mL 0.2956 mL 0.5913 mL 1.4782 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:
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    目錄號:
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