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(Z)-Endoxifen
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C25H27NO2
- MW: 373.49
Description
(Z)-Endoxifen is the more active Z-isomer of endoxifen (Axon 2190), an active tamoxifen metabolite and selective estrogen receptor modulator. It inhibits estrogen-stimulated MCF-7 proliferation with reported IC50 values of 0.01–0.10 µM and potently inhibits growth of estrogen-stimulated BT474 cells.
Z-Endoxifen is a key mediator of tamoxifen pharmacology and provides much stronger (approximately 100-fold) ERα antagonism than the parent drug in reported assays. It is relevant for endocrine therapy research and ER-positive breast cancer model systems.
Key Features
- Active Z-isomer of endoxifen
- Selective estrogen receptor modulator
- Potent antagonist of ERα-driven proliferation
- Key metabolite in tamoxifen pharmacology
Applications
- Estrogen receptor pharmacology
- ER-positive breast cancer research
- Tamoxifen metabolite studies
- Endocrine therapy response assays
More Information
| Parent CAS No. | 112093-28-4 |
|---|---|
| Chemical Name | (Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol |
| MFCD | MFCD09840374 |
| Short Description | SERM |
References
- P. Elkins et al. Characterization of the isomeric configuration and impurities of (Z)-endoxifen by 2D-NMR, high resolution LC-MS, and quantitative HPLC analysis. J. Pharm. Biomed. Anal. 2014, 88, 174-179.
- J.R. Hawse et al. Endoxifen’s Molecular Mechanisms of Action Are Concentration Dependent and Different than That of Other Anti-Estrogens. PLoS One. 2013, 8, e54613.
- A Ahmad et al. Endoxifen, a New Cornerstone of Breast Cancer Therapy: Demonstration of Safety, Tolerability, and Systemic Bioavailability in Healthy Human Subjects. Clin. Pharmacol. Ther. 2010, 88(6), 814–817.
- M.D. Johnson et al. Pharmacological Characterization of 4-hydroxy-N-desmethyl Tamoxifen, a Novel Active Metabolite of Tamoxifen. Breast Cancer Research and Treatment 2004, 85, 151-159.
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