R&D Systems Inc. Tocris Bioscience Boston Biochem

PD 0332991 isethionate

Cat. No. 4786

PD 0332991 isethionate C24H29N7O2.C2H6O4S [827022-33-3]

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Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one isethionate salt

Biological Activity

Potent 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 Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
573.66
Formula:
C24H29N7O2.C2H6O4S
Solubility:
Soluble to 100 mM in water and to 10 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
827022-33-3

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

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

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.

If you know of a relevant citation for this product please let us know.

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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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