Nanomedicine based on nanotechnology facilitates the development of both therapeutic and diagnostic agents. Especially, fluorescence-based imaging guidance for tumor resection has recently emerged as a fascinating tool using exogenous fluorescent contrast agents with objective and precise information of tumor tissues. However, the most contrast agents cannot inherently offer real-time visual information concerning selectivity and localization of the tumor because of a lack of cancer targeting property and insufficient sensitivity for acquiring fluorescent signal in real-time. For selective and active tumor targeting, these contrast agents were chemically conjugated with targeting moieties such as antibodies and peptides, which often fail in Food and Drug Administration (FDA) approval due to safety issues. Motivated by this point, we have developed nanocarriers to escape the most issues in regard to the clinical safety. In this study, we have demonstrated selective targeting of cancer cells (including in vivo xenograft models) and targeted ;;turn-on” fluorescence upon delivery of nanocarriers to achieve excellent sensitivity with high signal-to-noise ratio. Owing to the non-toxic and distinct fluorescence, we expect that our nanocarriers developed in this study will be ;;extremely fast’ to be exploited for clinical use.