Lys-PEG3-BA-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELys-PEG3-BACat.No.:HY-180964CASNo.:3057939-67-7分⼦式:C₃₈H₅₇ClN₉O₇P分⼦量:818.34作⽤靶点:PROTACs;Anaplasticlymphomakinase(ALK);EGFR作⽤通路:PROTAC;ProteinTyrosineKinase/RTK;JAK/STATSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Lys-PEG3-BA⼀种靶向EML4-ALK/EGFR的PROTAC降解剂，其对H3122细胞(表达EML4-ALK融合蛋⽩)和H1975细胞(携带EGFRL858R/T790M双突变)的DC50分别为1.32μM与19.66μM。体外实验中，Lys-PEG3-BA可通过重新调控泛素-蛋⽩酶体系统，抑制⾮⼩细胞肺癌细胞的增殖。Lys-PEG3-BA可⽤于⾮⼩细胞肺癌的相关研究[1][2]。体外研究Lys-PEG3-BA(0-20μM)leadsEML4-ALKdecertationinH3122(EML4-ALK)cellsandattainsa91%reductionat10μM[2].Lys-PEG3-BA(0-20μM)specificallytriggersthedegradationofEGFRinH1975(EGFR-L858R/T790M)cells,andattainsa52%reductionat20μM[2].Lys-PEG3-BA(48-72h)efficientlyinhibitsH3122(EML4-ALK)andH1975cellproliferationwithanIC50sof5.30μMat48hand18.56μMat72h,respectively[2].WesternBlotAnalysis[2]CellLine:H1975(EGFR-L858R/T790M)andH3122(EML4-ALK)Concentration:0,0.01,0.1,1,10and20μMIncubationTime:48(forH3122)or72h(forH1975)Result:SpecificallytriggeredthedegradationofEGFRinH1975(EGFR-L858R/T790M)cells,withoutaffectingthewild-typeEGFRproteinlevel.ResultedinapparentdownregulationoftheEML4ALKproteininH3122(EML4-ALK)cellsatvaryingdoses.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].ChenX,etal.Mightymini-PROTACs:anemergingclassofdegraders.EurJMedChem.2026Jan5;301:118202.[2].ZhangJ,etal.DistinctAminoAcid-BasedPROTACsTargetOncogenicKinasesforDegradationinNon-SmallCellLungCancer(NSCLC).JMedChem.2024Aug22;67(16):13666-13680.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-37