Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESIAIS117Cat.No.:HY-146022CASNo.:2353494-84-3分?式:C??H??ClN??O?PS分?量:1111.77作?靶點(diǎn):PROTACs;Anaplasticlymphomakinase(ALK)作?通路:PROTAC;ProteinTyrosineKinase/RTK儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性SIAIS117?種有效的Brigatinib-PROTAC降解劑。SIAIS117?種于Brigatinib和VHL-1結(jié)合的ALKPROTAC。SIAIS117能有效降解ALKG1202R點(diǎn)突變SIAIS117可阻斷SR和H2228癌細(xì)胞株的?長(zhǎng)。SIAIS117具有潛在的?細(xì)胞肺癌的抗增殖能?[1]。體外研究SIAIS117(0-10μM,72h)inhibitsSR,H2228,NCI-H69andNCI-H1688cellgrowth,withIC50valuesof1.7,46,799,and259nM,respectively[1].SIAIS117(0-500nM,24h)inhibitsthephosphorylationofALKandSTAT3[1].SIAIS117inhibitsthegrowthofG1202R-mutantALKcelllineanddegradesG1202R-ALKprotein[1].SIAIS117(100nM,24h)causessustaineddegradationofALKproteininSRcells[1].CellProliferationAssayCellLine:NSCLCcelllineH2228,Smallcelllungcancercelllines(NCI-H69,NCI-H1688)[1]Concentration:0-10μMIncubationTime:72hResult:InhibitedcellgrowthwithanabouttwofoldslowerIC50value(46nM)comparingtoSIAIS117NC(114nM).ShowedagoodgrowthinhibitioneffectonNCI-H69andNCI-H1688cellline,withIC50valuesof799and259nM,respectively.WesternBlotAnalysisCellLine:SR,H2228[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:0,1,10,50,100,500nMIncubationTime:24hResult:InhibitedallofthephosphorylationofALKat10nMandinhibitedpSTAT3inSRcell,degradedALKproteinsattheconcentrationstartingfrom50nMinH2228cell,andsignificantlydownregulatedUCK2andGAK.CausedsustaineddegradationofALKproteininSRcells.REFERENCES[1].SunN,RenC,KongY,etal.DevelopmentofaBrigatinibdegrader(SIAIS117)asapotentialtreatmentforALKpositivecancerresistance.EurJMedChem.2020;193:112190.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400