Two near infrared fluorescence probes (i.e., folate-PEG-ICG-Der-01 and LDL-ICG-Der-02) are synthesized. Here, over-expressed folate receptors and low density lipoprotein (LDL) receptors in some specific tumors are chosen as target. The residues of folic acid and LDL, as the targeted ligand, are covalently conjugated to organic near-infrared fluorescence dye ICG-Der-0 and ICG-Der-02 respectively, where near-infrared dyes are the output of fluorescence signal. The optical properties of the two probes are characterized by ultraviolet spectrophotometer and near-infrared fluorescence spectroscopy system. The imaging process of folate-PEG-ICG-Der-01 and LDL-ICG-Der-02 probes in tumors which over expressed folate receptors and LDL receptors is further detected by near-infrared fluorescence imaging system. The results show that as-prepared folate-PEG-ICG-Der-01 and LDL-ICG-Der-02 probes present higher fluorescence intensity and better photo stability than those corresponding near-infrared fluorescence dyes. And the results of in vivo near-infrared fluorescence imaging confirme that these two probes are highly bioactive, can efficiently target tumor sites, and finally be eliminated. Compared with LDL-ICG-Der-02, the targeting capability of folate-PEG-ICG-Der-01 probe is more effective, and has great potential in non-invasive real time early tumor diagnosis.