PD 0332991 isethionate

Name: PD 0332991 isethionate
Brand: Tocris Bioscience
SKU: 4786

Tocris Bioscience, part of Bio-Techne | Catalog # 4786

Citations (18)

COA / SDS

Potent cdk4 and cdk6 inhibitor; brain penetrant

Key Product Details

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)
Molecular Weight:	573.66

View Full Technical Details for PD 0332991 isethionate

Technical Data
Citations

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

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 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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References for PD 0332991 isethionate

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