Targeted delivery of therapeutic agents to cancer sites is a novel and promising approach to improve cancer treatment, as it will deliver high doses of drug molecules to tumor sites for maximum treatment efficacy while minimizing side effects to normal organs. In this proposal, we will integrate EphB4-targeted-delivery method and CML with molecular imaging, to develop a series of novel CMLs that can be accurately and precisely traced during each stage of their application through molecular imaging. The success of this imaging-guided approach will help us quickly select the most potent CML drug carrier with high cancer treatment efficacy and low toxic side effects based on their biodistribution, biokinetics, and toxicology.