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Phototherapy, involving PDT and PTT, has been acknowledged as a local and noninvasive medical technology to treat cancer.The integration of photodynamic therapy (PDT) with photothermal therapy (PTT) triggered by a single light irradiation has attracted great interest in cancer treatment recently.For PDT or PTT treatment, photosensitizer (PS) is administrated to absorb light energy to convert into sufficient reactive oxygen species (ROS) or heat, leading to tumor cell death.However, such multifunctional photosensitizers (PSs) still confront with poor tumor-specific accumulation.In this report, a tumor-targeted near-infrared (NIR) photosensitizer (IR-808) is designed to covalently conjugate with polyethylene glycol (PEG) and branched polyethylenimine (BPEI) dual-functionalized nanographene oxide (NGO), because the optimized laser wavelength of NGO for PTT is coincidentally consistent with that of IR-808 for PDT (808 nm).More importantly, high-performance PDT/PTT combination therapy is achieved by increasing the tumor accumulation of NGO via IR-808-assisted transport, and by improving the water solubility of IR-808 via the nanocarrier of PEG-and BPEI-modified NGO.In the two lines of cancer cells and their xenograft models,IR-808-conjugated NGO (NGO-808) is demonstrated to exhibit the improved water-solubility,cell penetration, tumor-targeted accumulation and efficiently phototherapy.Typically, just after a single injection of the NGO-808 and 5 min laser irradiation once, the tumors are ablated completely and no tumor recurrence is observed.