Droloxifene
Droloxifene is an anti-estrogen triphenylthylene selective estrogen receptor modulator (SERM); it is an analog of tamoxifen. Droloxifene acts as an estrogen receptor agonist in bone and as an estrogen receptor antagonist in breast tissue. As a result of these actions, this compound exhibits anticancer chemotherapeutic, chemopreventive, anti-osteoporotic, and anti-resorptive benefits. In breast cancer cells, droloxifene decreases production of NO and increases levels of pro-apoptotic TGF-β. Droloxifene increases apoptosis in luteal cells in vivo, increasing levels of c-myc and increasing the Bax/Bcl-2 ratio. In ovariectomized rats that act as a post-menopausal animal model, droloxifene inhibits bone resorption and turnover as well as estrogen-related bone loss. This compound also decreases levels of E-selectin and increases levels if vascular cellular adhesion molecule 1 (VCAM-1) in clinical settings.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18896939
| Cas No. |
82413-20-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C26H29NO2 |
| Formula Wt. |
387.51 |
| Chemical Name |
3-Hydroxytamoxifen |
| IUPAC Name |
3-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol |
| Melting Point |
127-129°C |
| Appearance |
White Crystal Powder |
Shelly W, Draper MW, Krishnan V, et al. Selective estrogen receptor modulators: an update on recent clinical findings. Obstet Gynecol Surv. 2008 Mar;63(3):163-81. PMID: 18279543.
Martin JH, Symonds A, Chohan S. Down-regulation of nitric oxide production by droloxifene and toremifene in human breast cancer cells. Oncol Rep. 2003 Jul-Aug;10(4):979-84. PMID: 12792756
Herrington DM, Brosnihan KB, Pusser BE, et al. Differential effects of E and droloxifene on C-reactive protein and other markers of inflammation in healthy postmenopausal women. J Clin Endocrinol Metab. 2001 Sep;86(9):4216-22. PMID: 11549652.
Leng Y, Feng Y, Cao L, et al. Effects of droloxifene on apoptosis and Bax, Bcl-2 protein expression of luteal cells in pseudopregnant rats. Acta Pharmacol Sin. 2001 Feb;22(2):155-62. PMID: 11741521.
Leng Y, Gu ZP, Cao L. Apoptosis induced by droloxifene and c-myc, bax and bcl-2 mRNA expression in cultured luteal cells of rats. Eur J Pharmacol. 2000 Dec 8;409(2):123-31. PMID: 11104825.
Knabbe C, Zugmaier G, Schmahl M, et al. Induction of transforming growth factor beta by the antiestrogens droloxifene, tamoxifen, and toremifene in MCF-7 cells. Am J Clin Oncol. 1991;14 Suppl 2:S15-20. PMID: 1835818.
