General Description
A cell-permeable Pt(IV) compound that, upon reduction inside cells, yields two molecules of the PDK (pyruvate dehydrogenase kinase) inhibitor DCA/dichloroacetate and one molecule of the apoptosis inducer Cisplatin (Cat. No. 232120). While the dual prodrug nature of Mitaplatin is shown to result in increased cell killing than Cisplatin in the human ovarian carcinoma A2780/CP70 cultures (IC50 = 3.34 and 6.0, respectively), the anticancer potency of Mitaplatin is often weaker than Cisplatin in other cancer cells tested, presumably due to insufficient prodrug reduction in these cells.
Note: Carboplatin, Cisplatin, and other platinum drugs are reported to be rendered inactive due to ligand displacement by the nucleophilic sulfur of DMSO. Solubilization with DMSO prior to culture treatment is not recommended.
