PD 0332991 isethionate

Cat. No. 4786 8 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent cdk4 and cdk6 inhibitor; brain penetrant

别名： Palbociclib

化学名： 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one isethionate salt

纯度： ≥98% (HPLC)

引用文献 (8)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 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.

许可信息

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.

技术数据 for PD 0332991 isethionate

分子量	573.66
公式	C₂₄H₂₉N₇O₂.C₂H₆O₄S
储存	Store at RT
纯度	≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PD 0332991 isethionate

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	water	57.37	100
	DMSO	5.74	10

制备储备液 for PD 0332991 isethionate

以下数据基于产品分子量 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.

浓度/溶剂体积/质量	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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产品说明书 for PD 0332991 isethionate

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PD 0332991 isethionate

参考文献是支持产品生物活性的出版物。

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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