Date published: 2026-4-25

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Droloxifene (CAS 82413-20-5)

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Application:
Droloxifene is a phenolic analog of tamoxifen
CAS Number:
82413-20-5
Molecular Weight:
387.51
Molecular Formula:
C26H29NO2
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Droloxifene, an analog of tamoxifen, is an anti-estrogen triphenylthylene selective estrogen receptor modulator. Droloxifene inhibits bone resorption and turnover as well as estrogen-related bone loss in ovariectomized rats.Droloxifene acts as an estrogen receptor agonist in bone and as an estrogen receptor antagonist in breast tissue. 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.


Droloxifene (CAS 82413-20-5) References

  1. Apoptosis induced by droloxifene and c-myc, bax and bcl-2 mRNA expression in cultured luteal cells of rats.  |  Leng, Y., et al. 2000. Eur J Pharmacol. 409: 123-31. PMID: 11104825
  2. Differential effects of E and droloxifene on C-reactive protein and other markers of inflammation in healthy postmenopausal women.  |  Herrington, DM., et al. 2001. J Clin Endocrinol Metab. 86: 4216-22. PMID: 11549652
  3. Effects of droloxifene on apoptosis and Bax, Bcl-2 protein expression of luteal cells in pseudopregnant rats.  |  Leng, Y., et al. 2001. Acta Pharmacol Sin. 22: 155-62. PMID: 11741521
  4. Apoptosis induced by droloxifene and C-myc, Bax, Bcl-2 protein expression in corpus luteum of pregnant rats.  |  Leng, Y., et al. 2001. Acta Pharmacol Sin. 22: 327-34. PMID: 11742585
  5. Down-regulation of nitric oxide production by droloxifene and toremifene in human breast cancer cells.  |  Martin, JH., et al. 2003. Oncol Rep. 10: 979-84. PMID: 12792756
  6. Droloxifene (3-hydroxytamoxifen) has membrane antioxidant ability: potential relevance to its mechanism of therapeutic action in breast cancer.  |  Wiseman, H., et al. 1992. Cancer Lett. 66: 61-8. PMID: 1451097
  7. Anti-implantation effect of droloxifene in rats and its relationship with anti-estrogenic activity.  |  Huang, Y., et al. 2005. Acta Pharmacol Sin. 26: 1243-7. PMID: 16174441
  8. Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.  |  Qin, Z., et al. 2007. J Med Chem. 50: 2682-92. PMID: 17489582
  9. Selective estrogen receptor modulators: an update on recent clinical findings.  |  Shelly, W., et al. 2008. Obstet Gynecol Surv. 63: 163-81. PMID: 18279543
  10. Induction of transforming growth factor beta by the antiestrogens droloxifene, tamoxifen, and toremifene in MCF-7 cells.  |  Knabbe, C., et al. 1991. Am J Clin Oncol. 14 Suppl 2: S15-20. PMID: 1835818
  11. Pharmacologic and biologic properties of droloxifene, a new antiestrogen.  |  Eppenberger, U., et al. 1991. Am J Clin Oncol. 14 Suppl 2: S5-14. PMID: 1962598
  12. Droloxifene, a new estrogen antagonist/agonist, prevents bone loss in ovariectomized rats.  |  Ke, HZ., et al. 1995. Endocrinology. 136: 2435-41. PMID: 7750465
  13. Common mechanism for the estrogen agonist and antagonist activities of droloxifene.  |  Grasser, WA., et al. 1997. J Cell Biochem. 65: 159-71. PMID: 9136075

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Droloxifene, 25 mg

sc-205660
25 mg
$163.00

Droloxifene, 100 mg

sc-205660A
100 mg
$500.00