To assess the synergy of combining chemotherapeutics with bioorthogonal activation of tumor-targeting PDCs, we conducted a study to investigate the antitumor effects of the activable PDC RGD-Dox in αvβ3-positive B16F10 melanoma cells, U87 brain glioma cells, and SKOV3 cells, as well as αvβ3-negative hepatic stellate (LX2) cells as a control. This evidence concerns the gene PDC and neoplasm.