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

Alantolactone  (Synonyms: 土木香内酯; (+)-Alantolactone; Alant camphor; Inula camphor)

目录号: HY-N0038 纯度: 99.94%
COA 产品使用指南

Alantolactone 是 STAT3 的选择性抑制剂,并具有抗肿瘤活性。Alantolactone 可诱导癌症相关的凋亡。

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Alantolactone Chemical Structure

Alantolactone Chemical Structure

CAS No. : 546-43-0

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规格 价格 是否有货 数量
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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50 mg ¥2800
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100 mg ¥4500
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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 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    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

     

    细胞效力
    (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]
    体外研究
    (In Vitro)

    Alantolactone 以剂量依赖性方式诱导 HepG2 细胞凋亡。研究发现,这种 Alantolactone 诱导的细胞凋亡与 GSH 耗竭、STAT3 激活抑制、ROS 生成、线粒体跨膜电位耗散以及 Bax/Bcl-2 比率和 caspase-3 激活增加有关[1]。Alantolactone 减少 STAT3 向细胞核的易位、其 DNA 结合和 STAT3 靶基因表达。Alantolactone 显著抑制 STAT3 激活,对 MAPK 和 NF-κB 转录具有边际效应;然而,这种作用不是通过抑制 STAT3 上游激酶来介导的[2]
    Alantolactone 在人结肠腺癌 HCT-8 细胞中诱导激活素/SMAD3 信号传导。Alantolactone 通过阻断激活素信号通路中 Cripto-1 与 IIA 型激活素受体的相互作用发挥抗肿瘤作用[4]
    Alantolactone (5 μg/mL,24 h) 抑制结肠腺癌HCT-8细胞增殖[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.
    体内研究
    (In Vivo)

    结果发现,与对照小鼠相比,Alantolactone 处理小鼠的平均肿瘤体积大约低 2.17 倍。然而,Alantolactone 的给药在实验期间不影响整体体重,表明没有明显的毒性。此外,与对照小鼠相比,Alantolactone 处理小鼠的平均肿瘤重量显著降低。更重要的是,Alantolactone 的给药导致肿瘤组织中 p-STAT3 和细胞周期蛋白 D1 表达的显著降低[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 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    土木香内酯;木香腦;土木香脑;阿兰内酯;木香油內酯

    结构分类
    初始来源
    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
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (430.44 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)

    配制储备液
    浓度 溶剂体积 质量 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

    动物实验:

    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: ≥ 2.5 mg/mL (10.76 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (10.76 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 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。

      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

    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: 99.94%

    参考文献

    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 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
    • 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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    目录号:
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