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  4. Tamoxifen

Tamoxifen  (Synonyms: ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen)

Cat. No.: HY-13757A Purity: 99.46%
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Tamoxifène (ICI 47699) est un modulateur sélectif des récepteurs des œstrogènes (SERM) qui bloque l'action des œstrogènes dans les cellules du sein et peut activer l'activité des œstrogènes dans d'autres cellules, comme les os, le foie, et les cellules utérines. Tamoxifène est un puissant activateur de Hsp90 et améliore l'activité d'ATPase du chaperon moléculaire Hsp90. Tamoxifène active l'autophagie et induit l'apoptosis.

Tamoxifen (ICI 47699) ist ein selektiver estrogen receptor-Modulator (SERM), der die Östrogenwirkung in Brustzellen blockiert und die Östrogenaktivität in anderen Zellen, wie Knochen-, Leber- und Gebärmutterzellen, aktivieren kann. Tamoxifen ist ein potenter Hsp90-Aktivator und steigert die Aktivität des molekularen Hsp90-Chaperons ATPase. Tamoxifen aktiviert die autophagy und induziert die apoptosis.

Tamoxifen (ICI 47699) 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. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.

For research use only. We do not sell to patients.

Tamoxifen Chemical Structure

Tamoxifen Chemical Structure

CAS No. : 10540-29-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
100 mg USD 25 In-stock
200 mg USD 35 In-stock
500 mg USD 60 In-stock
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Based on 114 publication(s) in Google Scholar

Other Forms of Tamoxifen:

Tamoxifen Related Antibodies

Top Publications Citing Use of Products

111 Publications Citing Use of MCE Tamoxifen

WB

    Tamoxifen purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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.

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    Description

    Tamoxifen (ICI 47699) 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 is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[5]. Tamoxifen activates autophagy and induces apoptosis[4]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[6].

    IC50 & Target[1][4]

    Estrogen receptor

     

    HSP90

     

    In Vitro

    Tamoxifen (ICI 47699) shows strong inhibition of MCF-7 cells (EC50=1.41 μM) and to a lesser extent the T47D cells (EC50=2.5 μM) but does not affect the MDA-MB-231 cells[2].

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

    Tamoxifen Related Antibodies
    In Vivo

    Tamoxifen can induce nephrotic syndrome and liver injury models. In male Sprague-Dawley rats (weighing 295-340g), the pharmacokinetic data following intravenous administration of Tamoxifen (10 mg/kg) show a maximum plasma concentration of 1566 ng/mL, an area under the plasma concentration-time curve from 0 to 24 hours of 4757 ng·h/mL, and a corresponding area from 0 to 1 hour of 5006 ng·h/mL. The drug's half-life is 5.8 hours[8][10].

    Induction of Cre recombination[8]
    Background
    MerCreMer mice is a kind of mice that expresses Cre recombinase protein, which is fused with two mutant estrogen receptor ligand-binding domains (Mer). Without the induction of Tamoxifen, Cre recombinase is in an inactive state. After Tamoxifen induction, the metabolite of Tamoxifen, 4-OHT (estrogen analog), binds to Mer to activate the activity of Cre recombinase, and then realizes gene knockout.
    Specific Mmodeling Methods
    Mice: transgenic mice • adult (6 weeks of age).
    Administration: 20 mg/kg • i.p. • once daily for 5 days.
    Note
    The hearts of control mice treated with Tamoxifen or physiological saline are perfused with phosphate buffered saline (PBS) in a retrograde manner for 2 minutes, targeting the aorta, left ventricle, and coronary vessels. Then, the hearts are perfused with X-gal staining solution overnight at room temperature to detect the activity of lacZ throughout the heart.
    Modeling Indicators
    Histological Changes: LacZ staining is present in both the left and right ventricles as well as the atriums, though the atrial staining appears less prominent due to the thinner atrial wall.
    All cardiomyocytes exhibit lacZ activity. The recombination rate in the heart is elevated, reaching 70%.
    Correlated Product(s): /
    Opposite Product(s): Cre Recombination Model

