120th General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Exhibition Hall 2+3
Time 10월 19일 (목요일) 11:00~12:30
Code MEDI.P-295
Subject Synthesis and biological evaluation of a novel [18F]DMFB as a potential PET agent for malignant melanoma
Authors Ayoung Pyo, Dong Yeon Kim*
Department of Nuclear Medicine, Chonnam National University Hwasun Hospital, Korea
Abstract The incidence of malignant melanoma has been increasing worldwide and there is still no effective treatment. Because of this cancer is a very aggressive, early detection in the earliest stages is very important to improve the survival of patients. In this study, we synthesized novel 18F labeled benzamide derivative. Furthermore, we evaluated biological characteristics in B16F10 (mouse melanoma) tumor bearing mice and lung / lymph node metastatic models. [18F]SFB was synthesized and used as prosthetic group. Amine derivative was dissolved in DMSO and added to dried [18F]SFB. The mixture was heated at 60°C for 30 min and purified by using HPLC. The mircoPET images were obtained at 10, 30, and 60 min after i.v. injection of [18F]DMFB (7.4MBq) in B16F10 bearing nude mice. The static images at 10, 30, and 60 min were acquired for 10 min. The overall non decay-corrected radiochemical yield was approximately 10–15%. In biodistribution studies, tumor uptake of [18F]DMFB (10, 30, 60 and 120 min % ID/g: 9.24, 10.8, 13.0, 10.6) retained from 10 to 120 min. Liver uptake of [18F]DMFB (10, 30, 60 and 120 min % ID/g: 11.19, 5.76, 2.47, 0.45) decreased from 10 to 120 min and showed fast clearance from liver. We performed microPET studies with [18F]DMFB. B16F10 tumor and metastasis lesions were visible after i.v. injection and [18F]DMFB retained for whole time (over 60 min). [18F]DMFB demonstrated malignant melanoma with high tumor uptake and specifically targeted metastatic lesions in B16F10 lung / lymph node metastasis model. [18F]DMFB might have a potential to be utilized as a novel melanoma imaging agent for PET.
E-mail payjal@naver.com