DOTAGA-anhydride is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide drug conjugates (RDCs). DOTAGA-anhydride can be used to label monoclonal antibodies (mAbs) such as trastuzumab (targeting HER2/neu receptor with an affinity of 5.5 nM) under mild conditions (PBS pH 7.4, 25 °C, 30 minutes) after chelation with indium-111. [111In-DOTAGA]-trastuzumab showed a tumor uptake of 65% ID/g in mice bearing breast cancer BT-474 xenografts 72 hours after injection, which is valuable for SPECT/CT imaging and biodistribution studies.
