(Z)-4-Hydroxytamoxifen

For research use only.

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

(Z)-4-Hydroxytamoxifen Chemical Structure

CAS No. 68047-06-3

(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.

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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

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: immature female rats
  • Dosages: 1.25 μg
  • Administration: SC
    (Only for Reference)

Solubility (25°C)

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

* 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.

Chemical Information

Molecular Weight 387.51
Formula

C26H29NO2

CAS No. 68047-06-3
Storage powder
in 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

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID