For research use only. Not for therapeutic Use.
Irosustat (Cat No.: I007362) is a potent and orally active steroid sulfatase inhibitor. It functions by irreversibly inhibiting the activity of steroid sulfatase, an enzyme involved in the metabolism of steroid hormones, including estrogens. By inhibiting this enzyme, Irosustat can reduce the levels of active estrogens in the body. This property makes it of interest in the field of hormone-related conditions, particularly in hormone-dependent cancers like breast and prostate cancer. If you need to, please contact us in time, and we will reply to you as soon as possible within 24 hours.
| Catalog Number | I007362 |
| CAS Number | 288628-05-7 |
| Synonyms | BN83495; BN-83495; BN 83495; STX 64667; STX64667; ST-64667; COUMATE. Irosustat.;6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate. |
| Molecular Formula | C14H15NO5S |
| Purity | ≥95% |
| Target | Steroid Sulfatase |
| Solubility | Soluble in DMSO, not in water |
| Storage | 2-8°C |
| IUPAC Name | (6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-3-yl) sulfamate |
| InChI | InChI=1S/C14H15NO5S/c15-21(17,18)20-9-6-7-11-10-4-2-1-3-5-12(10)14(16)19-13(11)8-9/h6-8H,1-5H2,(H2,15,17,18) |
| InChIKey | DSLPMJSGSBLWRE-UHFFFAOYSA-N |
| SMILES | C1CCC2=C(CC1)C(=O)OC3=C2C=CC(=C3)OS(=O)(=O)N |
| Reference | </br>1:A Phase 2, Randomized, Open-Label Study of Irosustat Versus Megestrol Acetate in Advanced Endometrial Cancer. Pautier P, Vergote I, Joly F, Melichar B, Kutarska E, Hall G, Lisyanskaya A, Reed N, Oaknin A, Ostapenko V, Zvirbule Z, Chetaille E, Geniaux A, Shoaib M, Green JA.Int J Gynecol Cancer. 2017 Feb;27(2):258-266. doi: 10.1097/IGC.0000000000000862. PMID: 27870712 </br>2:Population pharmacokinetic modelling of irosustat in postmenopausal women with oestrogen-receptor positive breast cancer incorporating non-linear red blood cell uptake. Parra-Guillen ZP, Cendrós Carreras JM, Peraire C, Obach R, Prunynosa J, Chetaille E, Trocóniz IF.Pharm Res. 2015 Apr;32(4):1493-504. doi: 10.1007/s11095-014-1555-4. Epub 2014 Oct 30. PMID: 25355461 </br>3:A phase I dose escalation study to determine the optimal biological dose of irosustat, an oral steroid sulfatase inhibitor, in postmenopausal women with estrogen receptor-positive breast cancer. Coombes RC, Cardoso F, Isambert N, Lesimple T, Soulié P, Peraire C, Fohanno V, Kornowski A, Ali T, Schmid P.Breast Cancer Res Treat. 2013 Jul;140(1):73-82. Epub 2013 Jun 25. PMID: 23797179 </br>4:In vitro evaluation of the interaction potential of irosustat with drug-metabolizing enzymes. Ventura V, Solà J, Peraire C, Brée F, Obach R.Drug Metab Dispos. 2012 Jul;40(7):1268-78. doi: 10.1124/dmd.111.044271. Epub 2012 Mar 26. PMID: 22451700 Free Article</br>5:Structure-activity relationship for the first-in-class clinical steroid sulfatase inhibitor Irosustat (STX64, BN83495). Woo LW, Ganeshapillai D, Thomas MP, Sutcliffe OB, Malini B, Mahon MF, Purohit A, Potter BV.ChemMedChem. 2011 Nov 4;6(11):2019-34. doi: 10.1002/cmdc.201100288. Epub 2011 Aug 25. PMID: 21990014 Free PMC Article</br>6:In vitro metabolism of irosustat, a novel steroid sulfatase inhibitor: interspecies comparison, metabolite identification, and metabolic enzyme identification. Ventura V, Solà J, Celma C, Peraire C, Obach R.Drug Metab Dispos. 2011 Jul;39(7):1235-46. doi: 10.1124/dmd.111.038315. Epub 2011 Apr 4. PMID: 21464173 Free Article</br>7:Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer. Palmieri C, Januszewski A, Stanway S, Coombes RC.Expert Rev Anticancer Ther. 2011 Feb;11(2):179-83. doi: 10.1586/era.10.201. Review. Erratum in: Expert Rev Anticancer Ther. 2011 Sep;11(9):1472. PMID: 21342037 |
