Irosustat-STX64-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIrosustatCat.No.:HY-14586CASNo.:288628-05-7Synonyms:STX64;BN83495;667-Coumate分?式:C??H??NO?S分?量:309.34作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(323.27mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.2327mL16.1634mL32.3269mL5mM0.6465mL3.2327mL6.4654mL10mM0.3233mL1.6163mL3.2327mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(8.08mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.08mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性Irosustat?種有效的類(lèi)醇硫酸酯酶(steroidsulfatase)抑制劑，IC50值為8nM，具有抗乳腺癌的活性。IC50&TargetIC50:8nM(Steroidsulfatase)[1],0.2nM(Steroidsulfatase,MCF-7cells)[2]體外研究Irosustat(667COUMATE)isapotentsteroidsulfataseinhibitor,withanIC50of8nM[1].Irosustat(667COUMATE)inhibitssteroidsulphatase(STS)activityinMCF-7cellswithanIC50of0.2nM,buthasnoeffectonthemorphologyorproliferationofMCF-7cellsat10μM[2].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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