R 547
Tocris Bioscience, part of Bio-Techne | Catalog # 5494
Potent and selective cdk inhibitor; orally bioavailable
Key Product Details
Description
Potent and selective cdk inhibitor; orally bioavailable
Product Description
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.Product Specifications
Molecular Weight
441.45
Formula
C18H21F2N5O4S
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
[4-Amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)methanone
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for R 547
For research use only
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