Authors:
Jianjun WangRadiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 China

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Jing YangRadiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 China

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Zeyi YanRadiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 China

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Xiaojiang DuanRadiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 China

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Cunmin TanRadiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 China

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Yinglin ShenRadiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 China

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Wangsuo WuRadiochemistry Lab, School of Nuclear Science and Technology, Lanzhou University, Lanzhou, 730000 China

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Abstract  

This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of [99mTc(CO)3(IDA–PEG3–CB)]. The novel chlorambucil derivative was successfully synthesized by conjugation of iminodiacetic acid (IDA) to chlorambucil via a pegylated linker. The ligand could be labeled by [99mTc(CO)3]+ core in high yield to get [99mTc(CO)3(IDA–PEG3–CB)], which was very hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [99mTc(CO)3(IDA–PEG3–CB)] accumulated in the tumor with favorable uptake and retention. The good accumulation in tumor tissue with high tumor/muscle ratios warrants further research to improve tumor targeting efficacy and pharmacokinetic profile of radiolabeled chlorambucil derivative by structural modification.

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Journal of Radionalytical and Nuclear Chemistry
Language English
Size A4
Year of
Foundation
1968
Volumes
per Year
1
Issues
per Year
12
Founder Akadémiai Kiadó
Founder's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
Publisher's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible
Publisher
Chief Executive Officer, Akadémiai Kiadó
ISSN 0236-5731 (Print)
ISSN 1588-2780 (Online)

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