Arzoxifene

Modify Date: 2024-01-05 19:16:35

Arzoxifene Structure
Arzoxifene structure
Common Name Arzoxifene
CAS Number 182133-25-1 Molecular Weight 475.59900
Density 1.234g/cm3 Boiling Point 656.4ºC at 760mmHg
Molecular Formula C28H29NO4S Melting Point N/A
MSDS N/A Flash Point 350.8ºC

 Use of Arzoxifene


Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile[1].

 Names

Name 2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol
Synonym More Synonyms

 Arzoxifene Biological Activity

Description Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile[1].
Related Catalog
Target

estrogen[1]

In Vitro Arzoxifene reduces estrogen receptor expression in endometrial cancer cell lines (ECC-1)[1].
In Vivo Arzoxifene inhibits MCF-7 breast cancer xenograft growth in oophorectomized athymic mice. Arzoxifene is reported to prevent body weight increase in oophorectomized rats[1].
References

[1]. Jackson LR, et al. Arzoxifene: the evidence for its development in the management of breast cancer. Core Evid. 2008;2(4):251-258.

 Chemical & Physical Properties

Density 1.234g/cm3
Boiling Point 656.4ºC at 760mmHg
Molecular Formula C28H29NO4S
Molecular Weight 475.59900
Flash Point 350.8ºC
Exact Mass 475.18200
PSA 79.40000
LogP 6.87740
Vapour Pressure 7.85E-18mmHg at 25°C
Index of Refraction 1.635

 Synthetic Route

~%

Arzoxifene Structure

Arzoxifene

CAS#:182133-25-1

Literature: Eli Lilly and Company Patent: US6653479 B1, 2003 ; Location in patent: Page/Page column 7-8 ;

~91%

Arzoxifene Structure

Arzoxifene

CAS#:182133-25-1

Literature: Eli Lilly and Company Patent: US6077852 A1, 2000 ; US 6077852 A

~85%

Arzoxifene Structure

Arzoxifene

CAS#:182133-25-1

Literature: Qin, Zhihui; Kastrati, Irida; Chandrasena, R. Esala P.; Liu, Hong; Yao, Ping; Petukhov, Pavel A.; Bolton, Judy L.; Thatcher, Gregory R. J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 11 p. 2682 - 2692

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Arzoxifene Structure

Arzoxifene

CAS#:182133-25-1

Literature: Qin, Zhihui; Kastrati, Irida; Chandrasena, R. Esala P.; Liu, Hong; Yao, Ping; Petukhov, Pavel A.; Bolton, Judy L.; Thatcher, Gregory R. J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 11 p. 2682 - 2692

~%

Arzoxifene Structure

Arzoxifene

CAS#:182133-25-1

Literature: Qin, Zhihui; Kastrati, Irida; Chandrasena, R. Esala P.; Liu, Hong; Yao, Ping; Petukhov, Pavel A.; Bolton, Judy L.; Thatcher, Gregory R. J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 11 p. 2682 - 2692

~%

Arzoxifene Structure

Arzoxifene

CAS#:182133-25-1

Literature: Qin, Zhihui; Kastrati, Irida; Chandrasena, R. Esala P.; Liu, Hong; Yao, Ping; Petukhov, Pavel A.; Bolton, Judy L.; Thatcher, Gregory R. J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 11 p. 2682 - 2692

 Synonyms

Arzoxifene
UNII-E569WG6E60