[CAS NO. 288628-05-7] Irosustat
PRODUCTS SPECIFICATIONS [288628-05-7]
DESCRIPTION [288628-05-7]
Overview
| MDL | MFCD12912443 |
|---|---|
| Molecular Weight | 309.34 |
| Molecular Formula | C14H15NO5S |
| SMILES | O=C1OC2=CC(OS(=O)(N)=O)=CC=C2C3=C1CCCCC3 |
1 Publications Citing Use of MCE
Summary
Irosustat is a potent steroid sulfatase inhibitor, with an IC 50 of 8 nM, and exhibits anti-breast cancer activity.
In Vitro
Irosustat (667 COUMATE) is a potent steroid sulfatase inhibitor, with an IC 50 of 8 nM [1] . Irosustat (667 COUMATE) inhibits steroid sulphatase (STS) activity in MCF-7 cells with an IC 50 of 0.2 nM, but has no effect on the morphology or proliferation of MCF-7 cells at 10 μM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Irosustat potently inhibits rat liver, with inhibition of >90% when at a 1 mg/kg concentration. Irosustat (2 mg/kg, p.o. for 5 d) blocks the uterine growth stimulated by oestrone sulfate (E1S) in ovariectomized rats. In addition, Irosustat (2, 10 mg/kg, p.o.) plus E1S dose-dependently decreases the growth of NMU-induced mammary tumors in ovariectomized rats [1] . Irosustat (667 COUMATE; 10 mg/kg, p.o.) shows 97.9 ± 0.06% inhibition on steroid sulphatase (STS) activity in rat liver [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 |
|---|---|---|---|---|
| NCT01662726 | Imperial College London|National Institute for Health Research, United Kingdom|Ipsen|Imperial College Healthcare NHS Trust|Guy´s and St Thomas´ NHS Foundation Trust|University of Southern California|QPS Netherlands B.V. |
Breast Neoplasms
|
August 2012 | Phase 2 |
| NCT01840488 | Ipsen |
Breast Cancer
|
April 2007 | Phase 1 |
| NCT01785992 | Imperial College London|Cancer Research UK |
Locally Advanced Breast Cancer|Metastatic Breast Cancer
|
October 2012 | Phase 2 |
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 : 100 mg/mL ( 323.27 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2327 mL | 16.1634 mL | 32.3269 mL |
| 5 mM | 0.6465 mL | 3.2327 mL | 6.4654 mL |
| 10 mM | 0.3233 mL | 1.6163 mL | 3.2327 mL |
References
- [1] Purohit A, et al. In vivo inhibition of estrone sulfatase activity and growth of nitrosomethylurea-induced mammary tumors by 667 COUMATE. Cancer Res. 2000 Jul 1;60(13):3394-6.
- [2] Raobaikady B, et al. Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2-methoxyoestradiol-bis-sulphamate. J Steroid Biochem Mol Biol. 2003 Feb;84(2-3):351-8.
Synonyms