生物活性 | |||
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描述 | The steroid sulfatase hydrolyses estrone sulfate and plays a key role in the regulation of estrogenic steroid formation. The inhibition of steroid sulfatase is an important therapeutic strategy for the treatment of postmenopausal women with breast cancer. Irosustat is a potent inhibitor of steroid sulfatase with an IC50 value of 8nM in a placental microsome assay. It is an orally active, irreversible, and nonsteroidal inhibitor. A single dose of irosustat (10mg/kg, p.o.) inhibited estrone sulfatase activity in rat liver by 93%. Administration of irosustat (2mg/kg, p.o.) for 5 days inhibited estrone sulfate-stimulated growth of uteri in ovariectomized rats. Irosustat (2 and 10mg/kg, p.o.) also suppressed estrone sulfate-stimulated tumor growth in a dose-dependent manner[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.23mL 0.65mL 0.32mL |
16.16mL 3.23mL 1.62mL |
32.33mL 6.47mL 3.23mL |
参考文献 |
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