An inhibitor of the cyclin-dependent kinases Cdk1/cyclin B

R547 – 1 mg

Brand:
Cayman
CAS:
741713-40-6
Storage:
-20
UN-No:
Non-Hazardous - /

Cyclin-dependent kinases (Cdks) are critical positive regulators of cell cycle progression and cellular transcription whose dysregulation can lead to the development of cancer. R547 is a diaminopyrimidine compound that inhibits Cdk1/cyclin B, Cdk2/cyclin E, and Cdk4/cyclin D1 (Kis = 1-3 nM).{29463} It is inactive against a panel of more than 120 unrelated kinases (Kis > 5 µM).{29463} R547 inhibits tumor cell proliferation (IC50s ≤ 0.6 µM in vitro), inducing cell cycle arrest at G1 and G2 phases and apoptosis as well as reducing phosphorylation of the retinoblastoma protein.{29463} It also demonstrates antitumor activity in vivo in various human tumor xenograft models.{29463}  

 

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Description

An inhibitor of the cyclin-dependent kinases Cdk1/cyclin B, Cdk2/cyclin E, and Cdk4/cyclin D1 (Kis = 1-3 nM); inhibits tumor cell proliferation (IC50s ≤ 0.6 µM in vitro), inducing cell cycle arrest and apoptosis as well as reducing phosphorylation of the retinoblastoma protein

Formal name: [4-amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)-methanone

Synonyms:  Ro 4584820

Molecular weight: 441.5

CAS: 741713-40-6

Purity: ≥98%

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 Cycle|G2/M||Research Area|Cancer|Cell Cycle|G2/S||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling

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