Gold complexes have been acknowledged as potential anticancer brokers towards numerous sorts of illnesses attributable to their inherent suppressions of antioxidant thioredoxin reductase (TrxR) exercise. Herein, a strong aggregation-induced emission luminogen (AIEgen), TBP-Au, was designed and synthesized by integrating an anticancer Au(I) moiety with an AIE-active photosensitizer (TBP), by which each the manufacturing and consumption routes of reactive oxygen species (ROS) have been elaborately thought of concurrently to spice up the anticancer efficacy. It has been demonstrated that TBP-Au may understand superior two-photon fluorescence imaging in tumor tissues with excessive decision and deep penetration in addition to long-term imaging in reside animals attributable to its AIE property. As well as, the introduction of a particular Au(I) moiety may tune the organelle specificity and effectively facilitate the ROS-determined photodynamic remedy (PDT). Extra impressively, TBP-Au may effectively eradicate most cancers cells underneath mild irradiation by way of the preconceived synergetic approaches from the PDT and the efficient suppression of TrxR, demonstrating that TBP-Au holds nice potential for exact most cancers theranostics.