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

Name: (E/Z)-4-Hydroxytamoxifen
Brand: MedChemExpress
SKU: HY-16950A
Rating: 5.0 (3 reviews)

Cat. No.: HY-16950A Purity: 99.62%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 68392-35-8

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 3 publication(s) in Google Scholar

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

(Z)-4-Hydroxy Tamoxifen-d₅ In-stock
4-Hydroxytamoxifen In-stock
(E)-4-Hydroxytamoxifen In-stock
(E/Z)-4-Hydroxytamoxifen (Standard) 견적 받기

3 Publications Citing Use of MCE (E/Z)-4-Hydroxytamoxifen

Cell Proliferation/Viability Assay

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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
순도&문서
References
고객리뷰

제품 설명

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.

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

분자량

387.51

화학식

C₂₆H₂₉NO₂

CAS No.

68392-35-8

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

Endogenous metabolite

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

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
10 mM	0.2581 mL	1.2903 mL	2.5806 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.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

Dosing volume
(per animal)

μL

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.

순도&문서

Purity: 99.62%

Select Batch:

Data Sheet (277 KB) SDS (604 KB)

COA (250 KB) RP-HPLC (254 KB)

Handling Instructions (2659 KB)

References

[1]. Mansel R, et al. A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women. Breast Cancer Res Treat. 2007 Dec;106(3):389-97. [Content Brief]

[2]. Desta Z, et al. Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75. [Content Brief]

[3]. Gamboa da Costa G, et al. DNA adduct formation and mutant induction in Sprague-Dawley rats treated with tamoxifen and its derivatives. Carcinogenesis. 2001 Aug;22(8):1307-15. [Content Brief]

[4]. Prossnitz ER, et al. International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators. Pharmacol Rev. 2015 Jul;67(3):505-40. [Content Brief]

Complete Stock Solution Preparation Table

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

(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

최근 본 상품:

상품명

Requested Quantity *

고객명 *

호칭

메일주소 *

전화번호 *

Department

회사명 *

City

도

Country or Region *

비고

상품명

Lot #

고객명 *

메일주소 *

전화번호

Department *

회사명 *

Country or Region *

비고

Name
이메일 *

	Sorry, but the email address you supplied was invalid.

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

고객리뷰

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

(E/Z)-4-Hydroxytamoxifen Related Antibodies

3 Publications Citing Use of MCE (E/Z)-4-Hydroxytamoxifen

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

(E/Z)-4-Hydroxytamoxifen Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

(E/Z)-4-Hydroxytamoxifen Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report