    Induction of liver injury[8][9]
    Background
    Tamoxifen reduces the hexose monophosphate shunt, thereby increasing the incidence of oxidative stress in rat hepatocytes, leading to liver injury.
    Specific Mmodeling Methods
    Albino rat &bull ; female &bull ; period: 7 days
    Administration: 45 mg/kg •ip • once daily for 7 days
    Note
    (1) The rats were kept in a standard laboratory environment, which was a 12-hour light/12-hour dark cycle with the temperature maintained at 25 ± 2°C. They had free access to food and water.
    (2) At the end of the experiment, the animals were euthanized by cervical dislocation under mild ether anesthesia. The blood samples were collected in heparinized centrifuge tubes and centrifuged to obtain serum. The abdomen was opened, and the liver was immediately dissected and removed. It was washed with ice-cold isotonic saline and blotted between two filter papers. The liver was wrapped in aluminum foil and stored at -80°C. A 10% (w/v) liver homogenate was prepared in ice-cold 0.1 M potassium phosphate buffer (pH 7.5) using an ultrasonicator.
    Modeling Indicators
    Molecular Changes: The activities of antioxidant enzymes, including glutathione S-transferase, glutathione peroxidase, and catalase, were significantly ↓, while the content of reduced glutathione also showed a ↓ trend. Concurrently, the levels of thiobarbituric acid reactive substances (TBARS) and liver transaminases, including serum glutamic-pyruvic transaminase (sGPT) and serum glutamic-oxaloacetic transaminase (sGOT), were significantly ↑.
    Correlated Product(s): /
    Opposite Product(s): /

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

    Animal Model: Aldh1l1-cre/ERT2 x Ai95 mice[3]
    Dosage: 75 mg/kg
    Administration: Injected for 5 days at 6 weeks of age
    Result: Resulted in the excision of the floxed exon and a gene knockout.
    Clinical Trial
    Molecular Weight

    371.51

    Formula

    C26H29NO
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC/C(C1=CC=CC=C1)=C(C2=CC=CC=C2)/C3=CC=C(C=C3)OCCN(C)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    Ethanol : 50 mg/mL (134.59 mM; Need ultrasonic)

    DMSO : 25 mg/mL (67.29 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6917 mL 13.4586 mL 26.9172 mL
    5 mM 0.5383 mL 2.6917 mL 5.3834 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.60 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (5.60 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  Corn Oil

      Solubility: 40 mg/mL (107.67 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
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    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
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    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.92%

    COA (248 KB) LCMS (112 KB) Elemental Analysis Report (106 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 2.6917 mL 13.4586 mL 26.9172 mL 67.2929 mL
    5 mM 0.5383 mL 2.6917 mL 5.3834 mL 13.4586 mL
    10 mM 0.2692 mL 1.3459 mL 2.6917 mL 6.7293 mL
    15 mM 0.1794 mL 0.8972 mL 1.7945 mL 4.4862 mL
    20 mM 0.1346 mL 0.6729 mL 1.3459 mL 3.3646 mL
    25 mM 0.1077 mL 0.5383 mL 1.0767 mL 2.6917 mL
    30 mM 0.0897 mL 0.4486 mL 0.8972 mL 2.2431 mL
    40 mM 0.0673 mL 0.3365 mL 0.6729 mL 1.6823 mL
    50 mM 0.0538 mL 0.2692 mL 0.5383 mL 1.3459 mL
    60 mM 0.0449 mL 0.2243 mL 0.4486 mL 1.1215 mL
    Ethanol 80 mM 0.0336 mL 0.1682 mL 0.3365 mL 0.8412 mL
    100 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.6729 mL
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    Tamoxifen Related Classifications

    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:

    Tamoxifen10540-29-1ICI 47699 (Z)-Tamoxifen trans-TamoxifenICI47699ICI-47699Estrogen Receptor/ERRHSPAutophagyApoptosisHeat shock proteinsestrogenmodulatorSERMbreastboneliveruterineHsp90chaperoneATPaseInhibitorinhibitorinhibit

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