121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-632
Subject Synthesis and in vitro stability evaluation of 89Zr-labeled Repebody as a PET imaging agent for EGFR expression in the tumor
Authors Seong Hui Yi, Eunbi Shin, Kyo-Chul Lee, JUNG-YOUNG KIM*
Korea Institute of Radiological & Medical Science, Korea
Abstract Repebody(rEgH9) was recently developed as a non-antibody scaffold which has high specificity and binding affinity (Kd = 301 pM) for an epidermal growth factor receptor (EGFR)[1]. In this study, we radiolabeled DFO-rEgH9 with 89Zr for PET imaging of EGFR expression in the tumor. The precursor, DFO-rEgH9 was prepared from DFO-benzyl isocyanate and repebody rEgH9 for 30 min at 50 oC. Radioligand 89Zr-DFO-rEgH9 was identified by the radio-TLC and evaluated stability in mouse and human serum in vitro. The radiochemical yield and purity of 89Zr-DFO-rEgH9 were 95% and 98%, respectively. 89Zr-DFO-rEgH9 was stable up to 24 h in both mouse and human serum in vitro. These results showed that 89Zr-DFO-rEgH9 has a potential as an imaging agent for EGFR overexpressed tumor. [1] Ange. Chemie-int. Ed. 54, 12020-12024(2015)
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