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R 547 is a potent and selective CDK inhibitor (Ki 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 (Ki > 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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 441.45. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.27 mL||11.33 mL||22.65 mL|
|5 mM||0.45 mL||2.27 mL||4.53 mL|
|10 mM||0.23 mL||1.13 mL||2.27 mL|
|50 mM||0.05 mL||0.23 mL||0.45 mL|
References are publications that support the biological activity of the product.
Chu et al (2006) 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. J.Med.Chem. 49 6549 PMID: 17064073
DePinto et al (2006) In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. Mol.Cancer Ther. 5 2644 PMID: 17121911
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Keywords: R 547, R 547 supplier, R547, Cyclin-dependent, protein, kinases, inhibitors, inhibits, potent, selective, cdk, Cdk1, cdk2, cdk3, cdk4, cyclin, D1, B, E, orally, bioavailable, Kinase, Non-selective, CDKs, 5494, Tocris Bioscience
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