Cancer is characterized by deregulation of cell proliferation and altered cell death apoptosis, which constitutes, in almost all instances, the minimal common platform upon which all neoplastic evolution occurs. The most implicit and clinically attractive anticancer strategies, therefore, consist of eliminating tumor cells by preventing their expansion and ultimately inducing cell death apoptosis. In this context, the non-invasive molecular assessment of tumor cell proliferation and apoptosis status using PET imaging constitutes a major strategy in preclinical studies to assess the efficacy of new anticancer therapeutics using small animal PET imaging, and in clinical settings for the monitoring of treatment responses in patients. For this purpose, a variety of PET tracers targeting specific molecular entities allowing the non-invasive measurement of biological processes, including cell proliferation and apoptosis, are under development for use in preclinical studies and clinical trials to non-invasively image in vivo the lifeline of tumors.