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Irosustat

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Chemical Structure| 288628-05-7 同义名 : STX64;BN83495;COUMATE. Irosustat.;ST-64667;STX 64667;667-Coumate
CAS号 : 288628-05-7
货号 : A579242
分子式 : C14H15NO5S
纯度 : 99%+
分子量 : 309.338
MDL号 : MFCD12912443
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(339.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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
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

[1]Palmieri C, Stein RC, et al. IRIS study: a phase II study of the steroid sulfatase inhibitor Irosustat when added to an aromatase inhibitor in ER-positive breast cancer patients. Breast Cancer Res Treat. 2017 Jun 13.

[2]Thomas MP, Potter BV. Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health. J Med Chem. 2015 Oct 8;58(19):7634-58.

[3]Purohit A, Woo LW, Potter BV, Reed MJ. 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.