To determine whether de-protection of mono-functionalized platinum(IV) prodrugs for targeted therapy with significant GLUT1 and OCT2 substrates can also perform cancer targeting in vivo, the biodistribution of Rha-Pt (2d), Gal-Pt (5d), Glc-Pt (6d), and satraplatin (5a) as positive controls in MCF-7 bearing animals were assessed by ICP-MS at 9 and 24 h post-administration (i.v.). Here, SLC22A2 is linked to cancer.