R 547

Biological Activity

R 547 is a potent and selective CDK inhibitor (K_i values are 1, 2, 3, 46, 171 and 260 nM for CDK4/cyclin D1, CDK1/cyclin B, CDK2/cyclin E, GSK3α, CDK7/cyclin H and GSK3β). Exhibits no effect against a panel of >120 other kinases (K_i > 5,000 nM). Inhibits the proliferation of tumor cell lines independent of multidrug resistant status, or p53 status. Suppresses retinoblastoma protein in tumor cells and xenografts. Also inhibits tumor growth in the HCT116 human colorectal tumor xenograft model in nude mice. Orally bioavailable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
   Chu et al.
   J.Med.Chem., 2006;49:6549
2. In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.
   DePinto et al.
   Mol.Cancer Ther., 2006;5:2644

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