Using nanotechnology, therapeutics can be combined with diagnostics for cancer treatment. To do this, a targeting ligand, an imaging contrast agent and an anti-tumour therapeutic agent were the minimum requirements for active targeting nanoassemblies. Here we have developed a novel active targeting theranostic agent, made up of just two components, aptamer AS1411 and graphene quantum dots (GQDs). Each component in our agent plays multiple roles. Confocal microscopy using a 488 nm laser shows that this agent has an excellent capability to label tumour cells selectively. On the therapeutic side, this agent induced a synergistic growth inhibition effect towards cancer cells when irradiated with a near infrared laser of 808 nm. The ultra-small size, good biocompatibility, intrinsic stable fluorescence, and near-infrared response character make GQDs a remarkable constituent to build theranostic agents.