Lys-PEG3-BA-生命科学试剂-MCE.pdfVIP

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Lys-PEG3-BA

Cat.No.:HY-180964

CASNo.: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:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性Lys-PEG3-BA是⼀种靶向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)andH1975cellproliferationwithanIC50sof

5.30μMat48hand18.56μMat72h,respectively[2].

WesternBlotAnalysis[2]

CellLine:H1975(EGFR-L858R/T790M)andH3122(EML4-ALK)

Concentration: