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Purity: ≥98%
Irosustat (formerly known as STX64, BN83495 or 667 coumate) is a novel potent and irreversible inhibitor of steroid sulfatase with an IC50 of 8 nM and has the potential for treating breast cancer. The development of potent steroid sulfatase inhibitors is an important new therapeutic strategy for the treatment of postmenopausal women with breast cancer. In a placental microsomal assay system, Irosustat emerged as the most potent inhibitor with an IC50 of 8 nM. Administration of a single dose (10 mg/kg, p.o.) of Irosustat inhibited rat liver estrone sulfatase activity by 93%. Irosustat was devoid of estrogenicity, as indicated by its failure to stimulate the growth of uteri in ovariectomized rats. In vivo, estrone sulfate-stimulated growth of uteri in ovariectomized rats was inhibited by Irosustat. Using the nitrosomethylurea-induced mammary tumor model, it was found that Irosustat caused regression of estrone sulfate-stimulated tumor growth in a dose-dependent manner. The identification of Irosustat as a potent steroid sulfatase inhibitor will enable the therapeutic potential of this type of therapy to be evaluated.
| ln Vitro |
With an IC50 of 8 nM, Irosustat (667 COUMATE) is a strong inhibitor of steroid sulfatase [1]. At 10 μM, isosustat (667 COUMATE) has no effect on MCF-7 cell shape or proliferation, but it inhibits the activity of steroid sulfatase (STS) in these cells with an IC50 of 0.2 nM [2].
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| ln Vivo |
Rat liver is efficiently inhibited by isosustat; at 1 mg/kg, >90% inhibition is seen. In ovariectomized rats, irosustat (2 mg/kg orally for 5 days) inhibits the development of the uterus in response to estrone sulfate (E1S). Moreover, in ovariectomized rats, the growth of NMU-induced mammary tumors was dose-dependently inhibited by Irosustat (2, 10 mg/kg, oral) in combination with E1S [1]. Steroid sulfatase (STS) activity in rat liver was inhibited by 97.9 ± 0.06% when Irosustat (667 COUMATE; 10 mg/kg, oral) was administered [2].
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| References |
[1]. Purohit A, et al. 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.
[2]. Raobaikady B, et al. Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2-methoxyoestradiol-bis-sulphamate. J Steroid Biochem Mol Biol. 2003 Feb;84(2-3):351-8 |
| Molecular Formula |
C14H15NO5S
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| Molecular Weight |
309.34
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| CAS # |
288628-05-7
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| Related CAS # |
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| SMILES |
O=S(OC1=CC(O2)=C(C=C1)C(CCCCC3)=C3C2=O)(N)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2327 mL | 16.1634 mL | 32.3269 mL | |
| 5 mM | 0.6465 mL | 3.2327 mL | 6.4654 mL | |
| 10 mM | 0.3233 mL | 1.6163 mL | 3.2327 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inactivation of E1-STS activity in placental microsomes by 665 COUMATE, 666 COUMATE, 667 COUMATE, 668 COUMATE, and 676 OXEPIN.Cancer Res.2000 Jul 1;60(13):3394-6. |
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Effect of E1S or E1S plus 667 COUMATE on the growth of NMU-induced mammary tumors in ovariectomized rats.Cancer Res.2000 Jul 1;60(13):3394-6. |
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COA
Effect of E1S, 667 COUMATE, or E1S plus 667 COUMATE on uterine growth.