Platinum agents can cause DNA damage and induce apoptosis to cancer cells, thus they became the backbone of cancer chemotherapy regimens, however, most cancers will develop drug resistance during the treatment.Meanwhile, most of the solid tumors meet energy needs largely by aerobic glycolysis, glycolysis in the presence of oxygen, called the Warburg effect, and Warburg effect is related to the resistance to apoptosis.Therefore, we use a biodegradable polymer carrier to conjugate with DACH-Pt and dichloroacetate (a PDK inhibitor which can reverse the Warburg effect to derepress the resistance to apoptosis, thus sensitize cancer cells to platinum), and assembled into nanoparticles for effective delivery and better synergism.In vitro and in vivo studies revealed that the combination of polymer-DCA and polymer-DACH-Pt are much better than the free drugs combined, in terms of both safety and antitumor efficay.