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Droloxifene

Droloxifene

Product ID D6957
Cas No. 82413-20-5
Purity ≥98%
Product Unit SizeCostQuantityStock
5 mg $97.70 In stock
25 mg $183.10 In stock
100 mg $563.60 In stock
250 mg $986.20 In stock
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Quicklinks

  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Custom Order

Description

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.

Product Info

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

Synonym

E-Droloxifene; 3-HYDROXYTAMOXIFEN; Droloxifenum [Latin]; Droloxifeno [Spanish]; FK-435

Melting Point

127-129°C

Solubility

Soluble in DMSO, Methanol. Insoluble in water.

Appearance

White Crystal Powder

Shipping and Storage

Store Temp

Ambient

Ship Temp

Ambient

Downloads

MSDS

D6957 MSDS PDF

Info Sheet

D6957 Info Sheet PDF

References

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.

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