| Bioactivity | Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity. | ||||||||||||
| Target | IC50: 8 nM (Steroid sulfatase), 0.2 nM (Steroid sulfatase, MCF-7 cells) | ||||||||||||
| Invitro | Irosustat (667 COUMATE) is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM[1]. Irosustat (667 COUMATE) inhibits steroid sulphatase (STS) activity in MCF-7 cells with an IC50 of 0.2 nM, but has no effect on the morphology or proliferation of MCF-7 cells at 10 μM[2]. | ||||||||||||
| 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]. | ||||||||||||
| Name | Irosustat | ||||||||||||
| CAS | 288628-05-7 | ||||||||||||
| Formula | C14H15NO5S | ||||||||||||
| Molar Mass | 309.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |