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.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PD 0332991 is reviewed on the chemical probes website.
Technical Data
| M. Wt | 573.66 |
| Formula | C24H29N7O2.C2H6O4S |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 827022-33-3 |
| PubChem ID | 11478676 |
| InChI Key | LYYVFHRFIJKPOV-UHFFFAOYSA-N |
| Smiles | O=C1C(C(C)=O)=C(C)C(C=NC(NC4=NC=C(N5CCNCC5)C=C4)=N3)=C3N1C2CCCC2.OCCS(=O)(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.74 | 10 | |
| water | 57.37 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 573.66. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.74 mL | 8.72 mL | 17.43 mL |
| 5 mM | 0.35 mL | 1.74 mL | 3.49 mL |
| 10 mM | 0.17 mL | 0.87 mL | 1.74 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.35 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Toogood et al (2005) Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J.Med.Chem. 48 2388 PMID: 15801831
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
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