Abstract: The aim of this work is to study on the tumor targeting of the FITC labeled folic derivate. N-(2-aminoethyl)-2-(4-aminophenyl)acetamide was synthesized by 2-(4-aminophenyl)acetic acid and coupled with α- and γ-carboxyl of folate, DMAP/EDCI was used as a coupling reagent to synthesize folate-derived FA-EA, FA-EA was labeled with FITC to get the compound FA-EA-(FITC)2. All the intermediates were identified with HPLC、1H NMR and MS. In vivo fluorescent imaging was carried in KB tumor-bearing nude mouse injected with FA-EA-(FITC)2 through tail vein, the distributions of FA-EA-(FITC)2 in major organs and tumor were observed after sacrificing KB tumor-bearing nude mouse which had been photographed in vivo. The results indicated that FA-EA-(FITC)2 accumulated within tumor obviously while it was nearly invisible in major organs, it manifest that FA-EA-(FITC)2 have preferable ability to target tumor. This work can supply evidence for further developing tumor-imaged agent on folate.

Key words: Folic Derivate, FITC, in vivo fluorescent imaging