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It is a disease with pronounced clinical and biological heterogeneities. The amplification of <jats:italic>MYCN<\/jats:italic>, whose key tumorigenic functions include the promotion of proliferation, facilitation of the cell's entry into the S phase, and prevention of cells from leaving the cell cycle, correlates with poor prognosis. Patients with a high proliferation index disease have low survival rates. Neuroblastoma is one of the most radioresponsive of all human tumors. To exploit this radiosensitivity, radioactive guanidine (<jats:italic>R<\/jats:italic>)\u2010(\u2013)\u20105\u2010[<jats:sup>125<\/jats:sup>I]iodo\u20103\u2032\u2010<jats:italic>O<\/jats:italic>\u2010[2\u2010(\u03b5\u2010guanidinohexanoyl)\u20102\u2010phenylacetyl]\u20102\u2032\u2010deoxyuridine (<jats:bold>9<\/jats:bold>, GPAID) was designed. This compound enters neuroblastoma cells much like metaiodobenzylguanidine (MIBG). Additionally, it cotargets DNA of proliferating cells, an attribute especially advantageous in the treatment of <jats:italic>MYCN<\/jats:italic>\u2010amplified tumors. GPAID was synthesized from the trimethylstannyl precursor with an average yield of &gt;90% at the no\u2010carrier\u2010added specific activities. The norepinephrine transporter\u2010aided delivery of GPAID to neuroblastoma cells was established in the competitive uptake studies with nonradioactive MIBG. The intracellular processing and DNA targeting properties were confirmed in the subcellular distribution experiments. Studies in a mouse model of neuroblastoma demonstrated the therapeutic potential of GPAID. The tin precursor of GPAID can be used to prepare compounds radiolabeled with single\u2010photon emission computed tomography (SPECT)\u2010 and positron\u2010emission tomography (PET)\u2010compatible radionuclides. Accordingly, these reagents can function as theranostics useful in the individualized and comprehensive treatment strategies comprising treatment planning and the assessment of tumor responses as well as the targeted molecular radiotherapy employing treatment doses derived from the imaging data.<\/jats:p>","DOI":"10.1002\/jlcr.3836","type":"journal-article","created":{"date-parts":[[2020,3,9]],"date-time":"2020-03-09T11:17:19Z","timestamp":1583752639000},"page":"312-324","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Radiolabeled (<i>R<\/i>)\u2010(\u2013)\u20105\u2010iodo\u20103\u2032\u2010<i>O<\/i>\u2010[2\u2010(\u03b5\u2010guanidinohexanoyl)\u20102\u2010phenylacetyl]\u20102\u2032\u2010deoxyuridine: A new theranostic for neuroblastoma"],"prefix":"10.1002","volume":"63","author":[{"given":"Zbigniew P.","family":"Kortylewicz","sequence":"first","affiliation":[{"name":"Department of Radiation Oncology, J. 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