A novel bifunctional maleimido CHX-A″ chelator for conjugation to thiol-containing biomolecules

A novel bifunctional maleimido CHX-A″ DTPA chelator 5 was developed and conjugated to the monoclonal antibody trastuzumab (Herceptin) and subsequently radiolabeled with 111In. The resulting 111In labeled immunoconjugate 2 was demonstrated to bind to SKOV-3 ovarian cancer cells comparably to an isothiocyanato CHX-A″ DTPA modified native trastuzumab, 1. Through efficient thiol-maleimide chemistry, antibodies, peptides or other targeting vectors can now be modified with an established radioactive metal chelating agent CHX-A″ DTPA for imaging and/or therapies of cancer.