Molecular Formula | C22H19BrF2N2O3 |
Molar Mass | 477.3 |
Density | 1.51 |
Appearance | powder |
Color | white to beige |
Storage Condition | 20-25°C |
In vitro study | PH-797804 acts on the human monocytic U937 cell line, blocking LPS-induced TNF-α production and p38 kinase activity with IC50 of 5.9 and 1.1 nM. No Inhibitory effect was observed on the JNK pathway (c-Jun phosphorylation) or ERK pathway (ERK phosphorylation) in U937 cells at concentrations up to 1 μm. PH-797804 inhibits RANKL-and M-CSF-induced osteoclast formation in primary rat bone marrow cells in a concentration-dependent manner with IC50 = 3 nM. PH-797804 IC50 values greater than 200 μm for the following targets: CDK2, ERK2, IKK1, IKK2, IKKi, MAPKAP2, MAPKAP3, MKK7 (>100 μm), MNK, MSK (>164 μm), PRAK, RSK2, and TBK1, illustrate that the activity of PH-797804 is specific. |
In vivo study | The acute inflammatory response induced by systemic administration of Endotoxin to rats and cynomolgus monkeys can be effectively inhibited by PH-797804 by oral administration. PH-797804 treatment model disease model, treated for 10 days, has strong anti-inflammatory activity, acting on streptococcal cell wall-induced arthritis and collagen-induced arthritis in rats and mice, significantly reducing joint inflammation and related bone loss. Dose-response analysis showed that the ED50 for rats and cynomolgus monkeys were 0.07 mg/kg and 0.095 mg/kg, respectively. PH-797804 inhibited LPS-induced TNF-α, IL-6, and MK-2 activity in a human Endotoxin challenge model in a dose-and concentration-dependent manner. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.095 ml | 10.476 ml | 20.951 ml |
5 mM | 0.419 ml | 2.095 ml | 4.19 ml |
10 mM | 0.21 ml | 1.048 ml | 2.095 ml |
5 mM | 0.042 ml | 0.21 ml | 0.419 ml |