[CAS NO. 182133-27-3] Arzoxifenehydrochloride
PRODUCTS SPECIFICATIONS [182133-27-3]
DESCRIPTION [182133-27-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 512.06 |
| Molecular Formula | C28H30ClNO4S |
| SMILES | OC1=CC=C(C(OC2=CC=C(OCCN3CCCCC3)C=C2)=C(C4=CC=C(OC)C=C4)S5)C5=C1.[H]Cl |
Summary
Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol .
IC50 & Target
Estrogen receptor [1]
In Vitro
Arzoxifene inhibits cell growth as effectively as the antiestrogen tamoxifen. Northern analysis reveals that arzoxifene exerts a statistically significant inhibition of pS2 and progesterone receptor B mRNA expression. Significant agonistic effect is observed on the antitrypsin mRNA expression. In contrast to estradiol and tamoxifen, arzoxifene does not upregulate cathepsin D mRNA and protein expression [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Arzoxifene prevents the ovariectomy-induced increase in body weight and serum cholesterol levels of treated rats and lowers them to below sham levels in a dose dependent manner, with maximum efficacy similar to estrogen or raloxifene. Arzoxifene (LY353381.HCl) prevents loss of bone due to ovariectomy with an ED 50 of about 0.01 mg/kg with maximal efficacy observed at 0.1-1 mg/kg/day. Arzoxifene (LY353381.HCl) antagonizes the estrogen-induced elevation in uterine weight down to vehicle-dosed control levels with ED 50 of 0.03 mg/kg/day [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00003428 | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) |
Breast Cancer
|
May 1998 | Phase 2 |
| NCT00005886 | University of Kansas Medical Center|National Cancer Institute (NCI) |
Breast Cancer
|
July 2000 | Phase 1 |
| NCT00003670 | Eli Lilly and Company |
Ovarian Cancer|Primary Peritoneal Cavity Cancer
|
October 1998 | Phase 2 |
| NCT00034125 | Eli Lilly and Company |
Breast Neoplasms
|
Phase 3 | |
| NCT00088010 | Eli Lilly and Company |
Osteoporosis, Postmenopausal
|
June 2004 | Phase 3 |
| NCT00383422 | Eli Lilly and Company |
Osteoporosis, Postmenopausal
|
October 2006 | Phase 3 |
| NCT00005879 | University of Kansas Medical Center|National Cancer Institute (NCI) |
Breast Cancer
|
August 2000 | Phase 2 |
| NCT00253539 | The Cleveland Clinic|National Cancer Institute (NCI) |
Breast Cancer|Hereditary Breast+Ovarian Cancer (brca1, brca2)
|
January 2002 | Phase 2 |
| NCT00003669 | Eli Lilly and Company |
Endometrial Cancer
|
November 1998 | Phase 2 |
| NCT00767299 | Eli Lilly and Company |
Osteoporosis
|
December 2008 | Phase 2 |
| NCT00085956 | Eli Lilly and Company |
Postmenopausal Bone Loss
|
April 2004 | Phase 3 |
| NCT00190697 | Eli Lilly and Company |
Breast Cancer|Endometrial Cancer|Ovarian Cancer
|
January 2001 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 48.82 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9529 mL | 9.7645 mL | 19.5290 mL |
| 5 mM | 0.3906 mL | 1.9529 mL | 3.9058 mL |
| 10 mM | 0.1953 mL | 0.9764 mL | 1.9529 mL |
Synonyms