R 547

Name: R 547
Brand: Tocris Bioscience
SKU: 5494

Tocris Bioscience, part of Bio-Techne | Catalog # 5494

COA / SDS

Potent and selective cdk inhibitor; orally bioavailable

Key Product Details

Description:	Potent and selective cdk inhibitor; orally bioavailable
Chemical Name:	[4-Amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)methanone
Purity:	≥98% (HPLC)
Molecular Weight:	441.45

View Full Technical Details for R 547

Technical Data
Citations

Biological Activity for R 547

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 for R 547

M. Wt	441.45
Formula	C₁₈H₂₁F₂N₅O₄S
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	741713-40-6
PubChem ID	6918852
InChi Key	JRNJNYBQQYBCLE-UHFFFAOYSA-N
Smiles	FC1=C(C(C2=C(N)N=C(NC3CCN(S(C)(=O)=O)CC3)N=C2)=O)C(OC)=CC=C1F

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.

Solubility for R 547

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	44.15	100

Preparing Stock Solutions for R 547

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

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References for R 547

References are publications that support the biological activity of the product.

DePinto 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. 2006 PMID: 17121911
Chu 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. 2006 PMID: 17064073