Home Endocrinology & Hormones Estrogen/progestogen Receptor modulator (Z)-4-Hydroxytamoxifen For research use only.

(Z)-4-Hydroxytamoxifen

Synonyms: (Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen

(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

(Z)-4-Hydroxytamoxifen Chemical Structure

CAS No. 68047-06-3

Purity & Quality Control

Batch: S895601 DMSO]78 mg/mL]false]Ethanol]10 mg/mL]false]Water]Insoluble]false Purity: 99.96%
99.96

(Z)-4-Hydroxytamoxifen Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models immature female rats
Dosages 1.25 μg
Administration SC
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

Chemical Information & Solubility

Molecular Weight 387.51 Formula

C26H29NO2
CAS No. 68047-06-3 SDF --
Smiles CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 78 mg/mL ( (201.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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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.

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