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Assessing Differences in Biochemical and Cell-based Profiles using Sutent as a Case Study
In this case study, we confirmed Tarceva®’s selectivity for the EFGR family when profiled against a panel of kinases using the SelectScreen® Kinase Profiling Service. Additional cellular profiling data was generated using a panel of cellular assays corresponding to different signaling pathways and correlated to the biochemical kinase profiling data. Furthermore, the SelectScreen® hERG Screening Service was used to confirm that Tarceva® did not indicate a risk for potential hERG liability.
Correlating Biochemical and Cell based Profiles for PI3K_Akt-mTOR using PI-103 as a Case Study
In this case study, we confirmed the selectivity of PI-103 for the PI3K/Akt/mTOR pathway by profiling a broad panel of kinases utilizing the SelectScreen® Kinase Profiling Service. This selectivity was also confirmed by profiling a broad panel of cell-based assays corresponding to different signal transduction pathways. Furthermore, using the SelectScreen® hERG Screening service we screened PI-103 for potential safety and liability risk.
Correlating Biochemical and Cell-based Profiles for EGFR using Tarceva as a Case Study
In this study, we identified that Nexavar® had a broad kinase inhibition profile within three distinct families. Although cell-based profiling indicated the same broad inhibition pattern across many signal transduction pathways, there were some observed differences in potency within the NFkappaB pathway. These differences in potency were observed using different cellular backgrounds indicating that the choice of relevant cellular backgrounds is important when profiling compounds.
Evaluating Biochemical and Cell Based Profiles using Nexavar as a Case Study
In this study, profiling a broad panel of kinases indicated a non-selective inhibition pattern for Sutent®. However, cell-based profiling indicated a more selective inhibitor profile than that suggested in the biochemical study. This case study establishes the importance of profiling your compound using both biochemical and cell-based assays.