Affiliation:
1. Department of Nuclear Medicine Peking University First Hospital Beijing China
2. Department of Nuclear Medicine Peking University International Hospital Beijing China
Abstract
We report the synthesis and biological evaluation of 131I‐labeled antihuman tumor‐derived immunoglobulin G (IgG) light chain monoclonal antibody (4E9) ([131I]I‐4E9) as a promising probe for tumor imaging. [131I]I‐4E9 was synthesized in radiochemical yield of 89.9 ± 4.7% with radiochemical purity of more than 99%. [131I]I‐4E9 showed high stability in normal saline and human serum. In cell uptake studies, [131I]I‐4E9 exhibited favorable binding affinity and high specificity in HeLa MR cells. In biodistribution studies, [131I]I‐4E9 showed high tumor uptake, high tumor/non‐tumor ratios, and specific binding in BALB/c nu/nu mice bearing human HeLa MR xenografts. Single‐photon emission computerized tomography (SPECT) imaging of [131I]I‐4E9 in the HeLa MR xenograft model demonstrated clear visualization of tumor after 48 h and confirmed specific binding in tumor. These findings suggest that [131I]I‐4E9 possesses favorable biological characteristics and warrants further investigation as a prospective probe for imaging and treatment of cancers.
Funder
National Natural Science Foundation of China
Subject
Organic Chemistry,Spectroscopy,Drug Discovery,Radiology, Nuclear Medicine and imaging,Biochemistry,Analytical Chemistry