Irosustat 是类固醇硫酸酯酶抑制剂(IC50:8 nM)，具有抗乳腺癌作用。

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

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. However, it has no effect on the morphology or proliferation of MCF-7 cells at 10 μM.

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. Moreover, 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.) exhibits 97.9 ± 0.06% inhibition on steroid sulphatase (STS) activity in rat liver.

MCF-7 cells are cultured in growth medium (minimum essential medium (MEM) containing, phenol red, 10% foetal calf serum (FCS) and essential nutrients). When the cells reach 60% confluency, they are treated with Irosustat (0.001-10 μM) in growth medium. After 72 h of incubation, photographs are taken under normal conditions of light and the number of attached cells in each flask is determined using a Coulter cell counter

Irosustat is formulated in propylene glycol.RatsLudwig rats bearing mammary tumors are used in the assay. Tumor development is monitored, and animals are ovariectomized when tumors reach 0.8-1.5 cm in diameter. Tumors are allowed to regress over a 12- to 13-day period to confirm their hormone-dependent status. Regrowth of tumors is stimulated with oestrone sulfate (E1S; 50 μg/day, s.c.). When tumors have regrown, animals continue to receive either E1S alone or E1S plus Irosustat at 10 mg/kg/day or 2 mg/kg/day, p.o., until tumor regression has occurred. Tumor volumes are calculated from two measured diameters.

288628-05-7

C14H15NO5S

309.34

667-Coumate;STX64;BN83495

DMSO:150 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years