(Z)-4-Hydroxytamoxifen

Catalog No.S8956 Synonyms: (Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen

For research use only.

(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.

(Z)-4-Hydroxytamoxifen Chemical Structure

CAS No. 68047-06-3

Purity & Quality Control

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Biological Activity

Description (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.
Targets
[3H]oestradiol binding Oestrogen Receptor [1]
(Cell-free assay)
3.3 nM
In vitro

(Z)-4-Hydroxytamoxifen 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] (Z)-4-Hydroxytamoxifen inhibits estradiol benzoate action and reduces the uterine growth rate in vivo.[2]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: MCF-7 cells
  • Concentrations: 0.1 nM - 10 μM
  • Incubation Time: 50 min
  • Method:

    MCF-7 cells are incubated at 37℃ for 50 min with 1 nM [3H]estradiol in the absence or presence of increasing amounts (0.1 nM - 10 μM) of (Z)-4-Hydroxytamoxifen or unlabeled estradiol (control). Bound compounds are then extracted with ethanol, and the amounts of estrogen receptor bound [3H]estradiol are measured.

Animal Research:

[3]

  • Animal Models: immature female rats
  • Dosages: 1.25 μg
  • Administration: SC

Solubility (25°C)

In vitro

DMSO 78 mg/mL
(201.28 mM)
Water Insoluble
Ethanol '''10 mg/mL

Chemical Information

Molecular Weight 387.51
Formula

C26H29NO2

CAS No. 68047-06-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05133674 Not yet recruiting Drug: Tamoxifen 20 mg Breast Cancer|Breast Carcinoma|Breast Tumors|Cancer of Breast|Malignant Neoplasm of Breast Karolinska University Hospital January 10 2022 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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