(Z)-4-Hydroxytamoxifen

Name: ( Z )-4-Hydroxytamoxifen
Brand: Tocris Bioscience
SKU: 3412

Tocris Bioscience, part of Bio-Techne | Catalog # 3412

(1)

Citations (45)

COA / SDS

Metabolite of tamoxifen (Cat. No. 0999)

Key Product Details

Chemical Name:	4-[(1Z)-1-[4-[2-(Dimethylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]phenol
Purity:	≥98%

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Technical Data
Citations / Reviews (1)

Biological Activity for (Z)-4-Hydroxytamoxifen

(Z)-4-Hydroxytamoxifen is an estrogen receptor antagonist (IC₅₀ = 27 μM). (Z)-4-Hydroxytamoxifen is a Tamoxifen (Cat. No. 0999) metabolite; that exhibits greater potency than the parent compound. (Z)-4-Hydroxytamoxifen also activates intein-linked inactive Cas9, reducing off-target CRISPR-mediated gene editing; system has ~25-fold higher specificity than wtCas9. (Z)-4-Hydroxytamoxifen binds to voltage-gated sodium channels, near the intracellular gate and inhibits the sodium current by delaying channel recovery from the inactivated state (IC₅₀ values are 297 nM and 2.1 �M for NavM and human Nav, respectively in HEK cells); this inhibition is independent of estrogen receptor modulation. Chemotherapeutic agent.

Technical Data for (Z)-4-Hydroxytamoxifen

Formula	C₂₆H₂₉NO₂
Storage	Store at +4°C
Purity	≥98%
CAS Number	68047-06-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for (Z)-4-Hydroxytamoxifen

Solubility

Soluble Soluble to 100 mM in DMSO and to 20 mM in ethanol

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References for (Z)-4-Hydroxytamoxifen

References are publications that support the biological activity of the product.

Yu and Forman Simple and efficient production of (Z)-4-hydroxytamoxifen, a potent estrogen receptor modulator. J.Org.Chem., 2003;68:9489 PMID: 14629178
Davis et al. Small molecule-triggered Cas9 protein with improved genome-editing specificity. Nat.Chem.Biol., 2015;11:316 PMID: 25848930
Jordan et al. A monohydroxylated metabolite of tamox. with potent antioestrogenic activity. J.Endocrinology, 1977;75:305 PMID: 591813
Desta et al. Comprehensive evaluation of tamox. sequential biotransformation by the human cytochrome P450 system in vitro: Prominent roles for CYP3A and CYP2D6. J.Pharm.Exp.Ther., 2004;310:1062 PMID: 15159443

(Z)-4-Hydroxytamoxifen

Tocris Bioscience, part of Bio-Techne | Catalog # 3412

Key Product Details

Biological Activity for (Z)-4-Hydroxytamoxifen

Technical Data for (Z)-4-Hydroxytamoxifen

Solubility for (Z)-4-Hydroxytamoxifen

Dilution Calculator

Reconstitution Calculator

References for (Z)-4-Hydroxytamoxifen

Product Documents for (Z)-4-Hydroxytamoxifen

COA

Certificate of Analysis

SDS

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