A mathematical model is developed to study the localization characteristics of anti-cancer agents in solid tumors. The model is general enough that it may be applied to many chemotherapeutic approaches to cancer treatment, but is firmly based on the biology of a particular new and promising two-step drug targeting strategy. Singular perturbation techniques are used to approximate the solution away from the capillary wall and in the boundary layer at the capillary-tissue interface. The solution to the full system of partial differential equations can also be approximated by an ordinary differential equation formulation whose solution provides a good analytic expression for the total concentration of conjugate in the tumor. From this result key parameters are isolated; the effects of the tumor vasculature, binding kinetics, and administration schedule are investigated; and the critical parameters that influence the retention of the agent in the tumor are determined. The model predicts that conjugate localizes best in well vascularized tissue, but is retained longer in poorly vascularized sections of the tumor. Also, reducing the dissociation rate by half almost doubles the half-life in the tumor. Comparisons of the model predictions with experimental observations are made and an excellent correlation exists.