882400-92-2Relevant academic research and scientific papers
Chemoselective Radiosyntheses of Electron-Rich [18F]Fluoroarenes from Aryl(2,4,6-trimethoxyphenyl)iodonium Tosylates
Kwon, Young-Do,Son, Jeongmin,Chun, Joong-Hyun
, p. 3678 - 3686 (2019/03/11)
Hypervalent diaryliodonium salts have been used to produce various [18F]fluoroarenes. The iodonium salt approach as a labeling precursor has been established to equally afford complex 18F-fluorinated molecules. Because of the inheren
[18F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent
Zhang, Bo,Fraser, Benjamin H.,Klenner, Mitchell A.,Chen, Zhen,Liang, Steven H.,Massi, Massimiliano,Robinson, Andrea J.,Pascali, Giancarlo
supporting information, p. 7613 - 7617 (2019/05/17)
Fluorine-18 is the most utilized radioisotope in positron emission tomography (PET), but the wide application of fluorine-18 radiopharmaceuticals is hindered by its challenging labelling conditions. As such, many potentially important radiotracers remain
Novel compound having tumor diagnosis or tumor growth inhibitory activity on EGFR mutant and medical uses comprising the same
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Page/Page column 18; 23, (2017/04/03)
The present invention relates to a novel compound having activities of diagnosing a tumor having an epidermal growth factor receptor (EGFR) mutant and inhibiting tumor growth, a salt thereof, a contrast medium comprising the same, and a pharmaceutical composition for treating or preventing EGFR-related cancer diseases comprising the same as an active ingredient. The novel compound or the salt thereof according to the present invention does not inhibit a wild type EGFR but selectively inhibits an EGFR variant, and thus can treat and prevent EGFR-related cancer diseases, including lung cancer, colon cancer or breast cancer. Particularly, the compound or the salt thereof according to the present invention can effectively treat and prevent non-small cell lung cancer upon which Iressa or Tarceva cannot have any significant effect. In addition, the compound or the salt thereof according to the present invention responses with a target of Gefitinib-sensitive cancer cells or cancer cells showing EGFR T790M mutation rather than wild type EGFR over-expressed cancer cells, and thus can be used advisably as a contrast medium capable of clearly differentiating EGFR-related cancer cells by imaging.COPYRIGHT KIPO 2017
Ortho-stabilized 18F-azido click agents and their application in PET imaging with single-stranded DNA aptamers
Wang, Lu,Jacobson, Orit,Avdic, Din,Rotstein, Benjamin H.,Weiss, Ido D.,Collier, Lee,Chen, Xiaoyuan,Vasdev, Neil,Liang, Steven H.
, p. 12777 - 12781 (2015/10/28)
Azido 18F-arenes are important and versatile building blocks for the radiolabeling of biomolecules via Huisgen cycloaddition ("click chemistry") for positron emission tomography (PET). However, routine access to such clickable agents is challenged by inefficient and/or poorly defined multistep radiochemical approaches. A high-yielding direct radiofluorination for azido 18F-arenes was achieved through the development of an ortho-oxygen-stabilized iodonium derivative (OID). This OID strategy addresses an unmet need for a reliable azido 18F-arene clickable agent for bioconjugation reactions. A ssDNA aptamer was radiolabeled with this agent and visualized in a xenograft mouse model of human colon cancer by PET, which demonstrates that this OID approach is a convenient and highly efficient way of labeling and tracking biomolecules. Markedly apt: A high-yielding direct radiofluorination strategy via ortho-oxygen-substituted iodonium derivatives is described. A ssDNA aptamer (sgc8), labelled with the resulting 18F azido agent through click chemistry, was used for PET imaging and provides the first example for the noninvasive in vivo PET imaging of protein tyrosine kinase 7 (PTK-7).
Single-step radiosynthesis of "18F-labeled click synthons" from azide-functionalized diaryliodonium salts
Chun, Joong-Hyun,Pike, Victor W.
, p. 4541 - 4547,7 (2020/08/31)
Positron emission tomography (PET) is an increasingly important biomedical imaging technique that relies on the development of radiotracers labeled with positron emitters to achieve biochemical specificity. Fluorine-18 (t 1/2 = 109.7 min) is an
Strain-promoted copper-free "click" chemistry for 18F radiolabeling of bombesin
Campbell-Verduyn, Lachlan S.,Mirfeizi, Leila,Schoonen, Anne K.,Dierckx, Rudi A.,Elsinga, Philip H.,Feringa, Ben L.
scheme or table, p. 11117 - 11120 (2012/02/02)
Click for PET: The GRP-receptor-specific peptide bombesin, which is often used for nuclear imaging of tumors, can be labeled with 18F in a mild and rapid manner by using a copper-free azide-alkyne "click" reaction. A range of azides can be used to provide peptides with different hydrophobicities. The resulting 18F radiopharmaceutical tracers (see scheme) maintain their high affinity for the targeted receptor in vitro in human prostate cancer cells. Copyright
