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Inhibitors•ScreeningLibraries•Proteins

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EGFR-IN-175

Cat.No.:HY-178009

分⼦式:C₃₃H₃₈N₁₀O₄S₂

分⼦量:702.85

作⽤靶点:EGFR;Apoptosis;Akt;PERK

作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK;Apoptosis;

PI3K/Akt/mTOR;CellCycle/DNADamage

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性EGFR-IN-175是⼀种⼝服有效且有选择性的的EGFRL858R/T790M/C797S抑制剂，其IC50值为18.94nM。

EGFR-IN-175能够诱导细胞凋亡(apoptosis)并导致G1期阻滞。EGFR-IN-175可下调p-EGFR、p-AKT和p-

ERK的表达。EGFR-IN-175可⽤于癌症研究，如肺癌研究[1]。

IC50TargetEGFRWTEGFRLR/TMEGFRLR/TM/CS

125.9nM(IC50)76.88nM(IC50)18.94nM(IC50)

体外研究EGFR-IN-175(CompoundM49)inhibitsproliferationofBaF3-EGFRL858R/T790M/C797S,A431andH1975

cellswithIC50valuesof0.77,5.11and5.94μM[1].

EGFR-IN-175(0.1-2.5μM)dose-dependentlydownregulatesphosphorylationlevelsofp-EGFR,p-AKT,and

p-ERKinBaF3-TMcells[1].

EGFR-IN-175(0.1-2.5μM,48h)inducesapoptosisandG1phasearrestinBaF3-TMcells[1].

ApoptosisAnalysis[1]

CellLine:BaF3-TMcells