The pursuit of efficient and highly target-selective transporters is an active topic in cancer targeting therapy. A novel cancer-targeting probe based on integrin αvβ3 monoclonal antibody labeled carbon nanotubes was developed to investigate cancer cell targeting in vitro. The results revealed that the system had a high efficiency in cancer cell targeting in integrin αvβ3 positive U87MG cells but low targeting in HUVEC cells, indicating that the high efficiency was due to the specific targeting property of integrin αvβ3 monoclonal antibody. Thus, the integrin αvβ3 monoclonal antibody labeled single-walled carbon nanotube (SWNT) probe is a potential carrier-candidate for cancer-imaging and drug-delivering in cancer therapy.