2. 诱导疾病模型产品 Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cell Cycle/DNA Damage Autophagy Apoptosis
  3. 遗传工程疾病模型 Estrogen Receptor/ERR HSP Autophagy Apoptosis
  4. Tamoxifen Citrate

Tamoxifen Citrate  (Synonyms: 枸橼酸他莫昔芬; ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate)

目录号: HY-13757 纯度: 99.93%
COA 产品使用指南

摩尔计算器

Tamoxifen Citrate (ICI 46474) 是一种口服有效的，选择性雌激素受体调节剂 (SERM)，可阻断乳腺细胞中的雌激素作用，并可激活其他细胞，如骨骼，肝脏和子宫细胞中的雌激素活性。Tamoxifen Citrate 是一种有效的 Hsp90 激活剂，可增强 Hsp90 分子伴侣 ATPase 的活性。Tamoxifen Citrate 还可以有效抑制传染性 EBOV Zaire 和 Marburg (MARV)，IC50 分别为 0.1 μM 和 1.8 μM。Tamoxifen Citrate 可以激活自噬 (autophagy)，诱导凋亡 (apoptosis)。Tamoxifen Citrate 还可以诱导 CreER(T2) 转基因小鼠的基因敲除。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Tamoxifen Citrate Chemical Structure

Tamoxifen Citrate Chemical Structure

CAS No. : 54965-24-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
In-stock
500 mg ￥500
In-stock
1 g ￥690
In-stock
5 g ￥2750
In-stock
10 g   询价  
50 g   询价  

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Customer Review

Other Forms of Tamoxifen Citrate:

Tamoxifen Citrate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 114 篇科研文献

WB

    Tamoxifen Citrate purchased from MCE. Usage Cited in: Redox Biol. 18 October 2022, 102509.

    Expression of TFRC in primary fibroblasts from TFRCflox/flox and TFRC−/− mice was assessed by western blot after 5 days of Tamoxifen intraperitoneal injection and 7 days of waiting.

    Tamoxifen Citrate purchased from MCE. Usage Cited in: Clin Transl Med. 2020 Jan;10(1):137-150.  [Abstract]

    Different transmission of MAPK8/FoxO signaling pathway in breast cancer cells (MCF-7, T47D, ZR-75, and MDA-MB-231) and liver cells (LO2) exposed to TAM (Tamoxifen).

    Tamoxifen Citrate purchased from MCE. Usage Cited in: Cell Commun Signal. 2019 May 23;17(1):50.  [Abstract]

    Tamoxifen inhibits the growth and metastasis of prostate tumors in vivo. Western blot analysis of the indicated proteins in prostate primary tumors tissues.

    查看 Estrogen Receptor/ERR 亚型特异性产品:

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    Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3].Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[5]. Tamoxifen Citrate activates autophagy and induces apoptosis[4].Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse[6].

    IC50 & Target[1][4]

    Estrogen receptor

     

    HSP90

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    DU-145 IC50
    11.2 μM
    Compound: Tam citrate
    Anticancer activity against human DU-145 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    Anticancer activity against human DU-145 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    		[PMID: 30772606]
    DU-145 IC50
    15.25 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against human DU145 cells after 18 hrs by MTT assay
    Cytotoxicity against human DU145 cells after 18 hrs by MTT assay
    		[PMID: 19932024]
    HEK293 IC50
    27.3 μM
    Compound: Tam citrate
    Cytotoxicity against HEK293 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    Cytotoxicity against HEK293 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    		[PMID: 30772606]
    HEK293 IC50
    30 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    		[PMID: 29352645]
    Ishikawa IC50
    12.5 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against human Ishikawa cells after 18 hrs by MTT assay
    Cytotoxicity against human Ishikawa cells after 18 hrs by MTT assay
    		[PMID: 19932024]
    MCF7 IC50
    0.796 μM
    Compound: Tamoxifen citrate
    Inhibition of 17-beta estradiol-induced cell proliferation in human MCF7 cells incubated for 6 days by acid red-52 staining based assay
    Inhibition of 17-beta estradiol-induced cell proliferation in human MCF7 cells incubated for 6 days by acid red-52 staining based assay
    		[PMID: 28882502]
    MCF7 IC50
    10.2 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against human MCF7 cells after 18 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 18 hrs by MTT assay
    		[PMID: 19932024]
    MCF7 IC50
    13.7 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    		[PMID: 29352645]
    MCF7 IC50
    6.2 μM
    Compound: Tam citrate
    Anticancer activity against human MCF7 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    Anticancer activity against human MCF7 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    		[PMID: 30772606]
    MCF7 IC50
    9.53 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay
    		[PMID: 32947093]
    MDA-MB-231 IC50
    10.71 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay
    		[PMID: 32947093]
    MDA-MB-231 IC50
    12.3 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against human MDA-MB-231 cells after 18 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 18 hrs by MTT assay
    		[PMID: 19932024]
    MDA-MB-231 IC50
    12.8 μM
    Compound: Tam citrate
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    		[PMID: 30772606]
    MDA-MB-231 IC50
    17.9 μM
    Compound: Tamoxifen citrate
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    		[PMID: 29352645]
    PC-3 IC50
    11.7 μM
    Compound: Tam citrate
    Anticancer activity against human PC-3 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    Anticancer activity against human PC-3 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
    		[PMID: 30772606]
    Vero C1008 IC50
    34.12 μM
    Compound: Tamoxifen Citrate
    IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
    IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
    		10.1101/2020.03.25.008482
    Vero C1008 CC50
    37.96 μM
    Compound: Tamoxifen Citrate
    CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
    CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
    		10.1101/2020.03.25.008482
    Vero C1008 CC50
    37.96 μM
    Compound: Tamoxifen Citrate
    CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
    CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
    		10.1101/2020.03.25.008482
    Vero C1008 IC50
    8.98 μM
    Compound: Tamoxifen Citrate
    IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
    IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
    		10.1101/2020.03.25.008482
    体外研究
    (In Vitro)

