An orally active

PD 0332991 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
827022-32-2
Storage:
-20
UN-No:
Non-Hazardous - /

PD 0332991 is an orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM) with no activity against a panel of 36 additional protein kinases.{28137} It has been reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest at nanomolar concentrations.{28137} PD 0332991 can inhibit the growth of certain ER-positive or HER2-amplified breast cancer cells (IC50s as low as 4 nM) and demonstrates synergy with tamoxifen (Item No. 13258) and trastuzumab, respectively.{28138} PD 0332991 inhibition of Cdk4 activity has been used to demonstrate a role for insulin-activated cyclinD1-Cdk4 signaling in the control of glucose metabolism that is independent of cell cycle progression.{26552}  

 

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Description

An orally active, selective inhibitor of Cdk4 (IC50 = 11 nM) and Cdk6 (IC50 = 16 nM) with antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest; used to demonstrate a role for insulin-activated cyclin D1-Cdk4 signaling in the control of glucose metabolism

Formal name: 6-​acetyl-​8-​cyclopentyl-​5-​methyl-​2-​[[5-​(1-​piperazinyl)​-​2-​pyridinyl]​amino]​-pyrido[2,​3-​d]​pyrimidin-​7(8H)​-​one, monohydrochloride

Synonyms:  Palbociclib

Molecular weight: 484

CAS: 827022-32-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Signaling||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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