The Gef/H-dot and Gen/H-dot complexes not only provided real-time dual-channel intraoperative NIR fluorescence image guidance and pathological assistance but also delivered both EGFR-TKI (Gef)/AI (Gen) simultaneously to the tumor sites for synergistic treatment with low nonspecific uptake by normal tissues to reduce adverse effects in orthotopic lung tumor and subcutaneous tumor mice models. The gene discussed is EGFR; the disease is neoplasm.