MB710-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMB710Cat.No.:HY-120373CASNo.:2230044-57-0分?式:C??H??IN?O?S分?量:457.29作?靶點(diǎn):MDM-2/p53作?通路: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:25mg/mL(54.67mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1868mL10.9340mL21.8680mL5mM0.4374mL2.1868mL4.3736mL10mM0.2187mL1.0934mL2.1868mL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.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:1.25mg/mL(2.73mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:1.25mg/mL(2.73mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性MB710?種氨苯并噻唑衍?物，致癌p53突變體Y220C的穩(wěn)定劑。MB710與Y220C緊密結(jié)合并穩(wěn)定p53-Y220C，Kd值為4?μM。MB710在p53-Y220C細(xì)胞系中顯?抗癌活性[1]。IC50&TargetKd:4?μM(p53-Y220C)體外研究MB710(0-200μM;72hours)showsrelativelylowtoxicityagainstallcelllinestestedatconcentrationsupto60?μM,whileshowinginitialselectiveviabilityreductionathigherconcentrations[1].MB710(72hours)treatscancercelllinesNUGC3,NUGC4,WI38andSW1088,withIC50sof90,120,>120,>120μM,respectively[1].MB710(0-120μM;72hours;HUH-7cells)showsstrongercytotoxiceffectsinpresenceofp53-Y220C[1].CellViabilityAssay[1]CellLine:NUGC3(mutantp53Y220C),HUH-7(mutantp53Y220C),NUGC4(p53WT),HUH-6cells(p53WT)Concentration:0-200μMIncubationTime:72hoursResult:Showedrelativelylowtoxicityagainstallcelllinestestedatconcentrationsupto60?μM.NUGC3wasthemostsensitivecellline.REFERENCES[1].BaudMGJ,etal.Aminobenzothiazolederivativesstabilizethethermolabilep53cancermutantY220Candshowanticanceractivityinp53-Y220Ccelllines.EurJMedChem.2018;152:101-114.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseo