(E/Z)-Droloxifene  (Synonyms: (E/Z)-3-Hydroxytamoxifen)

(E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC₅₀ value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity^[1][2][3][4].

387.51

C₂₆H₂₉NO₂

165813-01-4

OC1=CC=CC(/C(C2=CC=C(C=C2)OCCN(C)C)=C(CC)/C3=CC=CC=C3)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Robertson JF. Selective oestrogen receptor modulators/new antioestrogens: a clinical perspective. Cancer Treat Rev. 2004 Dec;30(8):695-706.  [Content Brief]

  [2]. Kawamura I, et al. The estrogenic and antiestrogenic activities of droloxifene in human breast cancers. Jpn J Pharmacol. 1993 Sep;63(1):27-34.  [Content Brief]

  [3]. Löser R, et al. Pharmacological activities of droloxifene isomers. Anticancer Res. 1988 Nov-Dec;8(6):1271-4.  [Content Brief]

  [4]. Hasmann M, et al. Preclinical data for Droloxifene. Cancer Lett. 1994 Sep 15;84(2):101-16.  [Content Brief]