Palbociclib
CDK4/CDK6 inhibitor / 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
Biochemicals & reagents
571190-30-2
PD-332991; PD0332991
1) El-Rayes et al. (2004), Cyclooxygenase-2-dependent and –independent effects of celecoxib in pancreatic cancer cell lines; Mol. Cancer Ther., 3 1427 2) Menu et al. (2008), A novel therapeutic combination using PD 0332991 and bortezomib: study in 5T33MM myeloma model; Cancer Res., 68 5519 3) Valenzuela et al. (2017), Palbociclib-induced autophagy and senescence in gastric cancer cells; Exp. Cell Res., 360 390 4) Palanisamy et al. (2016), Palbociclib: A new hope in the treatment of breast cancer; J. Cancer Res. Ther., 12 1220 5) Minton et al. (2017) Tumour immunology: Cell cycle inhibitors boost tumour immunogenicity; Nat. Rev. Immunol., 17 529
-20°C
TARGET: Kinase -- PATHWAY: Autophagy; Glycation; Cell cycle; Senescence; Carbohydrate metabolism -- RESEARCH AREA: Immunology; Cell death -- DISEASE AREA: Cancer; DiabetesAgeing