Radioiodinated Small-Molecule Tyrosine Kinase Inhibitor for HER2-Selective SPECT Imaging.

ABSTRACT: One of the most clinically relevant molecular aberrations in breast cancer is overexpression of human epidermal growth factor receptor type 2 (HER2). We aimed to develop a radiolabeled tyrosine kinase inhibitor for HER2-targeted breast cancer imaging. In this study, a radioiodinated analog (^125/131I-IBA-CP) of the HER2-selective inhibitor CP724,714 was prepared and evaluated in HER2-positive or -negative subcutaneous human breast cancer xenografts. Methods: The CP724,714 analog IBA-CP was synthesized and assayed for its inhibitory activities against HER2 and 6 other tyrosine kinases. ^125/131I-IBA-CP was prepared using a copper-mediated radioiodination method with enhanced labeling yield and molar activity. In vitro biologic activity, including specific and nons

SUBMITTER: Tang L 

PROVIDER: S-EPMC6126446 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature