biostudies-literatureUnknown11(2)Zheng QConstitutive activation of signal transducer and activator of transcription 3 (STAT3) is a common feature in human non-small cell lung cancer (NSCLC). STAT3 plays an important role in cancer progression as a driver oncogene and acquired resistance of targeted therapies as an alternatively activated pathway. W2014-S with pharmacophore structure of imidazopyridine, which was firstly reported to be utilized in STAT3 inhibitor discovery, was screened out as a potent STAT3 inhibitor from a library of small molecules. The aim of this study is to investigate the antitumor activities and mechanisms of W2014-S in NSCLC and effect on epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) resistance <i>in vitro</i> and <i>in vivo</i>. <b>Methods:</b> SPR analysis, Co-immunoprecipitatTheranostics824-840https://www.ebi.ac.uk/biostudies/studies/S-EPMC7738869biostudies-literatureA novel STAT3 inhibitor W2014-S regresses human non-small cell lung cancer xenografts and sensitizes EGFR-TKI acquired resistance.PMC7738869Ouyang SHuang JShi SHu WMo JLiu PZheng QDong HZhang YZhu KZhang XQu XWang YfalseA novel STAT3 inhibitor W2014-S regresses human non-small cell lung cancer xenografts and sensitizes EGFR-TKI acquired resistance.Constitutive activation of signal transducer and activator of transcription 3 (STAT3) is a common feature in human non-small cell lung cancer (NSCLC). STAT3 plays an important role in cancer progression as a driver oncogene and acquired resistance of targeted therapies as an alternatively activated pathway. W2014-S with pharmacophore structure of imidazopyridine, which was firstly reported to be utilized in STAT3 inhibitor discovery, was screened out as a potent STAT3 inhibitor from a library of small molecules. The aim of this study is to investigate the antitumor activities and mechanisms of W2014-S in NSCLC and effect on epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) resistance <i>in vitro</i> and <i>in vivo</i>. <b>Methods:</b> SPR analysis, Co-immunoprecipitat2021-01-01T00:00:00Z20212026-05-02T23:30:16.481Z2021-02-20T19:43:07ZS-EPMC77388693339150710.7150/thno.49600