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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 for PD 0332991 isethionate
PD 0332991 isethionate is a 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 for PD 0332991 isethionate
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 isethionate is reviewed on the Chemical Probes website.
Technical Data for PD 0332991 isethionate
| M. Wt | 573.66 |
| Formula | C24H29N7O2.C2H6O4S |
| Storage | Store 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 for PD 0332991 isethionate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 57.37 | 100 | |
| DMSO | 5.74 | 10 |
Preparing Stock Solutions for PD 0332991 isethionate
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 for PD 0332991 isethionate
References for PD 0332991 isethionate
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
If you know of a relevant reference for PD 0332991 isethionate, please let us know.
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8 Citations 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
Elmar et al (2021) Human cells lacking CDC14A and CDC14B show differences in ciliogenesis but not in mitotic progression. J Cell Sci 134 PMID: 34432036
Elmar et al (2021) Human cells lacking CDC14A and CDC14B show differences in ciliogenesis but not in mitotic progression. J Cell Sci 134 PMID: 33328327
Jacques et al (2017) Cell-Cycle Regulation Accounts for Variability in Ki-67 Expression Levels. Cancer Res 77 2722-2734 PMID: 28283655
Jia et al (2022) Selective activation and down-regulation of Trk receptors by neurotrophins in human neurons co-expressing TrkB and TrkC. J Neurochem 161 463-477 PMID: 35536742
Michael A et al (2020) Differentiation of PTH-Expressing Cells From Human Pluripotent Stem Cells. Endocrinology 161 PMID: 32810225
Elmar et al (2020) Human cells lacking CDC14A and CDC14B show differences in ciliogenesis but not in mitotic progression. J Cell Sci PMID: 34005417
Charlotta et al (2020) CEP44 ensures the formation of bona fide centriole wall, a requirement for the centriole-to-centrosome conversion. Nat Commun 11 903 PMID: 32060285
Do you know of a great paper that uses PD 0332991 isethionate from Tocris? Please let us know.
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