MS1943-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMS1943Cat.No.:HY-133129CASNo.:2225938-17-8分?式:C??H??N?O?分?量:718.93作?靶點(diǎn):HistoneMethyltransferase;Apoptosis作?通路:Epigenetics;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(173.87mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.3910mL6.9548mL13.9096mL5mM0.2782mL1.3910mL2.7819mL10mM0.1391mL0.6955mL1.3910mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥6.25mg/mL(8.69mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥6.25mg/mL(8.69mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6.25mg/mL(8.69mM);ClearsolutionBIOLOGICALACTIVITY?物活性MS1943?種?創(chuàng)的，具有?服?物活性的EZH2選擇性降解劑，其IC50為120nM。MS1943顯著降低了許多三性乳腺癌和其他癌及?癌細(xì)胞系中的EZH2蛋??平。MS1943有效地阻?了多個三性乳腺癌和其他癌細(xì)胞系的增殖。IC50&TargetEZH2120nM(IC50)體外研究MS1943(0.625-5μM;3days)inhibitscellgrowthwithanGI50of2.2μM[1].MS1943(0.625-5μM;4days)inducescelldeathinMDA-MB-468cells.MS1943effectivelyreducesEZH2levelsinBT549,HCC70andMDA-MB-231TNBCcells,aswellasKARPAS-422andSUDHL8lymphomacellsandPNT2non-cancerousprostatecells[1].MS1943(1.25-5.0μM;2days)inhibitsEZH2andSUZ12proteinlevelsinaconcentration-andtimedependentmanner,withoutaffectingEEDproteinlevels,whereastheH3K27me3markwasalsosuppressed[1].CellViabilityAssay[1]CellLine:MDA-MB-468cellsConcentration:0.625,1.25,2.5,5μMIncubationTime:3daysResult:InhibitscellgrowthwithanGI50of2.2μM.WesternBlotAnalysis[1]CellLine:MDA-MB-468cellsConcentration:1.25,2.5,5.0μMIncubationTime:2daysResult:ReducedEZH2proteinlevelsinaconcentration-andtime-dependentmanner.體內(nèi)研究MS1943(150mg/kgbodyweight;i.p.;oncedailyfor36days)suppressestumorgrowth[1].MS1943inducesapoptosisintheMDA-MB-468xenograftmodel[1].Asinglei.p.injectionofMS1943at50mg/kgbodyweightachievedapeakplasmaconcentration(Cmax)of2.9μMandresultedinplasmaconcentrationsaboveitscellularIC50valuefor~2h.Asingle150mg/kgbody2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEweightp.o.doseachievedCmaxof1.1μM,butplasmaconcentrationswerebelowthecellularIC50value[1].AnimalModel:Eight-week-oldfemaleBALB/cnudemice(MDA-MB-468xenografts)[1]Dosage:150mg/kgbodyweightAdministration:i.p.;oncedailyfor36daysResult:Suppressestumorgrowth.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ResearchSquarePreprint.2021Dec.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MaA,etal.Discoveryofafirst-in-classEZH2selectivedegrader.NatChemBiol.2020Feb;16(2):214-222.McePdfHeightCaution:Producthasnotbeenfullyval