| Products/Services Used | Details | Operation |
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| Peptide Synthesis | The FGFR1 kinase assays with recombinant cytoplasmic domain of the FGFR1 tyrosine kinase (Millipore, Cat. N. 14-582) were performed in a total volume of 30 µl containing 10 mM MOPS (рН 7.2), 0.1 mM sodium orthovanadate, 0.2 mM EDTA, 0.002 % Brij 35, 0.2 mg/ml BSA, 0.02 % βmercaptoethanole, 250 mM of peptide substrate (KKKSPGEYVNIEFG, GenScript), various concentrations of inhibitor dissolved in DMSO (final DMSO concentration in probe less than 1%) and 7 ng of enzyme. | Get A Quote |
Fibroblast grow factor receptor 1 (FGFR1) is an important anti-cancer target that plays crucial role in oncogenesis and oncogenic angiogenesis. The structure-activity relationship (SAR) of N-phenylthieno[2，3-d]pyrimidin-4-amines was investigated. Binding of active compounds with FGFR1 kinase was analyzed by molecular modeling studies. Selected active thieno[2，3-d]pyrimidines were tested for selectivity and antiproliferative activity. The most active compounds， 3-({6-phenylthieno[2，3-d]pyrimidin-4-yl}amino)phenol and 3-({5-phenylthieno[2，3-d]pyrimidin-4-yl}amino)phenol have IC?? 0.16 and 0.18 μM， respectively. The results presented here may help to identify new thienopyrimidines with optimized cell ... More
