PD 0332991 isethionate

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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)
Datasheet
Citations (8)
Reviews

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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


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8 Citations for PD 0332991 isethionate

Citations are publications that use Tocris products. Selected citations for PD 0332991 isethionate include:

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


Do you know of a great paper that uses PD 0332991 isethionate from Tocris? Please let us know.

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