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  3. Tamoxifen Citrate

Tamoxifen Citrate  (Synonyms: ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate)

Cat. No.: HY-13757 Purity: 99.95%
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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.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. Tamoxifen Citrate activates autophagy and induces apoptosis.Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse.

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

Tamoxifen Citrate Chemical Structure

Tamoxifen Citrate Chemical Structure

CAS No. : 54965-24-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
500 mg USD 66 In-stock
1 g USD 91 In-stock
5 g USD 317 In-stock
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Customer Review

Based on 84 publication(s) in Google Scholar

Other Forms of Tamoxifen Citrate:

Top Publications Citing Use of Products

81 Publications Citing Use of MCE Tamoxifen Citrate

WB

    Tamoxifen Citrate 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 Citrate 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 Citrate 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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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    In Vitro

    Tamoxifen Citrate (ICI 46474) 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.

    In Vivo

    Injection of pre-mutant mice with Tamoxifen Citrate (75 mg/kg; injected for 5 days at 6 weeks of age) results in the excision of the floxed exon and, thus, in a gene knockout[3].
    Blood pharmacokinetic parameters shows: Tamoxifen (Tamoxifen (HY-13757A): 10 mg/kg; i.v.) has a maximum plasma concentration of 1566 ng/mL from 0 to 24 hours plasma concentration-time The total area under the curve is 4757 ng·h/mL, the total area under the plasma concentration-time curve from 0-1 is 5006 ng·h/mL, and the half-life is 5.8 h in male Sprague-Dawley rats (295-340 g)[10].

    1. 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: Tamoxifen (HY-13757A) 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.

    Clinical Trial
    Molecular Weight

    563.64

    Formula

    C32H37NO8

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)\C3=CC=CC=C3.O=C(CC(C(O)=O)(O)CC(O)=O)O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (88.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 10 mg/mL (17.74 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    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)

    C1

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    Volume (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 (3.69 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 (3.69 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 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: 10 mg/mL (17.74 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

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    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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    %
    Saline
    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, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    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: 99.95%

    References
    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.

    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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 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
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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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