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  1. JAK/STAT Signaling Stem Cell/Wnt Apoptosis TGF-beta/Smad
  2. STAT Apoptosis TGF-beta/Smad
  3. Alantolactone

Alantolactone  (Synonyms: 土木香內酯; (+)-Alantolactone; Alant camphor; Inula camphor)

目錄號: HY-N0038 純度: 99.94%
COA 產品使用指南 技術支持

Alantolactone 是 STAT3 的選擇性抑制劑,并具有抗腫瘤活性。Alantolactone 可誘導癌癥相關的凋亡。

MCE 的所有產品僅用作科學研究或藥證申報,我們不為任何個人用途提供產品和服務

Alantolactone Chemical Structure

Alantolactone Chemical Structure

CAS No. : 546-43-0

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10 mM * 1 mL in DMSO ¥550
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5 mg ¥500
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10 mg ¥770
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25 mg ¥1600
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Customer Review

Other Forms of Alantolactone:

    Alantolactone purchased from MCE. Usage Cited in: Stem Cells. 2019 Feb;37(2):190-201.  [Abstract]

    Western blot images show Smad2/3 phosphorylation is lower than baseline in the sh-GPM6B cells and higher than baseline in the GPM6B-sgRNA cells. The phosphorylation of Smad2/3 in the sh-GPM6B TGF-β1 group is elevated by Alantolactone and the phosphorylation is reduced by treatment with SB431542.

    Alantolactone purchased from MCE. Usage Cited in: Stem Cells. 2019 Feb;37(2):190-201.  [Abstract]

    Western blot analyses show the repression of SMC specific markers in the sh-GPM6B TGF-β1 group are abolished by Alantolactone in the sh-GPM6B and the enrichment of SMC specific markers in the GPM6B-sgRNA cells is cancelled by treatment with SB431542.

    查看 STAT 亞型特異性產品:

    • 生物活性

    • 純度 & 產品資料

    • 參考文獻

    生物活性

    Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone induces apoptosis in cancer[1][2][3].

    IC50 & Target

    STAT3

     

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.55 μg/mL
    Compound: 6
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
    [PMID: 23451797]
    HepG2 IC50
    1.3 μg/mL
    Compound: 6
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
    [PMID: 23451797]
    HT-1080 IC50
    0.696 μg/mL
    Compound: 6
    Antiproliferative activity against human HT1080 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
    Antiproliferative activity against human HT1080 cells assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
    [PMID: 23451797]
    HUVEC IC50
    2.4 μg/mL
    Compound: 6
    Antiproliferative activity against human HUVEC assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
    Antiproliferative activity against human HUVEC assessed as inhibition of cell proliferation after 72 hrs by CCK8 assay
    [PMID: 23451797]
    MDA-MB-231 IC50
    15 μM
    Compound: 23
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
    [PMID: 33650861]
    RAW264.7 IC50
    1.17 μM
    Compound: 29
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated for 30 mins before LPS challenge measured 24 hrs after LPS challenge by Griess reaction method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated for 30 mins before LPS challenge measured 24 hrs after LPS challenge by Griess reaction method
    [PMID: 21924800]
    體外研究
    (In Vitro)

    Alantolactone 以劑量依賴性方式誘導 HepG2 細胞凋亡。研究發(fā)現(xiàn),這種 Alantolactone 誘導的細胞凋亡與 GSH 耗竭、STAT3 激活抑制、ROS 生成、線粒體跨膜電位耗散以及 Bax/Bcl-2 比率和 caspase-3 激活增加有關[1]。Alantolactone 減少 STAT3 向細胞核的易位、其 DNA 結合和 STAT3 靶基因表達。Alantolactone 顯著抑制 STAT3 激活,對 MAPK 和 NF-κB 轉錄具有邊際效應;然而,這種作用不是通過抑制 STAT3 上游激酶來介導的[2]。
    Alantolactone 在人結腸腺癌 HCT-8 細胞中誘導激活素/SMAD3 信號傳導。Alantolactone 通過阻斷激活素信號通路中 Cripto-1 與 IIA 型激活素受體的相互作用發(fā)揮抗腫瘤作用[4]
    Alantolactone (5 μg/mL,24 h) 抑制結腸腺癌HCT-8細胞增殖[4]

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

    Cell Viability Assay[4]

    Cell Line: HCT-8 cells.
    Concentration: 5 μg/mL (~21.6 μM).
    Incubation Time: 24 h.
    Result: Activated the activin signaling pathway in HCT-8 cells.
    體內研究
    (In Vivo)

    結果發(fā)現(xiàn),與對照小鼠相比,Alantolactone 處理小鼠的平均腫瘤體積大約低 2.17 倍。然而,Alantolactone 的給藥在實驗期間不影響整體體重,表明沒有明顯的毒性。此外,與對照小鼠相比,Alantolactone 處理小鼠的平均腫瘤重量顯著降低。更重要的是,Alantolactone 的給藥導致腫瘤組織中 p-STAT3 和細胞周期蛋白 D1 表達的顯著降低[2]。

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

    Animal Model: Female athymic BALB/c nude mice at the age of 6 weeks[2].
    Dosage: 2.5 mg/kg.
    Administration: I.P. injection every 2 days.
    Result: Exhibited anti-cancer activity.
    分子量

    232.32

    Formula

    C15H20O2

    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    土木香內酯;木香腦;土木香腦;阿蘭內酯;木香油內酯

    結構分類
    初始來源
    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: 

    DMSO 中的溶解度 : 100 mg/mL (430.44 mM; 超聲助溶; 吸濕的 DMSO 對產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 質量 1 mg 5 mg 10 mg
    1 mM 4.3044 mL 21.5220 mL 43.0441 mL
    5 mM 0.8609 mL 4.3044 mL 8.6088 mL
    查看完整儲備液配制表

    * 請根據(jù)產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年內使用, -20°C儲存時,請在1年內使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    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 (10.76 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (10.76 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 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 中國技術支持聯(lián)系。
    動物實驗體內工作液的配制方法 : 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 & 產品資料

    純度: 99.94%

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產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年內使用, -20°C儲存時,請在1年內使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.3044 mL 21.5220 mL 43.0441 mL 107.6102 mL
    5 mM 0.8609 mL 4.3044 mL 8.6088 mL 21.5220 mL
    10 mM 0.4304 mL 2.1522 mL 4.3044 mL 10.7610 mL
    15 mM 0.2870 mL 1.4348 mL 2.8696 mL 7.1740 mL
    20 mM 0.2152 mL 1.0761 mL 2.1522 mL 5.3805 mL
    25 mM 0.1722 mL 0.8609 mL 1.7218 mL 4.3044 mL
    30 mM 0.1435 mL 0.7174 mL 1.4348 mL 3.5870 mL
    40 mM 0.1076 mL 0.5381 mL 1.0761 mL 2.6903 mL
    50 mM 0.0861 mL 0.4304 mL 0.8609 mL 2.1522 mL
    60 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7935 mL
    80 mM 0.0538 mL 0.2690 mL 0.5381 mL 1.3451 mL
    100 mM 0.0430 mL 0.2152 mL 0.4304 mL 1.0761 mL
    Help & FAQs
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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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    目錄號:
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