PD 0332991 isethionate
Cat. No. 4786
Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[
Biological ActivityPotent Cdk4/6 inhibitor (IC50 values are 11 and 15 nM for Cdk4 and Cdk6 respectively). Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC50 values are > 10 μM). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines; blocks growth of intracranial glioblastoma multiforme xenografts in mice. Brain penetrant.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Fry et al (2004) Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol.Cancer Ther. 3 1427. PMID: 15542782.
Toogood et al (2005) Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J.Med.Chem. 48 2388. PMID: 15801831.
Michaud et al (2010) Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth of glioblastoma multiforme intracranial xenografts. Cancer Res. 70 3228. PMID: 20354191.
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Keywords: PD 0332991 isethionate, supplier, PD0332991, isethionate, cyclin, dependent, kinases, Cdk4, Cdk6, selective, potent, inhibitors, inhibits, antitumor, G1, cell, cycle, arrest, brain, penetrant
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