Chemotherapy　(CMT)　and　photodynamic　therapy　(PDT)　are　dose-dependent　treatments,　and　overdose　of　these　treatment　will　destroy　normal　cells　and　cause　serious　side　effects.　Hence,　it　is　urgent　to　monitor　the　therapeutic　effects　and　exploit　a　more　resultful　and　noninvasive　treatment　mode　to　alleviate　side　effects　to　normal　tissues.　Inspired　by　the　design　of　molecular　targeted　drug　and　the　GSH　responsive　function　of　copper(II)　porphyrin,　we　have　designed　and　synthesized　a　novel　compound　(E-CuTPP),　in　which　a　small　molecular　targeted　drug　(erlotinib)　and　a　copper　porphyrin(II)　are　conjugated.　We　demonstrated　that　E-CuTPP　can　exhibit　higher　toxicity　towards　epidermal　growth　factor　receptor　(EGFR)　overexpressed　cancer　cells.　Furthermore,　E-CuTPP　can　monitor　intracellular　glutathione　fluctuations,　which　is　closely　related　to　apoptosis.　Upon　treatment,　the　fluorescence　of　E-CuTPP　will　dramatically　increase,　which　can　timely　estimate　the　therapeutic　efficiency.