Irosustat

SKU: orb1302837

Description

Irosustat (667-Coumate) is a highly potent steroid sulfatase inhibitor, demonstrating an IC50 of 8 nM. It has shown promising anti-cancer activity in breast cancer research, with studies investigating its effects in both in vitro cellular models and in vivo xenograft experiments.

Key Properties

• CAS Number: 288628-05-7
• MW: 309.34
• Purity: 99.33%
• Formula: C₁₄H₁₅NO₅S
• SMILES: NS(=O)(=O)Oc1ccc2c3CCCCCc3c(=O)oc2c1
• Target: Others
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.47 mM);DMSO:55 mg/mL (177.8 mM)

Bioactivity

• Target IC50:
  Steroid sulfatase (MCF-7 cells):0.2 nM|Steroid sulfatase:IC50:8 nM
• In Vivo:
  Irosustat effectively inhibits over 90% of rat liver activity at a concentration of 1 mg/kg. At doses of 2 mg/kg administered orally for five days, it impedes uterine growth induced by oestrone sulfate (E1S) in ovariectomized rats. Additionally, when combined with E1S, Irosustat, at dosages of 2 and 10 mg/kg administered orally, reduces the growth of NMU-induced mammary tumors in these rats in a dose-dependent manner. Moreover, at a dosage of 10 mg/kg administered orally, Irosustat (identified as 667 COUMATE) achieves a 97.9 ± 0.06% inhibition of steroid sulphatase (STS) activity in rat liver.
• In Vitro:
  Irosustat (667 COUMATE), a potent steroid sulfatase inhibitor, exhibits an IC50 of 8 nM and inhibits steroid sulfatase (STS) activity in MCF-7 cells with an IC50 of 0.2 nM, without affecting the morphology or proliferation of MCF-7 cells at 10 μM.
• Cell Research:
  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
• Animal Research:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

667-Coumate, BN 83495, BN83495, BN-83495, Inhibitor, Irosustat, inhibit, STX64, STX-64, STX 64, steroid sulfatase

Compound Identifiers

PubChem CID

5287541