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  1. PROTAC Apoptosis Autophagy
  2. Autophagy Apoptosis Ligands for E3 Ligase
  3. Thalidomide

Thalidomide  (Synonyms: 沙利度胺)

目錄號: HY-14658 純度: 99.92%
COA 產(chǎn)品使用指南

Thalidomide 能夠抑制 cereblon (cullin-4 E3 泛素連接酶復合物 CUL4-RBX1-DDB1 的一部分),Kd 值約為 250 nM,具有免疫調(diào)節(jié)、抗炎、抗腫瘤作用。Thalidomide 可以作為分子膠來增強底物。

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Thalidomide Chemical Structure

Thalidomide Chemical Structure

CAS No. : 50-35-1

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥616
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200 mg ¥560
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500 mg ¥1000
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5 g   詢價  

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Customer Review

Other Forms of Thalidomide:

    Thalidomide purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    Kelly cells are treated with increasing concentrations of Thalidomide and co-treated with 5 μM Bortezomib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Thalidomide purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    H9 hESC are treated with increasing concentrations of Thalidomide, Lenalidomide, Pomalidomide, or DMSO as a control. Following 24 h of incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Thalidomide purchased from MCE. Usage Cited in: Nat Commun. 2017 May 22;8:15398.  [Abstract]

    HEK293T cells are treated with 50 μg/mL Cycloheximide and increasing concentrations of Lenalidomide, Thalidomide or with DMSO, and cells are incubated for 6?h. ZFP91 and GAPDH levels are detected using anti-ZFP91 or anti-GAPDH immunoblotting.

    查看 Ligands for E3 Ligase 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

    Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

    IC50 & Target

    Cereblon

     

    體外研究
    (In Vitro)

    Thalidomide 具有免疫調(diào)節(jié)、抗炎和抗血管生成的癌癥特性,靶向 cereblon (CRBN),這是 cuLlin-4 E3 泛素連接酶復合物 CuL4-RBX1-DDB1 的一部分,Kd 為~250 nM[1]
    Thalidomide (50 μg/mL) 增強 Icotinib 對 PC9 和 A549 細胞增殖的抗腫瘤活性,這種作用與細胞凋亡和細胞遷移相關。此外,Thalidomide 和 Icotinib 抑制 PC9 細胞中的 EGFR 和 VEGF-R2 通路[3]

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

    體內(nèi)研究
    (In Vivo)

    Thalidomide (100 mg/kg,口服) 抑制膠原蛋白沉積,下調(diào) α-SMA 和膠原蛋白 I 的 mRNA 表達水平,并顯著降低 RILF 小鼠的促炎細胞因子。Thalidomide 通過抑制 ROS 和下調(diào)依賴于 Nrf2 狀態(tài)的 TGF-β/Smad 通路來減輕 RILF[2]。
    Thalidomide (200 mg/kg,口服) 聯(lián)合 Icotinib 對荷瘤 PC9 細胞的裸鼠表現(xiàn)出協(xié)同抗腫瘤作用,抑制腫瘤生長并促進腫瘤死亡[3]。

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

    Clinical Trial
    分子量

    258.23

    Formula

    C13H10N2O4

    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    沙利度胺

    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 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 100 mg/mL (387.25 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 3.8725 mL 19.3626 mL 38.7252 mL
    5 mM 0.7745 mL 3.8725 mL 7.7450 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,避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6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?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: ≥ 2.5 mg/mL (9.68 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (9.68 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實驗周期在半個月以上的動物實驗酌情使用。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中,混合均勻。

    以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 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: 0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (77.45 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑: 10% Tween-80 in PBS

      Solubility: 20 mg/mL (77.45 mM); 懸濁液; 超聲助溶

    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: 99.92%

    參考文獻
    Cell Assay
    [2]

    THP-1 cells, A549 cells and KYSE30 cells are cultured in RPMI-1640 Medium supplemented with 10% fetal bovine serum and maintained at 37?°C in an atmosphere of 5% CO2 and 95% room air. THP-1 cells is irradiated with a single dose of 4?Gy 6-MV X-ray and treated with or without Thalidomide (0.2?μmol/mL)-containing medium for 48?h after radiation. The concentration of Thalidomide is selected based on the preliminary results[2].

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

    Animal Administration
    [2]

    Mice[2]
    A total of 24?WT C57BL/6 mice are randomly divided into 4 groups for the experiments (n?=?6 in each group): a control group, an irradiated group, a group irradiated along with Thalidomide, and a Thalidomide only group. Based on the preliminary results, 100 mg/kg Thalidomide is used in the experiment. Thalidomide is dissolved in DMSO vehicle. The treatment group receives the indicated dose of Thalidomide in 200? μL by gavage every other day beginning on day 1 for six treatments. The control mice receives 200 μL 0.1% DMSO contained-saline only. The lungs are harvested at 12 weeks after irradiation for the analysis. A total of 20 Nrf2-/- mice are randomly divided into 4 groups for the experiments (n?=?5 in each group). The experiment procedures of Nrf2-/- mice are the same as WT C57BL/6 mice. In addition, a total of 30?WT C57BL/6 mice are randomly divided into 5 groups for the subsequent experiments (n?=?6 in each group): a control group, an irradiated group, a group irradiated along with CDDO-Me and Thalidomide, a group irradiated along with CDDO-Me, and a group irradiated along with Thalidomide. 600 ng and 100 mg/kg are selected as the dose of CDDO-Me and Thalidomide for the experiment, respectively. The treatment group receives the indicated dose of CDDO-Me or Thalidomide in 200 μL by gavage every other day beginning on day 1 for six times. For the combined group of CDDO-Me and Thalidomide, CDDO-Me is delivered in 200 μL by gavage every other day beginning on day 1 for six treatments. Thalidomide is delivered in 200 ?μL by gavage every other day beginning on day 2 for six treatments[2].

    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,避免反復凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6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 3.8725 mL 19.3626 mL 38.7252 mL 96.8129 mL
    5 mM 0.7745 mL 3.8725 mL 7.7450 mL 19.3626 mL
    10 mM 0.3873 mL 1.9363 mL 3.8725 mL 9.6813 mL
    15 mM 0.2582 mL 1.2908 mL 2.5817 mL 6.4542 mL
    20 mM 0.1936 mL 0.9681 mL 1.9363 mL 4.8406 mL
    25 mM 0.1549 mL 0.7745 mL 1.5490 mL 3.8725 mL
    30 mM 0.1291 mL 0.6454 mL 1.2908 mL 3.2271 mL
    40 mM 0.0968 mL 0.4841 mL 0.9681 mL 2.4203 mL
    50 mM 0.0775 mL 0.3873 mL 0.7745 mL 1.9363 mL
    60 mM 0.0645 mL 0.3227 mL 0.6454 mL 1.6135 mL
    80 mM 0.0484 mL 0.2420 mL 0.4841 mL 1.2102 mL
    100 mM 0.0387 mL 0.1936 mL 0.3873 mL 0.9681 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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    產(chǎn)品名稱:
    Thalidomide
    目錄號:
    HY-14658
    需求量: