Most nanoparticle-based bioresearch for clinical applications is unable to overcome the clinical barriers of efficacy (e.g., sensitivity and selectivity), safety for human use, and scalability for mass-production processes. Here, we proposed a promising concept of using a biocompatible nanocarrier that delivers natural fluorescent precursors into cancerous cells. The nanocarrier is a biopolymeric nanoparticle that can be easily loaded with fluorescent precursors to form a fluorescent moiety via a biosynthesis pathway. Once delivered into cancerous cells, the nanocarriers are selectively turned on and distinctively fluoresce upon excitation. We, therefore, demonstrated the efficacy of the selective turn-on fluorescence of the nanocarriers in in vitro coculture models and in vivo tumor-bearing models.