CAS 97752-20-0

Droloxifene citrate

Description:

Droloxifene citrate is a synthetic compound that belongs to the class of selective estrogen receptor modulators (SERMs). It is primarily characterized by its ability to bind to estrogen receptors, exerting both estrogenic and anti-estrogenic effects depending on the target tissue. This dual action makes it a candidate for therapeutic applications, particularly in the treatment of hormone-dependent cancers, such as breast cancer, and in managing conditions like osteoporosis. The compound is typically administered in its citrate salt form, which enhances its solubility and bioavailability. Droloxifene citrate has been studied for its potential to reduce the risk of breast cancer recurrence and to alleviate menopausal symptoms. Its pharmacological profile includes a favorable safety margin, although, like other SERMs, it may be associated with side effects such as hot flashes or thromboembolic events. Overall, Droloxifene citrate represents a significant area of research in the field of oncology and women's health, with ongoing studies to fully elucidate its therapeutic potential and mechanisms of action.

Formula: C₂₆H₂₉NO₂·C₆H₈O₇

InChI: InChI=1S/C26H29NO2.C6H8O7/c1-4-25(20-9-6-5-7-10-20)26(22-11-8-12-23(28)19-22)21-13-15-24(16-14-21)29-18-17-27(2)3;7-3(8)1-6(13,5(11)12)2-4(9)10/h5-16,19,28H,4,17-18H2,1-3H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/b26-25+;

InChI key: InChIKey=GTJXPMSTODOYNP-BTKVJIOYSA-N

SMILES: C(=C(/CC)\C1=CC=CC=C1)(\C2=CC=C(OCCN(C)C)C=C2)/C3=CC(O)=CC=C3.C(CC(O)=O)(CC(O)=O)(C(O)=O)O

Synonyms:

• (E)-1-[4'-(2-Dimethylaminoethoxy)phenyl]-1-(3-hydroxyphenyl)-2-phenylbut-1-ene Citrate
• (E)-3-[1-[4-[2-(Dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]phenol Citrate (1:1) (Salt)
• (E)-a-[p-[2-(dimethylamino)ethoxy]phenyl]-a'-ethyl-3-stilbenol Citrate
• 3-[(1E)-1-{4-[2-(Dimethylamino)ethoxy]phenyl}-2-phenylbut-1-en-1-yl]phenol 2-hydroxypropane-1,2,3-tricarboxylate (1:1)
• 3-[(1E)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-2-phenylbut-1-en-1-yl]phenol 2-hydroxypropane-1,2,3-tricarboxylate (salt)
• 97752-20-0
• Droloxifene citrate
• Phenol, 3-[(1E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
• Phenol, 3-[(1E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (salt)
• Phenol, 3-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]-, (E)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (salt)

Droloxifene Citrate

Controlled Product

CAS: 97752-20-0

Applications Droloxifene is a non-steroidal anti-oestrogen that is structurally related to Tamoxifen (T006000), a drug used to prevent the occurrence of breast cancer in postmenopausal women. Droloxifene has a very high binding affinity to estrogen receptors and is used, similarly to Tamoxifen, to prevent and treat breast cancer.
References Coombes, R., et al.: New Engl. J. Med., 350, 1081 (2004); Geisler, J., et al.: J. Ster. Biochem. Mol. Biol., 55, 193 (1995); Hasmann, M., et al.: Cancer Lett., 84, 101 (1994); Powles, T., et al.: Lancet 352, 98 (1998)

Formula: C₂₆H₂₉NO₂·C₆H₈O₇

Color and Shape: Neat

Molecular weight: 579.64

Ref: TR-D679200

Droloxifene citrate

Controlled Product

CAS: 97752-20-0

Droloxifene is a selective estrogen receptor modulator that has been shown to be effective in the treatment of breast cancer. It is also used to treat postmenopausal osteoporosis and prevent osteoporotic fractures. Droloxifene binds to the estrogen receptors, preventing estradiol from binding. This prevents the proliferation of cancer cells, which are dependent on estrogens for growth. The drug has been shown to be well tolerated in human serum and not associated with any adverse effects.

Formula: C₂₆H₂₉NO₂·C₆H₈O₇

Purity: Min. 95%

Molecular weight: 579.64 g/mol

Ref: 3D-FD76626