2. Vitamin D Related/Nuclear Receptor GPCR/G Protein Metabolic Enzyme/Protease
  3. Estrogen Receptor/ERR Adhesion G Protein-coupled Receptors (AGPCRs) Drug Metabolite
  4. (E/Z)-4-Hydroxytamoxifen

(E/Z)-4-Hydroxytamoxifen  (Synonyms: Afimoxifene; 4-OHT)

Cat. No.: HY-16950A Purity: 99.62%
COA
SDS
Handling Instructions Technical Support

(E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity.

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

CAS No. : 68392-35-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of (E/Z)-4-Hydroxytamoxifen:

(E/Z)-4-Hydroxytamoxifen Related Antibodies

Top Publications Citing Use of Products
IP
Cell Proliferation/Viability Assay
WB
RT-PCR

    (E/Z)-4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Drug Resist Updat. 2026 Jan:84:101319.  [Abstract]

    Representative quantification of ZBP1 recruitment to the HR-DSB locus near the AsiSI cleavage site in AsiSI-ER-U2OS cells treated with or without 4-OHT(300 nM, 4 h).

    (E/Z)-4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2020 Aug;20(2):1441-1451.  [Abstract]

    The viability of T47D cells treated with 0-10 µmol 4-OH Tam was detected using the Cell Counting Kit-8 assay.

    (E/Z)-4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2020 Aug;20(2):1441-1451.  [Abstract]

    The protein levels of AGR3 and ER in T47D cells treated with 0, 2, 4, 6, 8 and 10 µmol 4-OH Tam for 24 h were detected by western blotting.

    (E/Z)-4-Hydroxytamoxifen purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2020 Aug;20(2):1441-1451.  [Abstract]

    RNA expression levels of ESR1 were detected in T47D cells after the addition of different concentrations of 4‑OH Tam for 24 h.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity[1][2][3][4].

    IC50 & Target

    Estrogen receptor

     

    Human Endogenous Metabolite

     

    In Vitro

    (E/Z)-4-Hydroxytamoxifen (10 μM, 0-90 min) oxidized by CYP2D6 represents a minor route of Tamoxifen metabolism, and then is converted to 3,4- dihydroxytamoxifen and Endoxifen (HY-18719E)[3].

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

    (E/Z)-4-Hydroxytamoxifen Related Antibodies
    In Vivo

    (E/Z)-4-Hydroxytamoxifen (20.9 mg/kg, gavage or i.p., daily for 7 days) reduces the body weight and induces a significant increase in ethoxyresorufin O-deethylase activity in rats[3].

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

    Animal Model: Sprague-Dawley rats[3]
    Dosage: 20.9 mg/kg
    Administration: gavage or i.p., daily for 7 days
    Result: Caused a significant reduction in body weight and induced a significant increase in ethoxyresorufin O-deethylase activity in rats.
    Clinical Trial
    Molecular Weight

    387.51

    Formula

    C26H29NO2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC1=CC=C(/C(C2=CC=C(OCCN(C)C)C=C2)=C(C3=CC=CC=C3)\CC)C=C1
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 83.33 mg/mL (215.04 mM; Need ultrasonic; 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 2.5806 mL 12.9029 mL 25.8058 mL
    5 mM 0.5161 mL 2.5806 mL 5.1612 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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 (5.37 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.37 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    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 +
    % 
    +
    %
    Tween-80 +
    %
    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).
    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: 99.62%

    SDS (604 KB)

    COA (250 KB) RP-HPLC (254 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5806 mL 12.9029 mL 25.8058 mL 64.5145 mL
    5 mM 0.5161 mL 2.5806 mL 5.1612 mL 12.9029 mL
    10 mM 0.2581 mL 1.2903 mL 2.5806 mL 6.4514 mL
    15 mM 0.1720 mL 0.8602 mL 1.7204 mL 4.3010 mL
    20 mM 0.1290 mL 0.6451 mL 1.2903 mL 3.2257 mL
    25 mM 0.1032 mL 0.5161 mL 1.0322 mL 2.5806 mL
    30 mM 0.0860 mL 0.4301 mL 0.8602 mL 2.1505 mL
    40 mM 0.0645 mL 0.3226 mL 0.6451 mL 1.6129 mL
    50 mM 0.0516 mL 0.2581 mL 0.5161 mL 1.2903 mL
    60 mM 0.0430 mL 0.2150 mL 0.4301 mL 1.0752 mL
    80 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8064 mL
    100 mM 0.0258 mL 0.1290 mL 0.2581 mL 0.6451 mL
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    (E/Z)-4-Hydroxytamoxifen 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:

    (E/Z)-4-Hydroxytamoxifen68392-35-8Afimoxifene 4-OHTEstrogen Receptor/ERRAdhesion G Protein-coupled Receptors (AGPCRs)Drug MetaboliteInhibitorinhibitorinhibit

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