(Z)-4-Hydroxytamoxifen
Tocris Bioscience | Catalog # 3412
Key Product Details
Description
Alternative Names
Product Description
(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 µM for NavM and human Nav, respectively in HEK cells); this inhibition is independent of estrogen receptor modulation. Chemotherapeutic agent.
Product Specifications for (Z)-4-Hydroxytamoxifen
Molecular Weight
Formula
Storage
Purity
Chemical Name
CAS Number
PubChem ID
InChI Key
SMILES
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.75 | 100 | |
| Ethanol | 7.75 | 20 |
Preparing Stock Solutions for (Z)-4-Hydroxytamoxifen
The following data is based on the product molecular weight 387.51.
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.58 mL | 12.90 mL | 25.81 mL |
| 5 mM | 0.52 mL | 2.58 mL | 5.16 mL |
| 10 mM | 0.26 mL | 1.29 mL | 2.58 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
Calculators
Background References
References are publications that support the biological activity of the product. See our Citations tab to view 57 publications citing the usage of this product.
- Sula A tamoxifen receptor within a voltage-gated sodium channel. Mol.Cell. 2021 PMID: 33503406
- Seeger Inhibition of human breast cancer cell proliferation with estradiol metabolites is as effective as with tamoxifen. Horm.Metab.Res. 2004 PMID: 15156405
- Davis Small molecule-triggered Cas9 protein with improved genome-editing specificity. Nat.Chem.Biol. 2015 PMID: 25848930
- Yu and Forman Simple and efficient production of (Z)-4-hydroxytamoxifen, a potent estrogen receptor modulator. J.Org.Chem. 2003 PMID: 14629178
- Desta 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 PMID: 15159443
- Jordan A monohydroxylated metabolite of tamox. with potent antioestrogenic activity. J.Endocrinology 1977 PMID: 591813
Product Documents for (Z)-4-Hydroxytamoxifen
Certificate of Analysis
To download a Certificate of Analysis, please enter a lot or batch number in the search box below.
Product Specific Notices for (Z)-4-Hydroxytamoxifen
For research use only
Related Research Areas
Citations for (Z)-4-Hydroxytamoxifen
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Species: MouseAssay Type: In VivoVerified Customer | Posted 05/23/2019.5mg/ml dissolved in 1% tween 80 and 2.5% DMSO, injected 5mg/kg i.p.used for tamoxifen TRAPing using ERT-cre mice. given 3hrs post behavior. single dose was sufficient for recombination
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