On Target Driven Efficacy Assessment of CDK2 Inhibitors in the Right Biological Context

Target Engagement and Selectivity Profiling in K562 and MCF7 Cells CETSA® is a label-free method for assessing target engagement of small molecule-protein interactions. Target engagement determination is especially important in oncology, where cell death is often used as the efficacy readout. A key caveat is that the observed cell death must be driven by the intended target rather than by off-target effects, which could represent a future liability. In this study, we assessed the selectivity profiles of three different CDK2 inhibitor probes in both our standard cell line, K562, and an indication-specific cell line, MCF-7.