Recommanded Product: 5-Amino-2-fluoropyridine. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about 18F-Labeled Pyrido[3,4-d]pyrimidine as an Effective Probe for Imaging of L858R Mutant Epidermal Growth Factor Receptor. Author is Kimura, Hiroyuki; Okuda, Haruka; Ishiguro, Masumi; Arimitsu, Kenji; Makino, Akira; Nishii, Ryuichi; Miyazaki, Anna; Yagi, Yusuke; Watanabe, Hiroyuki; Kawasaki, Ikuo; Ono, Masahiro; Saji, Hideo.
In non-small-cell lung carcinoma patients, L858R mutation of epidermal growth factor receptor (EGFR) are often found and mol. target therapy using EGFR tyrosine kinase inhibitors is effective for the patients. However, the treatment frequently develops drug resistance by secondary mutation, of which approx. 50% is a T790M mutation. Thus, the ability to predict whether EGFR will undergo secondary mutation is extremely important. We synthesized a novel radiofluorinated 4-(anilino)pyrido[3,4-d]pyrimidine derivative ([18F]APP-1) and evaluated its potential as a positron emission tomog. (PET) imaging probe to discriminate different tumor of mutation. EGFR inhibition assay, cell-uptake and biodistribution study showed that [18F]APP-1 binds specifically to the L858R mutant EGFR but not to the L858R/T790M mutant. Finally, PET imaging study using [18F]APP-1 with tumor-bearing mice, the H3255 tumor (L858R mutant) was more clearly visualized than the H1975 tumor (L858R/T790M mutant).
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