In vivo evaluation of the biodistribution of 11C-labeled PD153035 in rats without and with neuroblastoma implants
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Synthesis and evaluation of novel F-18 labeled 4-aminoquinazoline derivatives: Potential PET imaging agents for tumor detection
2012, Bioorganic and Medicinal Chemistry LettersRadiolabelled receptor-tyrosine-kinase targeting drugs for patient stratification and monitoring of therapy response: Prospects and pitfalls
2010, The Lancet OncologyCitation Excerpt :Up to now, the TKI probes most studied, and the first in clinical assessments, are quinazoline-based inhibitors of EGFR-TK. By use of 11C-PD153035, a high contrast visualisation of tumour xenografts (tumour-to-contralateral side ratio of 15) has been shown in rats.67 However, high liver uptake, predominantly hepatobiliary excretion, and relatively rapid washout of radioactivity from the tumours were also shown.
Synthesis and radiopharmacological investigation of 3-[4′-[<sup>18</sup>F]fluorobenzylidene]indolin-2-one as possible tyrosine kinase inhibitor
2009, Bioorganic and Medicinal ChemistryA fully automated two-step synthesis of an <sup>18</sup>F-labelled tyrosine kinase inhibitor for EGFR kinase activity imaging in tumors
2009, Applied Radiation and IsotopesExperimental results and related clinical implications of PET detection of epidermal growth factor receptor (EGFr) in cancer
2009, Annals of OncologyCitation Excerpt :Until now, many labelled reversible and irreversible TK compounds were synthesized, each one with good chemical properties and high inhibitory potency in vitro [12, 87] (Table 3). One of the first labelled compounds, 11C-4-(3-bromoanilino)-6,7-dimethoxyquinazoline (11C-PD153035), was reported in 1999 by Fredriksson et al. [88] in human neuroblastoma xenograft rats and obtained some really preliminary results on the in vivo biodistribution of the tracer. In 2001, Bonasera et al. [89] synthesized five 4-(anilino)quinazoline derivatives (ML01) radiolabelled with fluorine-18 (18F) in the aniline moiety.