142685-25-4Relevant articles and documents
In situ monitoring of bindings between dasatinib and its target protein kinases using magnetic nanoparticles in live cells
Kim, Dae-Joong,Yi, Yong-Weon,Jin, Hwan Kim
, p. 16466 - 16467 (2008)
We report a novel technology, called In Cell IT, for in situ monitoring of bindings between a small molecule kinase inhibitor and its target protein kinases in live cells using a kinase inhibitor, dasatinib, as a model compound. Streptavidin-attached MNPs were coated by biotinylated dasatinib, and then these dasatinib-MNPs were transferred into cells. In the cells, the MNPs were aligned to the same direction of the magnetic field and EGFP-tagged target protein kinases were bound to dasatinib-MNPs. Using this technology, we demonstrated the bindings between dasatinib and its target protein kinases including SRC, ABL1, and CSK in live cells. The specificity of these bindings was also confirmed by cold competition using unbiotinylated dasatinib in the same cells. Copyright
Synthesis of [18F]-labeled EF3 [2-(2-nitroimidazol-1-yl)-N-(3,3,3-trifluoropropyl)-acetamide], a marker for PET detection of hypoxia
Josse, Olivier,Labar, Daniel,Georges, Benoit,Grégoire, Vincent,Marchand-Brynaert, Jacqueline
, p. 665 - 675 (2007/10/03)
[18F]-2-(2-Nitroimidazol-1-yl)-N-(3,3,3-trifluoropropyl)-acetamide ([18F]-EF3) has been prepared, in 65% chemical yield and 5% radiochemical yield, by coupling 2,3,5,6-tetrafluorophenyl 2-(2-nitroimidazol-1-yl) acetate 1 with [18F]-3,3,3-trifluoropropylamine 7. This original radiolabelled key-synthon was obtained in 40% overall chemical yield by oxidative [18F]-fluorodesulfurization of ethyl N-phthalimido-3-aminopropane dithioate 4, followed by deprotection with hydrazine of the resulting [18F]-N-phthalimido-3,3,3-trifluoropropylamine 5. All the process was performed within 90min, from the [18F]-HF production in the cyclotron to the purification of the final target. Copyright
Selective binding complementary oligonucleotides
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, (2008/06/13)
In a matched pair of oligonucleotides (ODNS) each member of the pair is complementary or substantially complementary in the Watson Crick sense to a target sequence of duplex nucleic acid where the two strands of the target sequence are themselves compleme