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Tocris/PD 0332991 isethionate/4786/50/50 mg

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货号: 4786/50

品牌: Tocris

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Description: Potent, selective Cdk4/6 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 Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent Cdk4/6 inhibitor (IC₅₀ values are 11 and 15 nM for Cdk4 and Cdk6 respectively). Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC₅₀ values are > 10 μM). 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	5.74	10
	water	57.37	100

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 solvent 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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

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

Keywords: PD 0332991 isethionate, supplier, PD0332991, isethionate, cyclin, dependent, kinases, Cdk4, Cdk6, selective, potent, inhibitors, inhibits, antitumor, G1, cell, cycle, arrest, brain, penetrant, Palbociclib, Cyclin-dependent, Kinase, Cyclin-dependent, Kinase, Tocris Bioscience

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