Palbociclib

Potent and selective inhibitor of Cdk4, IC50 = 11 nM and Cdk6, IC50 = 16 nM.1 Inhibits phosphorylation of Rb protein and cell cycle progression through G1 in primary 5T33MM cells and sensitized these cells to killing by a proteasome inhibitor (bortezomib) in mouse models.2 Induces autophagy and senescence in AGS gastric cancer cells.3 Clinically useful breast cancer agent.4 Cell cycle inhibitors boost tumor immunogenicity.5