General description
A cell-permeable imidazopyrimidine compound that acts a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (IC50 = 10 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src even at concentrations as high as 4.7 µM. Shown to inhibit Syk-mediated cellular functions in vitro and exhibit good oral bioavailability and in vivo effacacy in the treatment of various allgery and asthma conditions in rat models.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Syk
Product competes with ATP.
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Yamamoto, N., et al. 2003. J. Pharm. Exp. Ther.306, 1174.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥97% (HPLC) |
| form | solid |
| potency | 10 nM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,desiccated (hygroscopic),protect from light |
| color | yellow |
| solubility | DMSO: 10 mg/mL,water: 20 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | [n]21c(ncc2)cc(nc1Nc4ncccc4C(=O)N)c3cc(c(cc3)OC)OC |
| InChI | 1S/C20H18N6O3/c1-28-15-6-5-12(10-16(15)29-2)14-11-17-22-8-9-26(17)20(24-14)25-19-13(18(21)27)4-3-7-23-19/h3-11H,1-2H3,(H2,21,27)(H,23,24,25) |
| InChI key | JWQOJVOKBAAAAR-UHFFFAOYSA-N |
