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(Z)-4-Hydroxytamoxifen Estrogen Receptor modulator

Name: (Z)-4-Hydroxytamoxifen
SKU: S8956
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8956

(Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [³H]oestradiol binding to oestrogen receptor.

Chemical Structure

Molecular Weight: 387.51

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

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Chemical Information, Storage & Stability

Molecular Weight	387.51	Formula	C₂₆H₂₉NO₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	68047-06-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	(Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen			Smiles	CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (201.28 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45% water Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (12.90mM)	Taking the 1 mL working solution as an example, add 100 μL of 50 mg/ml clear DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue adding Dilute 450 μL ddH2O to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	10% DMSO 1 90% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (6.45mM)	Taking the 1 mL working solution as an example, add 100 μL of 25 mg/ml clear DMSO stock solution to 900 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	[3H]oestradiol binding Oestrogen Receptor ^[1] (Cell-free assay) 3.3 nM
In vitro	This compound is a partial estrogen that binds to estrogen receptors with relative binding affinity (RBA) of 2.9 and blocks the growth of the MCF-7 human mammary tumor cell line in vitro.^[2]
In vivo	(Z)-4-Hydroxytamoxifen is a partial estrogen with antiestrogenic properties, and the cis isomer is less potent than the trans isomer.^[3] This compound inhibits estradiol benzoate action and reduces the uterine growth rate in vivo.^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/591813/ [2] https://pubmed.ncbi.nlm.nih.gov/3385723/ [3] https://pubmed.ncbi.nlm.nih.gov/6781873/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05133674	Unknown status	Breast Cancer\|Breast Carcinoma\|Breast Tumors\|Cancer of Breast\|Malignant Neoplasm of Breast	Karolinska University Hospital	April 4 2022	Phase 2

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