(E/Z) -Droloxifene

(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].

Product Specifications

CAS Number

[165813-01-4]

Product Name Alternative

(E/Z) -3-Hydroxytamoxifen

UNSPSC

12352005

Target

Apoptosis; Estrogen Receptor/ERR

Related Pathways

Apoptosis; Vitamin D Related/Nuclear Receptor

Field of Research

Cancer

Smiles

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

Molecular Formula

C26H29NO2

Molecular Weight

387.51

References & Citations

[1]Robertson JF. Selective oestrogen receptor modulators/new antioestrogens: a clinical perspective. Cancer Treat Rev. 2004 Dec;30 (8) :695-706.|[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. |[3]Löser R, et al. Pharmacological activities of droloxifene isomers. Anticancer Res. 1988 Nov-Dec;8 (6) :1271-4.|[4]Hasmann M, et al. Preclinical data for Droloxifene. Cancer Lett. 1994 Sep 15;84 (2) :101-16.