PD 0332991 isethionate
Tocris Bioscience, part of Bio-Techne | Catalog # 4786
Potent cdk4 and cdk6 inhibitor; brain penetrant
Key Product Details
Description
Potent cdk4 and cdk6 inhibitor; brain penetrant
Alternative Names
Palbociclib
Product Description
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
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.Product Specifications
Molecular Weight
573.66
Formula
C24H29N7O2.C2H6O4S
Storage
Store at RT
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Jorda How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 2018 PMID: 30234987
- Toogood Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J.Med.Chem. 2005 PMID: 15801831
- Fry Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol.Cancer Ther. 2004 PMID: 15542782
- Michaud Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth of glioblastoma multiforme intracranial xenografts. Cancer Res. 2010 PMID: 20354191
Product Specific Notices for PD 0332991 isethionate
For research use only
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