(Z)-4-Hydroxytamoxifen

Catalog No.S8956 Batch:S895601

Technical Data

Formula

C₂₆H₂₉NO₂

Molecular Weight

387.51

CAS No.

68047-06-3

Solubility (25°C)*

In vitro

DMSO

78 mg/mL (201.28 mM)

Ethanol

10 mg/mL (25.8 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	10% DMSO 1 90% corn oil	2.5mg/ml	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.
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45% water	5.0mg/ml	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[3]}	Animal Models immature female rats Dosages 1.25 μg Administration SC

Cell Assay:^{^[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 Study:^{^[3]}

Animal Models
immature female rats
Dosages
1.25 μg
Administration
SC

References

Selleck's (Z)-4-Hydroxytamoxifen has been cited by 2 publications

YAP-mediated GPER signaling impedes proliferation and survival of prostate epithelium in benign prostatic hyperplasia [ iScience, 2024, 27(3):109125]	PubMed: 38420594
Use of the dTAG system in vivo to degrade CDK2 and CDK5 in adult mice and explore potential safety liabilities [ Toxicol Sci, 2023, kfad049]	PubMed: 37228089

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.