Prinaberel-ERB-041-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPrinaberelCat.No.:HY-14933CASNo.:524684-52-4Synonyms:ERB-041分?式:C??H??FNO?分?量:271.24作?靶點(diǎn):EstrogenReceptor/ERR;Wnt;Apoptosis作?通路:Others;StemCell/Wnt;Apoptosis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:≥40mg/mL(147.47mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.6868mL18.4339mL36.8677mL5mM0.7374mL3.6868mL7.3735mL10mM0.3687mL1.8434mL3.6868mL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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/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:≥5mg/mL(18.43mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:5mg/mL(18.43mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(18.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性Prinaberel(ERB-041)?種有效的選擇性雌激素受體β(ERβ)激動(dòng)劑，對(duì)?，??和??ERβ的IC50分別為5.4、3.1和3.7nM。Prinaberel對(duì)ERβ的選擇性ERα的200倍以上。Prinaberel有效的?膚癌化學(xué)預(yù)防劑，可通過抑制WNT/β-catenin信號(hào)通路發(fā)揮作?。Prinaberel誘導(dǎo)巢癌細(xì)胞凋亡(apoptosis)。IC50&TargethERβratERβmouseERβhERα5.4nM(IC50)3.1nM(IC50)3.7nM(IC50)1200nM(IC50)mouseERαratERα750nM(IC50)620nM(IC50)體外研究Prinaberel(ERB-041)(0-60μM;24hours)treatmentofhumanSCCcellsinducescelldifferentiation,cellcyclearrestandreducescolonyformation[2].Prinaberelshowsamarkedreductionintheexpressionofinflammationregulatoryproteinssuchasp-NFκBp65,iNOSandCOX-2inA431cells.Prinabereldiminishesphosphorylated-PI3Kand-AKT,whichisassociatedwiththeenhancementinE-cadherinexpressionandreductioninmigrationofA431cells[2].Prinaberel(0.01-10μM)inhibitscellproliferationinadose-andtime-dependentmanner[3].Prinaberel(10μM;48hours)promotesovariancancer(SKOV-3cells)apoptosis[3].WesternBlotAnalysis[2]CellLine:A431cellsConcentration:0,20,40and60μMIncubationTime:24hoursResult:ReductionintheexpressionofG1cyclins(D1,D2andD3)andCDK4.CellProliferationAssay[3]CellLine:SKOV-3,A2780CPorOVCAR-3cellsConcentration:0.01,0.1and10μMIncubationTime:24-48hoursResult:Showedsignificantlyinhibitoryeffectoncellproliferation.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)研究Prinaberel(2mg/mouse;topically;30minpriortoUVBirradiationfor30weeks)suppressesdevelopmentofsquamouscellcarcinomainSKH-1hairlessmice[2].PrinaberelreducesproliferationandangiogenesisandinducesapoptosisinUVB-inducedskintumors.Prinaberelsuppressespro-inflammatorysignalingpathwayinUVB-inducedskintumors.PrinabereldiminishedtumorinvasivenessviaPI3K-AKTpathwayandWNTsignaling[2].AnimalModel:Six-toeight-weeks-oldSKH-1hairlessfemalemice[2]Dosage:2mg/mousein200μlethanolAdministration:Topically;30minpriortoUVB(180mJ/cm2)irradiationfor30weeksResult:DiminishedUVB-inducedskintumordevelopmentinSKH-1hairlessmice.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ResearchSquarePreprint.2021Jul.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MalamasMS,etal.Designandsynthesisofaryldiphenolicazolesaspotentandselectiveestrogenreceptor-betaligands.JMedChem.2004;47(21):5021-5040.[2].ChaudharySC,etal.Erb-041,anestrogenreceptor-βagonist,inhibitsskinphotocarcinogenesisinSKH-1hairlessmicebydownregulatingtheWNTsignalingpathway.CancerPrevRes(Phila).2014;7(2):186-198.[3].ChanKKL,etal.Estrogenreceptormodulatorsgenistein,daidzeinandERB-041inhibitcellmigration,invasion,proliferationandsphereformationviamodulationofFAKandPI3K/AKTsignalinginovariancancer.CancerCellInt.2018;18:65.Published2018Mce