Synthesis and evaluation of a novel 68Ga-labeled DOTA-benzamide derivative for malignant melanoma imaging.
Malignant melanoma displays a highly aggressive metastasis. Thus, early diagnosis of malignant melanoma is important for patient survival. We designed and synthesized a novel (68)Ga-labeled benzamide derivative that specifically binds to melanoma as demonstrated by its ability to bind to melanin. (68)Ga-SCN-DOTA-PCA was synthesized with a radiochemical yield of ~80% and a radiochemical purity of >97% by analytical HPLC. The in vitro binding of (68)Ga-SCN-DOTA-PCA to melanin and its cellular uptake demonstrated the selective uptake in melanin. In addition, the biodistribution and micro-PET imaging of (68)Ga-SCN-DOTA-PCA in B16F10 tumor models showed the specific accumulation in melanoma. These results suggest that (68)Ga-SCN-DOTA-PCA would be a promising agent for melanoma diagnosis.
Radiation Instrumentation Research Division, Korea Atomic Energy Research Institute, Jeongeup, Republic of Korea.
Hee-Jung
HJ
Kim
Dong-Yeon
DY
Kim
Jeong-Hoon
JH
Park
Seung-Dae
SD
Yang
Min-Goo
MG
Hur
Jung-Joon
JJ
Min
Kook-Hyun
KH
Yu
D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D005710:Gallium Radioisotopes / Q000737:chemistry; D006207:Half-Life; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D008546:Melanoma, Experimental / Q000000981:diagnostic imaging*; D051379:Mice; D008810:Mice, Inbred C57BL; D049268:Positron-Emission Tomography; D011342:Procainamide / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014184:Transplantation, Homologous
D001549:Benzamides; D005710:Gallium Radioisotopes; D006573:Heterocyclic Compounds, 1-Ring; D019275:Radiopharmaceuticals; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid; C037689:benzamide; D011342:Procainamide