Given the critical importance of FGFR1 in the pathogenesis and development of NSCLC, this study identified two novel, non-ATP-competitive inhibitors of FGFR1 kinase, i.e., Ad23 and Af23, both of which exhibited good anti-tumor activity in vitro and in vivo. Here, FGFR1 is linked to non-small cell lung carcinoma.