Ruthenium complexes are among the most extensively studied and developed luminescent transition-metal complexes for anticancer applications. Dinuclear Ru(II) complexes have caught significant interest for larger size, higher charge, and variable complex shapes. In this concept, we have explored past and recent works on the possible biological applications of versatile tetrapyrido[3,2-a : 2,3-c : 3,2-h : 2''',3'''-j]phenazine (tppz)-based dinuclear Ru(II) complexes with a focus on their use as quadruplex DNA probes, organelle imaging, and phototherapeutic agents. This concept also points out that a particular type of dinuclear Ru(II) complexes can act as multitargeting and multifunctional anticancer agents -making this an exciting research area in which an array of further applications will likely emerge.