[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547)

Description

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 (K_is = 1-3 nM). It is inactive against a panel of more than 120 unrelated kinases (K_is > 5 μM). 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. It also demonstrates antitumor activity in vivo in various human tumor xenograft models.

What are the applications of Application

R547 is a selective inhibitor of cell cycle and transcriptional cyclin dependent kinases including Cdk1, Cdk2, and Cdk4.

storage

Store at +4°C