The integration of cancer-specific molecular target and magnetic manipulation into a single platform endows the nano-composites with multiple properties, such as dual-targeting capabilities, controllable release, and dual-therapeutical effects (drug and hyperthermia therapy), which have showed tremendous promise for cancer nanomedicine while concurrently reducing toxic side effects [1].Herein, based on our previous research [2], we report a novel graphene oxide/Fe304 nanocomposite functionalized with a cRGD peptide to cater to anticancer drugs.The drug-carrier system was synthesized by combination of a simple and effective chemical deposition method with O2 inducing and air slow oxidation processes, followed by binding camptothecin (CPT) on the ultra-fine graphene oxide (GO) flakes of hybrid by π-π stacking and grafting cRGD peptide on the carboxyl terminals of GO by covalently conjugating.The characterizations of physicochemical properties of the as-prepared copolymers were performed.The cytotoxicity in vitro of delivery system was measured using Annexin V/PI co-labeling on LSCM and FCM.Under magnetic induction and NIR triggering, targeting and tumor inhibitory evaluation in vivo were conducted using optical living images of the tumor-bearing mice.The results show that the size range of the copolymers was from 150 to 170 nm under simulate physiological medium.The tumor inhibitory rate of 76% reflected that the resulting copolymers could be promising to treat cancer by specific binding and targeting release drug to tumor.