    Tamoxifen Citrate (ICI 46474) 对 MCF-7 细胞 (EC50=1.41 μM) 表现出强烈的抑制作用，对 T47D 细胞的抑制作用较小 (EC50=2.5 μM) 但不影响 MDA-MB-231 细胞[2]。

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

    Tamoxifen Citrate 相关抗体:
    体内研究
    (In Vivo)

    Tamoxifen 可用于构建肝损伤模型，在雄性 Sprague-Dawley 大鼠 (体重 295-340g) 中，静脉注射 Tamoxifen (10 mg/kg) 后的药代动力学参数显示最大血浆浓度为 1566 ng/mL，0 至 24 小时的血浆浓度-时间曲线下面积为 4757 ng·h/mL，0 至 1 小时的曲线下面积为 5006 ng·h/mL，药物的半衰期为 5.8 小时[10]。

    诱导肝损伤模型[8][9]
    致病原理
    Tamoxifen 会降低己糖单磷酸旁路，从而增加大鼠肝细胞中氧化应激的发生率，导致肝脏损伤。
    具体造模方法：
    大鼠：白化病大鼠 • 雌性 • 处理 7 days
    给药方式：45 mg/kg • 腹腔注射 • 每天一次，连续 7 天
    Note
    (1) 大鼠处于标准的实验室环境下，即 12 小时光照/12 小时黑暗循环，温度保持在 25 ± 2°C，且可以自由获取食物和水。
    (2) 实验结束后，动物在轻度乙醚麻醉下通过颈椎脱位处死。将血液样本收集在肝素化的离心管中，离心得到血清。剖开腹部，立即解剖取出肝脏，用冰冷的等渗盐水洗涤，并在两张滤纸之间吸干。肝脏用铝箔包裹，在-80℃下保存。使用超声仪在冰冷的0.1 M 磷酸钾缓冲液（PH 7.5）中制备10%（w/v）的肝匀浆。
    造模成功指标
    分子变化：抗氧化酶(谷胱甘肽S转移酶、谷胱甘肽过氧化物酶和过氧化氢酶) 活性显著 ↓，还原型谷胱甘肽含量 ↓，同时硫代巴比妥酸反应物质(TBARS) 和肝脏转氨酶(血清谷丙转氨酶sGPT 和血清谷草转氨酶sGOT) 水平显著 ↑。
    相关产品： /
    拮抗产品： /

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

    563.64

    Formula

    C32H37NO8
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    枸橼酸他莫昔芬； 他莫昔芬柠檬酸盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (88.71 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)

    Ethanol 中的溶解度 : 10 mg/mL (17.74 mM; 超声助溶)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.7742 mL 8.8709 mL 17.7418 mL
    5 mM 0.3548 mL 1.7742 mL 3.5484 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, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 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: ≥ 2.08 mg/mL (3.69 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (3.69 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 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。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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： Corn Oil

      Solubility: 10 mg/mL (17.74 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (17.74 mM); 澄清溶液; 超声助溶

    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

    只
    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）。

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    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: 99.93%

    COA (294 KB) LCMS (267 KB)

    产品使用指南 (1538 KB)
    参考文献
    Animal Administration
    [3]

    Mice[3]
    Seven-week old TmcsMed1-/- mice and the wild-type littermates are then administered Tamoxifen intraperitoneally at a daily dose of 65 mg/kg body weight for 5 days and then killed at selected intervals after initiation of Tamoxifen treatment. For each experiment 3 to 5 mice for control and csMed1-/- are used. To obtain survival curve 41 csMed1-/- and 41 csMed1fl/fl mice are used. Thirteen TmcsMed-/- mice and the same number of littermates are used for the survival curve experiments using Tamoxifen inducible model.

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

    Tamoxifen Citrate 相关分类

    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, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 1.7742 mL 8.8709 mL 17.7418 mL 44.3546 mL
    5 mM 0.3548 mL 1.7742 mL 3.5484 mL 8.8709 mL
    10 mM 0.1774 mL 0.8871 mL 1.7742 mL 4.4355 mL
    15 mM 0.1183 mL 0.5914 mL 1.1828 mL 2.9570 mL
    DMSO 20 mM 0.0887 mL 0.4435 mL 0.8871 mL 2.2177 mL
    25 mM 0.0710 mL 0.3548 mL 0.7097 mL 1.7742 mL
    30 mM 0.0591 mL 0.2957 mL 0.5914 mL 1.4785 mL
    40 mM 0.0444 mL 0.2218 mL 0.4435 mL 1.1089 mL
    50 mM 0.0355 mL 0.1774 mL 0.3548 mL 0.8871 mL
    60 mM 0.0296 mL 0.1478 mL 0.2957 mL 0.7392 mL
    80 mM 0.0222 mL 0.1109 mL 0.2218 mL 0.5544 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.

    Keywords:

    Tamoxifen54965-24-1ICI 46474(Z)-Tamoxifentrans-Tamoxifen枸橼酸他莫昔芬 他莫昔芬柠檬酸盐ICI46474ICI-46474Estrogen Receptor/ERRHSPAutophagyApoptosisHeat shock proteinsestrogenmodulatorSERMbreastboneliveruterineHsp90chaperoneATPaseInhibitorinhibitorinhibit

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