JCN037-JGK037-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEJCN037Cat.No.:HY-136430CASNo.:2305154-31-6Synonyms:JGK037分?式:C??H??BrFN?O?分?量:376.18作?靶點(diǎn):EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK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:250mg/mL(664.58mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6583mL13.2915mL26.5830mL5mM0.5317mL2.6583mL5.3166mL10mM0.2658mL1.3292mL2.6583mL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，并請注意儲備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6.25mg/mL(16.61mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性JCN037(JGK037)有效的、共價(jià)的、能透過?腦屏障的EGFR抑制劑，對EGFR、p-wtEGFR和pEGFRvⅢ的IC50值分別為2.49nM、3.95nM和4.48nM。IC50&Target2.49nM(EGFR),3.95nM(p-wtEGFR),4.48nM(pEGFRvⅢ)[1].體外研究JCN037exhibitsGI50valuesof329nMand1116nMinHK301cellsandGBM39cells,respectively[1].WesternBlotAnalysis[1].CellLine:GBM39andGS025cells.Concentration:0-3333nMIncubationTime:Result:DownregulatedpEGFRvⅢ,pAkt,p-ERK,andp-S6proteinlevels,significantly.體內(nèi)研究JCN037(compound5)exhibitsloworalbioavailabilityduetoarapidhydroxylationofthefused1,4-dioxanering,suggestingfirstpassmetabolism[1].JCN037(compound5,300mg/kg,BID)treatmentprovidesasignificantsurvivalbenefit,wherebymediansurvivalincreasedby47%from37.5daysto55dayswith5treatment[1].REFERENCES[1].JonathanE.Tsang,etal.DevelopmentofaPotentBrain-PenetrantEGFRTyrosineKinaseInhibitoragainstMalignantBrainTumors.ACSMed.Chem.Lett.2020.May1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-82