Biological Activity
Selective p38α and β kinase inhibitor (EC50 = 0.1 μM for p38α). Selective for p38α/β over a panel of 48 other human kinases. Inhibits LPS-induced TNFα release from PBMCs. Also inhibits cytokine release in an LPS-induced endotoxemia model in mice. Orally bioavailable.
Technical Data
| M. Wt | 398.41 |
| Formula | C24H16F2N4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 755753-89-0 |
| PubChem ID | 24822135 |
| InChI Key | VMAKTIDYMSNPOV-UHFFFAOYSA-N |
| Smiles | CN1C=C2C(N=C(C(C3=CC=NC=C3)=C2C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 19.92 | 50 | |
| DMSO | 39.84 | 100 | |
| ethanol | 39.84 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 398.41. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.51 mL | 12.55 mL | 25.1 mL |
| 5 mM | 0.5 mL | 2.51 mL | 5.02 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Mihara et al (2008) A potent and selective p38 inhibitor protects against bone damage in murine collagen-induced arthritis: a comparison with neutralization of mouse TNFalpha. Br.J.Pharmacol. 154 153 PMID: 18297096
Keywords: Org 48762-0, supplier, Org48762-0, MAPK, mitogen-activated, protein, kinases, inhibitors, inhibits, p38, α, β, alpha, beta, selective, orally, bioavailable, p38, p38, Tocris Bioscience
