Palbociclib (PD0332991)
Kinase inhibitor: CDK4 / CDK6; Autophagy modulator. Inhibits SARS-CoV in silico, probably through blocking the main protease, Mpro (3CLpro, Nsp5). Laise et al. bioRxiv, May 17 2020, https://doi.org/10.1101/2020.05.12.091256; Verma et al. Preprints, Apr 9 2020, https://doi:10.20944/preprints202004.0149.v1; Hosseini and Amanlou Preprints, Feb 28 2020, https://doi:10.20944/preprints202002.0438.v1.
- Datasheet: view or download
- Applications:Approved drug (U.S.) that could be repurposed
Biochemicals & reagents
571190-30-2
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
447.53
-20°C (des.)
Palbociclib is a potent and selective inhibitor of Cdk4, IC50 = 11 nM and Cdk6, IC50 = 16 nM (1). This compound 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). It also induces autophagy and senescence in AGS gastric cancer cells (3) and is clinically useful breast cancer agent (4). Furthetmore, cell cycle inhibitors boost tumor immunogenicity (5).