TCP1 is a novel vasculature‐targeting peptide. It was discovered through the in vivo phage library selection. It was demonstrated that TCP1 peptide exhibited the homing ability to the tumor neovasculature and was capable of efficiently delivering imaging agents and chemotherapeutic drugs to this target site. The current study is to further investigate the targeting ability of TCP1 to deliver anti‐cancer drugs and imaging agents, and demonstrate the specificity of TCP1 on the putative target on tumor blood vessels and explore the potential mechanisms. In this study, we observed that TCP‐1 peptide delivered GFP only to tumor blood vessel other than normal organs after GFP or TCP‐1/GFP injection. Results in TNF‐α or TCP‐1/TNF‐α targeted delivery showed that TCP‐1/TNF displayed stronger effects than TNF‐α alone in the induction of apoptosis and reduction in number of microvessels in the tumors but without significant effect in systemic toxicity. To identify the cell surface targets for TCP1, we incubated the colon 26 cell with biotin‐TCP1 probe peptide and performed the pull‐down assay by neutravidin‐agarose beads. Preliminary western‐blot data showed that some membrane proteins on colon 26 cells could bind to TCP1 after incubation with biotin‐TCP1 probe. Taken together TCP1 peptide appears to be a promising agent in molecular imaging and drug delivery for gastrointestinal cancers.