Identification | Back Directory | [Name]
Phenol, 3-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]- | [CAS]
165813-01-4 | [Synonyms]
Phenol, 3-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]- | [Molecular Formula]
C26H29NO2 | [MOL File]
165813-01-4.mol | [Molecular Weight]
387.51 |
Chemical Properties | Back Directory | [Boiling point ]
526.6±50.0 °C(Predicted) | [density ]
1.092±0.06 g/cm3(Predicted) | [solubility ]
DMF: 30 mg/ml DMF: PBS (pH 7.2) (1:3): 0.25 mg/ml DMSO: 15 mg/ml Ethanol: 1 mg/ml | [pka]
9.73±0.10(Predicted) |
Hazard Information | Back Directory | [Uses]
(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]. | [References]
[1] Robertson JF. Selective oestrogen receptor modulators/new antioestrogens: a clinical perspective. Cancer Treat Rev. 2004 Dec;30(8):695-706. DOI:10.1016/j.ctrv.2004.04.003 [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. DOI:10.1254/jjp.63.27 [3] L?ser R, et al. Pharmacological activities of droloxifene isomers. Anticancer Res. 1988 Nov-Dec;8(6):1271-4. PMID:3218958 [4] Hasmann M, et al. Preclinical data for Droloxifene. Cancer Lett. 1994 Sep 15;84(2):101-16. DOI:10.1016/0304-3835(94)90364-6 |
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