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PH 797804
- Soluble in DMSO and EtOH
- MF: C22H19BrF2N2O3
- MW: 477.3
Description
Highly potent, selective and metabolically stable inhibitor of p38 MAPK (p38α cascade IC50: 2.3 nM); an ATP-competitive, readily reversible inhibitor of the α isoform of human p38 MAP kinase, exhibiting a Ki of 5.8 nM; clinical candidate.
*PH 797804 is an (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer. Be careful that racemate of PH 797804 is wrongly provided by other supplier as drug PH 797804 itself. The less potent (+)-rotating atropisomer is also available (inquire). Be right about your drug.
The racemate, (±)-PH797804 (Axon 2786) is also available.
More Information
| Parent CAS No. | 586379-66-0 |
|---|---|
| Chemical Name | 3-(3-bromo-4-(2,4-difluorobenzyloxy)-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide |
| SMILES | C1(OCC2C=CC(F)=CC=2F)C=C(C)N(C2C(C)=CC=C(C(=O)NC)C=2)C(=O)C=1Br |
| MFCD | N.A. |
| InChi | InChI=1S/C22H19BrF2N2O3/c1-12-4-5-14(21(28)26-3)9-18(12)27-13(2)8-19(20(23)22(27)29)30-11-15-6-7-16(24)10-17(15)25/h4-10H,11H2,1-3H3,(H,26,28) |
| InChiKey | KCAJXIDMCNPGHZ-UHFFFAOYSA-N |
| CID | 22049997 |
| Short Description | p38 MAPK inhibitor |
References
- HR Hope et al. Anti-Inflammatory Properties of a Novel N-Phenyl Pyridinone Inhibitor of p38 Mitogen-Activated Protein Kinase: Preclinical-to-Clinical Translation. J. Pharmacol. Exp. Ther. 2009, 331(3), 882-895.
- SR Selness et al. Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase. Bioorg. Med. Chem. Lett. 2011, 21(13), 4066-4071.
- L Xing et al. Discovery and Characterization of Atropisomer PH-797804, a p38 MAP Kinase Inhibitor, as a Clinical Drug Candidate. ChemMedChem. 2012, 7(2), 273–280.
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