Title: Arzoxifene
CAS Registry Number: 182133-25-1
CAS Name: 2-(4-Methoxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]benzo[
b]thiophene-6-ol
Synonyms: [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]2-(4-methoxyphenyl)]benzo[
b]thiophene
Manufacturers' Codes: LY-353381
Molecular Formula: C28H29NO4S
Molecular Weight: 475.60
Percent Composition: C 70.71%, H 6.15%, N 2.95%, O 13.46%, S 6.74%
Literature References: Selective estrogen receptor modulator (SERM). Prepn: A. D. Palkowitz, K. J. Thrasher,
EP 729956;
idem, US 5981765 (1996, 1999 both to Eli Lilly). Pharmacology: M. Sato
et al., Endocrinology 139, 4642 (1998); N. Suh
et al., Cancer Res. 61, 8412 (2001). Clinical pharmacokinetics: P. N. Münster
et al., J. Clin. Oncol. 19, 2002 (2001). Review of clinical evaluations and therapeutic potential: S. Chan,
Semin. Oncol. 29, Suppl. 1, 129-133 (2002).
Properties: Solid from hexane, mp 174-176°.
Melting point: mp 174-176°
Derivative Type: Hydrochloride
CAS Registry Number: 182133-27-3
Molecular Formula: C28H29NO4S.HCl
Molecular Weight: 512.06
Percent Composition: C 65.68%, H 5.91%, N 2.74%, O 12.50%, S 6.26%, Cl 6.92%
Properties: Crystals from ethanol/ethyl acetate, mp 156-160°.
Melting point: mp 156-160°
Therap-Cat: Antineoplastic (hormonal).
Keywords: Antineoplastic (Hormonal); Antiestrogens; Selective Estrogen Receptor Modulator (SERM).