Irosustat-STX64-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIrosustatCat.No.:HY-14586CASNo.:288628-05-7Synonyms:STX64;BN83495;667-Coumate分⼦式:C₁₄H₁₅NO₅S分⼦量:309.34作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(323.27mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2327mL16.1634mL32.3269mL5mM0.6465mL3.2327mL6.4654mL10mM0.3233mL1.6163mL3.2327mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.08mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.08mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.08mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Irosustat⼀种有效的类醇硫酸酯酶(steroidsulfatase)抑制剂，IC50值为8nM，具有抗乳腺癌的活性。IC50&TargetIC50:8nM(Steroidsulfatase)[1],0.2nM(Steroidsulfatase,MCF-7cells)[2]体外研究Irosustat(667COUMATE)isapotentsteroidsulfataseinhibitor,withanIC50of8nM[1].Irosustat(667COUMATE)inhibitssteroidsulphatase(STS)activityinMCF-7cellswithanIC50of0.2nM,buthasnoeffectonthemorphologyorproliferationofMCF-7cellsat10μM[2].体内研究Irosustatpotentlyinhibitsratliver,withinhibitionof>90%whenata1mg/kgconcentration.Irosustat(2mg/kg,p.o.for5d)blockstheuterinegrowthstimulatedbyoestronesulfate(E1S)inovariectomizedrats.Inaddition,Irosustat(2,10mg/kg,p.o.)plusE1Sdose-dependentlydecreasesthegrowthofNMU-inducedmammarytumorsinovariectomizedrats[1].Irosustat(667COUMATE;10mg/kg,p.o.)shows97.9±0.06%inhibitiononsteroidsulphatase(STS)activityinratliver[2].PROTOCOLCellAssay[2]MCF-7cellsareculturedingrowthmedium(minimumessentialmedium(MEM)containing,phenolred,10%foetalcalfserum(FCS)andessentialnutrients).Whenthecellsreach60%confluency,theyaretreatedwithIrosustat(0.001-10μM)ingrowthmedium.After72hofincubation,photographsaretakenundernormalconditionsoflightandthenumberofattachedcellsineachflaskisdeterminedusingaCoultercellcounter[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats[1]Administration[1]Ludwigratsbearingmammarytumorsareusedintheassay.Tumordevelopmentismonitored,andanimalsareovariectomizedwhentumorsreach0.8-1.5cmindiameter.Tumorsareallowedtoregressovera12-to13-dayperiodtoconfirmtheirhormone-dependentstatus.Regrowthoftumorsisstimulatedwithoestronesulfate(E1S;50μg/day,s.c.).Whentumorshaveregrown,animalscontinuetoreceiveeitherE1SaloneorE1SplusIrosustatat10mg/kg/dayor2mg/kg/day,p.o.,untiltumorregressionhasoccurred.Tumorvolumesarecalculatedfromtwomeasureddiameters[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•MolCellEndocrinol.2022Jan15;111561.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PurohitA,etal.Invivoinhibitionofestronesulfataseactivityandgrowthofnitrosomethylurea-inducedmammarytumorsby667COUMATE.CancerRes.2000Jul1;60(13):3394-6.[2].RaobaikadyB,etal.InhibitionofMCF-7breastcancercellproliferationandinvivosteroidsulphataseactivityby2-methoxyoestradiol-bis-sulphamate.JSteroidBiochemMolBiol.2003Feb;84(2-3):351-8.McePdfHeig