Here we screened the ICCB Known Bioactive library of 12,640 compounds for the enhancement of the cytotoxicity of AC220 and identified TAK-165, a potent and irreversible HER2 (encoded by ERBB2) inhibitor, as a compound that can effectively induce cell death in different cancer cell lines when used in combined therapy with AC220. Here, ERBB2 is linked to cancer.