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Irosustat

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Catalog No. T4464Cas No. 288628-05-7
Alias STX64, BN83495, 667-Coumate

Irosustat (667-Coumate) is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.

Irosustat

Irosustat

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Purity: 99.33%
Catalog No. T4464Alias STX64, BN83495, 667-CoumateCas No. 288628-05-7
Irosustat (667-Coumate) is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30In StockIn Stock
5 mg$47In StockIn Stock
10 mg$80In StockIn Stock
25 mg$173In StockIn Stock
50 mg$292In StockIn Stock
100 mg$417In StockIn Stock
200 mg$593-In Stock
1 mL x 10 mM (in DMSO)$48In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.33%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Irosustat (667-Coumate) is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
Targets&IC50
Steroid sulfatase:IC50:8 nM, Steroid sulfatase (MCF-7 cells):0.2 nM
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.
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.
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.
SynonymsSTX64, BN83495, 667-Coumate
Chemical Properties
Molecular Weight309.34
FormulaC14H15NO5S
Cas No.288628-05-7
SmilesNS(=O)(=O)Oc1ccc2c3CCCCCc3c(=O)oc2c1
Relative Density.1.48 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (177.8 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.47 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2327 mL16.1634 mL32.3269 mL161.6344 mL
5 mM0.6465 mL3.2327 mL6.4654 mL32.3269 mL
10 mM0.3233 mL1.6163 mL3.2327 mL16.1634 mL
20 mM0.1616 mL0.8082 mL1.6163 mL8.0817 mL
50 mM0.0647 mL0.3233 mL0.6465 mL3.2327 mL
100 mM0.0323 mL0.1616 mL0.3233 mL1.6163 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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