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Endoxifen hydrochloride
- (E/Z)-Endoxifen hydrochloride
- Parent CAS: 110025-28-0
- Soluble in water and DMSO
- MF: C25H27NO2.HCl
- MW: 409.95
Description
Metabolite of Tamoxifen and a selective estrogen receptor modulator (SERM); Potently inhibits the growth of estrogen-stimulated BT474 cells (IC50: 54 nM). Approximately 100-fold more potent as an antagonist of the ERα than the parent drug. Drug for the treatment of estrogen receptor (ER) positive breast cancer.
Hydrochloride salt of Endoxifen (Axon 2190) which dissolves readily in water and aqueous media. The more active isomer, Z-Endoxifen (Axon 2221) is also available.
More Information
| Parent CAS No. | 110025-28-0 |
|---|---|
| Chemical Name | 4-(1-(4-(2-(Methylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol hydrochloride |
| SMILES | C1(O)=CC=C(C(C2=CC=C(OCCNC)C=C2)=C(C2=CC=CC=C2)CC)C=C1.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C25H27NO2.ClH/c1-3-24(19-7-5-4-6-8-19)25(20-9-13-22(27)14-10-20)21-11-15-23(16-12-21)28-18-17-26-2;/h4-16,26-27H,3,17-18H2,1-2H3;1H |
| InChiKey | RPFIMPDXTABYCN-UHFFFAOYSA-N |
| CID | 54613017 |
| 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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