Cancer poses a number of challenges in diagnostic and clinical applications of novel molecular therapies. However, new knowledge of cancer biology and tumor micro-environmental opens opportunities to meet these challenges. For instance, the discontinuous vascular walls found in many types of tumors provide an opportunity for enhanced delivery of nanoparticle-based therapies. The continued development of cancer nanotechnology holds the promise for personalized oncology in which genetic and protein biomarkers can be used to diagnose and treat cancer. The accurate assessment of tumor stage is essential as local or systemic therapies are administered in a stage-specific fashion. A major goal in current nanoparticle research and biolabeling in general, is the development of preparations that are long-circulating and can label-specific locations or biomarkers with high selectivity. Specifically, nanoparticles need to be stable in biological media, for example, in tissue samples or in the bloodstream of living organisms, and show little or no biologically induced agglomeration or rapid clearance by components of the immune system. Ideally, targeted nanoparticles should recognize a biological receptor with high selectivity while demonstrating little nonspecific binding to other cellular components.