Gly-PEG3-BA-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

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Gly-PEG3-BA

Cat.No.:HY-180966

CASNo.: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:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性Gly-PEG3-BA是⼀种靶向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]。

IC50TargetEML4-ALK

体外研究Gly-PEG3-BA(0-20μM,72h)exhibitshighlytarget-selectiveactivityagainstEGFRinH1975cells(harboring

theEGFRL858R/T790Mdoublemutation)andinducesdose-dependenttargeteddegradationoftheEML4-

ALKfusionproteininH3122(EML-ALK)cells[1].

Gly-PEG3-BA(0-20μM,48or72h)tunedownEML4-ALKandEGFRmutantefficientlyandconferpotent

antiproliferationactivityinH3122(EML-ALK)andH1975(EGER-L858R/T790M)cellswithIC50valuesof

0.84and20.74μM[1].