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Endoxifen
- 4OHNDtam - N-Desmethyl-4-hydroxytamoxifen
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C25H27NO2
- MW: 373.49
Description
Endoxifen is an active metabolite of tamoxifen and a selective estrogen receptor modulator (SERM) that potently inhibits estrogen-stimulated BT474 cell growth, with reported IC50 of 54 nM. It is approximately 100-fold more potent than tamoxifen as an ERα antagonist in reported assays.
Endoxifen links CYP-mediated tamoxifen metabolism to estrogen receptor blockade in ER-positive breast cancer. It is relevant for endocrine therapy research, estrogen receptor pharmacology and studies of tamoxifen response variability.
Key Features
- Active tamoxifen metabolite
- Selective estrogen receptor modulator
- Potent ERα antagonist activity
- Inhibits estrogen-stimulated breast cancer cell growth
Applications
- Estrogen receptor pharmacology
- ER-positive breast cancer models
- Tamoxifen metabolism studies
- Endocrine therapy response research
Related products: The water-soluble Endoxifen hydrochloride is available as Axon 2707; the more active Z-isomer is available as Axon 2221.
More Information
| Parent CAS No. | 110025-28-0 |
|---|---|
| Chemical Name | (E/Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol |
| MFCD | MFCD09840374 |
| Short Description | SERM |
References
- 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.
- M. Goetz et al. Tamoxifen, HER2, and Endoxifen: The Role of CYP2D6 as a Predictor of Tamoxifen Resistance in ER+/HER2+ Breast Cancer. Cancer Res 2009, 69, Abstract nr 2006 (S3).
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