Palbociclib

Light-yellow or off-yellow powder, beige. Soluble in DMSO (2mg/ml). Chemical. CAS: 571190-30-2. Formula: C24H29N7O2. MW: 447.53. Palbociclib is a potent and selective inhibitor of CDK4 (IC50=11nM) and CDK6 (IC50=16nM). Displays selectivity for Cdk4/6 over a panel of 36 additional protein kinases. It exhibits selective antiproliferation activity against Rb-positive human breast/colon/lung/leukemia cancer cultures and displays in vivo efficacy against various advanced stage human tumor xenografts in mice. It 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. Induces autophagy and senescence in AGS gastric cancer cells. It is a clinically useful breast cancer agent. In addition cell cycle inhibitors have been shown to boost tumor immunogenicity.