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R 547
- RO4584820
- Soluble in DMSO
- MF: C18H21F2N5O4S
- MW: 441.45
Description
R 547 (RO4584820) is a potent and selective CDK1, CDK2 and CDK4 inhibitor with reported Ki values of 1 nM, 3 nM and 1 nM, respectively. It shows weak activity against a broad panel of unrelated kinases in reported profiling.
CDK1, CDK2 and CDK4 regulate cell-cycle progression through G1/S and mitotic checkpoints. R 547 is useful for studying CDK-driven tumor proliferation across models with differing retinoblastoma protein, p53 and multidrug-resistance status.
Key Features
- Potent CDK1/CDK2/CDK4 inhibitor
- Reported Ki: 1 nM (CDK1), 3 nM (CDK2), 1 nM (CDK4)
- Broad reported selectivity over unrelated kinases
- Antiproliferative activity across diverse tumor cell lines
Applications
- Cell-cycle checkpoint studies
- CDK inhibitor profiling
- Cancer proliferation assays
- Rb and p53 pathway research
More Information
| Parent CAS No. | 741713-40-6 |
|---|---|
| Chemical Name | (4-amino-2-(1-(methylsulfonyl)piperidin-4-ylamino)pyrimidin-5-yl)(2,3-difluoro-6-methoxyphenyl)methanone |
| SMILES | C(C1=CN=C(NC2CCN(S(C)(=O)=O)CC2)N=C1N)(C1=C(OC)C=CC(F)=C1F)=O |
| MFCD | MFCD09970629 |
| InChi | InChI=1S/C18H21F2N5O4S/c1-29-13-4-3-12(19)15(20)14(13)16(26)11-9-22-18(24-17(11)21)23-10-5-7-25(8-6-10)30(2,27)28/h3-4,9-10H,5-8H2,1-2H3,(H3,21,22,23,24) |
| InChiKey | JRNJNYBQQYBCLE-UHFFFAOYSA-N |
| CID | 6918852 |
| Short Description | CDK (1/2/4) inhibitor |
References
- XJ Chu et al. 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 (...). J. Med. Chem. 2006, 49(22), 6549-6560.
- W DePinto et al. 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, 5(11), 2644-2658.
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