It is well documented that organic cation transporter 2 (OCT2) plays important roles in the cellular accumulation and consequent cytotoxicity of platinum complexes containing the (1R,2R)-cyclohexane-1,2-diamine (DACH) ligand.[21] OCT2-mediated cellular uptake has been suggested as a leading factor responsible for the sensitivity of colorectal cancer to oxaliplatin.[21] Because the Glc-Pts reported here bear the chelating DACH ligand, we investigated the potential of 1 to undergo translocation via OCT2, a transporter overexpressed in certain types of cancer cells and tumor samples from patients.[21–22] Expression of OCT2 in a panel of cancer cell lines was confirmed by Western blotting analysis (Figure S10b). A2780 cells were incubated with 10 μM 1 for 8 h in the presence or absence of EDG and/or the OCT2 inhibitor cimetidine (Ctd)