Gly-PEG3-BA-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGly-PEG3-BACat.No.:HY-180966CASNo.:3057939-66-6分⼦式:C₃₄H₄₈ClN₈O₇P分⼦量:747.22作⽤靶点:PROTACs;EGFR作⽤通路:PROTAC;JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Gly-PEG3-BA⼀种靶向EML4-ALK的PROTAC降解剂。Gly-PEG3-BA在H3122细胞(EML4-ALK阳性细胞)中可有效降解EML4-ALK蛋⽩，其DC50为0.50μM；Gly-PEG3-BA在H1975细胞(EGFRL858R/T790M双突变细胞)中能显著降低EGFR突变体(L858R/T790M)的蛋⽩⽔平，对应的DC50值为20.15μM。此外，Gly-PEG3-BA对H3122细胞与H1975细胞均具有强效抗增殖活性，其IC50分别为0.84μM与20.74μM。Gly-PEG3-BA可⽤于⾮⼩细胞肺癌的相关研究[1]。IC50&TargetEML4-ALK体外研究Gly-PEG3-BA(0-20μM,72h)exhibitshighlytarget-selectiveactivityagainstEGFRinH1975cells(harboringtheEGFRL858R/T790Mdoublemutation)andinducesdose-dependenttargeteddegradationoftheEML4-ALKfusionproteininH3122(EML-ALK)cells[1].Gly-PEG3-BA(0-20μM,48or72h)tunedownEML4-ALKandEGFRmutantefficientlyandconferpotentantiproliferationactivityinH3122(EML-ALK)andH1975(EGER-L858R/T790M)cellswithIC50valuesof0.84and20.74μM[1].Gly-PEG3-BA(0-72h,48or72h)effectivelydecreasesEML4-ALKorEGFRmutantproteinlevelsinadose-dependentmannerinH3122andH1975cells[1].Gly-PEG3-BAinducesthedegradationofEML4-ALKandmutantEGFR,andthisdegradationprocessismediatedbyZYG11BandZER1inH3122andH1975cells(knockeddownZYG11BandZER1expression)[1].WesternBlotAnalysis[1]CellLine:H1975(harboringtheEGFRL858R/T790Mdoublemutation),A549,H1299,PC9,1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEH3122(EML4-ALK)cellsConcentration:0,0.01,0.1,1,10and20μMIncubationTime:72hResult:TriggeredthedegradationofEGFRwithoutaffectingthewild-typeEGFRproteinlevelinA549andH1299cellsortheEGFRdel19mutantproteinlevelsinPC9cells.ResultedanapparentdownregulationoftheEML4ALKproteininH3122cellsatvaryingdoses.WesternBlotAnalysis[1]CellLine:H3122(EML-ALK),H1975(EGER-L858R/T790M)cellsConcentration:0,0.01,0.1,0.25,0.5,0.75,1,2.5,5,7.5,10μM,or0,10,12.5,15,17.5and20μMIncubationTime:48(forH3122cell)or72h(forH1975cell)Result:EffectivelyreducedEML4-ALKinH3122(EML-ALK)cells,withaDC50valueof0.50μM,andattaineda98%reductionat-10μM.EffectivelyreducedEGFRlevelswithDC50of20.15μMandachieveda43%ataround20μMinH1975(EGER-L858R/T790M)cells.WesternBlotAnalysis[1]CellLine:H3122(EML-ALK),H1975(EGER-L858R/T790M)cellsConcentration:10(forH3122)or20(forH1975)μMIncubationTime:0,0.25,0.75,1.5,3,6,12and24h(forH3122)or0,12,24,36,48and72h(forH1975)Result:ledtoadecreaseinEML4-ALKorEGFRmutantproteinlevelsat15minand24h.REFERENCES[1].ZhangJ,etal.DistinctAminoAcid-BasedPROTACsTargetOncogenicKinasesforDegradationinNon-SmallCellLungCancer(NSCLC).JMedChem.2024Aug22;67(16):13666-13680.[2].ChenX,etal.Mightymini-PROTACs:anemergingclassofdegraders.EurJMedChem.2026Jan5;301:118202.McePdfHeightCaution:Producthasnotbeenfullyvali