| Assay Method Information | |
| | Inhibition Assay |
| Description: | The object of this assay was to test the inventive compounds for the kinase inhibitory activity in vitro. In this assay, an isotopic labeling method was used to label the gamma phosphate group on ATP. EGFR (including wild type, L858R mutant type and L858R/T790M double mutant type), VEGFR2, ALK, BTK, c-KIT, c-SRC, MET, PDGFRalpha and FLT3 kinases were tested in vitro for the activity inhibition. Staurosporine was used as a reference molecule (or referred to as a positive control). The kinase inhibitory activities of the tested compounds were expressed in the IC50 value (half inhibition concentration) or the kinase activity inhibitory rate by the tested compounds at 10 uM. The IC50 value can be obtained by the calculation of the inhibitory rates at a series of different concentrations of the tested compounds. 1. Materials: 20mM 3-(N-morpholinyl)propylsulfonic acid (MOPS); 1mM Ethylenediaminetetraacetic acid (EDTA); 0.01% Polyethylene glycol lauryl ether (Brij-35). |
| Affinity data for this assay | |
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