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EGFR-IN-176

Cat.No.:HY-178057

CASNo.:2754394-10-8

分⼦式:C₃₅H₄₅N₁₁O₃S

分⼦量:699.87

作⽤靶点:EGFR;Akt;Anaplasticlymphomakinase(ALK)

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

PI3K/Akt/mTOR

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性EGFR-IN-176是⼀种⼝服活性且ATP竞争性的EGFR突变体抑制剂(特别是C797S介导的EGFR三重突变体)。

EGFR-IN-176对三重突变细胞的⽣长具有⾼度选择性抑制作⽤，包括Ba/F3EGFR19del/T790M/C797S(IC50=

0.001nM)和Ba/F3EGFRL858R/T790M/C797S(IC50=0.04nM)。EGFR-IN-176能够有效抑制Ba/F3和PC-9

细胞(分别表达EGFR19del/T790M/C797S或EGFRL858R/T790M/C797S突变)中AKT信号通路的活化，且该

抑制作⽤呈现剂量依赖性。EGFR-IN-176选择性抑制携带EGFR三重突变的细胞系中的EGFR信号传导，对表

达野⽣型EGFR的A431细胞⽆抑制作⽤。EGFR-IN-176可有效抑制ALK的酶活性(IC500.5nM)。EGFR-IN-

176在⼩⿏实验中有效抑制肿瘤⽣长，并显⽰出良好的抗⾮⼩细胞肺癌作⽤[1]。

体外研究EGFR-IN-176(Compound31r,0.0045nM-10,000nM,48h)exhibitsextremelypotentandselectivegrowth

inhibitoryactivityagainstcellsharboringEGFRtriplemutationinvitro,includingBa/F3

EGFR19del/T790M/C797S(IC50=0.001nM)andBa/F3EGFRL858R/T790M/C797S(IC50=0.04nM),with

lowcytotoxicitytowardswild-typeEGFRcellsA431(I