Photoactivated anticancer chemotherapy distinguishes itself by its high selectivity by virtue of the spatiotemporal control of irradiation. However, short photoactivation wavelengths limit its application. Herein, an amphiphilic Ru(II) complex, cis-[Ru(bpy)(2)(C18H37CN)(2)](2+) (bpy = 2,2'-bipyridine), was embedded along with a poly(ethylene glycol, PEG)-modified lipid onto the surfaces of oleate-capped lanthanide-doped upconversion nanoparticles (UCNPs). The resultant core-shell hybrid system is water-dispersible, stable in the dark, and releases a DNA covalent-binding agent of [Ru(bpy)(2)(H2O)(2)](2+) upon 980 nm laser irradiation, providing guidelines for developing near-infrared (NIR) light triggered chemotherapeutics.