Title: Droloxifene
CAS Registry Number: 82413-20-5
CAS Name: 3-[(1E)-1-[4-[2-(Dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]phenol
Additional Names: (E)-a-[p-[2-(dimethylamino)ethoxy]phenyl]--ethyl-3-stilbenol; (E)-1-[4¢-(2-dimethylaminoethoxy)phenyl]-1-(3-hydroxyphenyl)-2-phenylbut-1-ene; 3-hydroxytamoxifen
Molecular Formula: C26H29NO2
Molecular Weight: 387.51
Percent Composition: C 80.59%, H 7.54%, N 3.61%, O 8.26%
Literature References: Estrogen-receptor antagonist. Prepn: H. Schickaneder et al., EP 54168; eidem, US 5047431 (1982, 1991 both to Klinge); P. C. Ruenitz et al., J. Med. Chem. 25, 1056 (1982). Symposium on pharmacology and clinical studies: Am. J. Clin. Oncol. 14, Suppl. 2, S1-S63 (1991). Clinical trial in breast cancer: P. F. Bruning, Eur. J. Cancer 28A, 1404 (1992).
Properties: Colorless crystals from ether, mp 162-163° (Schickaneder); also reported as white crystals from benzene-hexane, mp 160-162° (Ruenitz).
Melting point: mp 162-163° (Schickaneder); mp 160-162° (Ruenitz)
Derivative Type: Citrate
CAS Registry Number: 97752-20-0
Manufacturers' Codes: K-21060E; FK-435
Molecular Formula: C26H29NO2.C6H8O7
Molecular Weight: 579.64
Percent Composition: C 66.31%, H 6.43%, N 2.42%, O 24.84%
Properties: Slightly sol in water, methanol, ethanol. Insol in chloroform.
Therap-Cat: Antineoplastic (hormonal).
Keywords: Antineoplastic (Hormonal); Antiestrogens; Selective Estrogen Receptor Modulator (SERM).

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