Successful development of safe and effective nanoprobes for tumor targeting and selective therapy is a challenging task. Although gold nanorods(GNRs) have the potential to perform such a role, the toxicity of surfactant cetyltrimethylammonium bromides (CTAB) on their surfaces limits their applications. Here, polyamidoamine dendrimer was applied to replace CTAB molecules on the surface of gold nanorods. When the resultant dendrimer-modified gold nanorods conjugated with arginine-glycine-aspartic acid (RGD) peptides, they showed highly selective targeting and destructive effects on the cancer cells and solid tumors under near-infrared laser irradiation. Also, we successfully observed the disappearance of tumors implanted in four sample mice from test group of ten. High-performance RGD-conjugated dendrimer-modified GNR nanoprobes exhibit great potential in applications such as tumor targeting, imaging, and selective photothermal therapy.