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Submit ReviewPD 0332991 isethionate
Description: Potent cdk4 and cdk6 inhibitor; brain penetrant
Alternative Names: Palbociclib
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
Purity: ≥98% (HPLC)
Biological Activity
Potent cyclin-dependent kinase 4 (cdk4) and cdk6 inhibitor (IC50 values are 11 nM and 15 nM respectively). Also displays activity at cdk2, cdk5 and cdk9 (IC50 values reported to be 1.6, 1.8 and 0.42-1.1 μM, respectively). 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 57.37 | 100 | |
| DMSO | 5.74 | 10 |
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 the degree 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 biological activity of the product.
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
Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987
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1 Citation for PD 0332991 isethionate
Citations are publications that use Tocris products. Selected citations for PD 0332991 isethionate include:
Garcia et al (2019) Huntington's Disease Patient-Derived Astrocytes Display Electrophysiological Impairments and Reduced Neuronal Support. Front Neurosci 13 669 PMID: 31316341
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.