Irosustat

CAS No. 288628-05-7

Irosustat( STX64 | STX-64 | STX 64 | BN83495 | COUMATE. Irosustat )

Catalog No. M18370 CAS No. 288628-05-7

Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 43 In Stock
5MG 71 In Stock
10MG 120 In Stock
25MG 259 In Stock
50MG 437 In Stock
100MG 626 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    Irosustat
  • Note
    Research use only, not for human use.
  • Brief Description
    Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
  • Description
    Irosustat, also known as STX64, BN83495 and 667 coumate, is a potent, irreversible inhibitor of steroid sulfatase. Inhibition of steroid sulfatase (STS), the enzyme responsible for the hydrolysis of steroid sulfates, represents a potential novel treatment for postmenopausal women with hormone-dependent breast cancer. Estrone and DHEA are formed by this sulfatase pathway and can be converted to steroids (estradiol and androstenediol, respectively), which have potent estrogenic properties. STX64 (667 coumate) is a potent tricylic coumarin-based sulfamate that irreversibly inhibits STS activity (IC50 = 8 nM in a placental microsomal assay system). Estrone sulfamate (EMATE) is also a potent STS inhibitor, but has estrogenic activity.(In Vitro):Irosustat (667 COUMATE) is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM. 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.(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. Irosustat (667 COUMATE; 10 mg/kg, p.o.) shows 97.9 ± 0.06% inhibition on steroid sulphatase (STS) activity in rat liver.
  • In Vitro
    Irosustat (667 COUMATE) is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM. 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.
  • 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. Irosustat (667 COUMATE; 10 mg/kg, p.o.) shows 97.9 ± 0.06% inhibition on steroid sulphatase (STS) activity in rat liver.
  • Synonyms
    STX64 | STX-64 | STX 64 | BN83495 | COUMATE. Irosustat
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    steroid sulfatase
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    288628-05-7
  • Formula Weight
    309.34
  • Molecular Formula
    C14H15NO5S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 150 mg/mL; 484.90 mM
  • SMILES
    NS(=O)(=O)Oc2ccc3C=1CCCCCC=1C(=O)Oc3c2
  • Chemical Name
    6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate.

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Purohit A,etal.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.
molnova catalog
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