Cas No.: | 575474-82-7 |
Chemical Name: | R-112; R 112 |
Synonyms: | R-112; R 112 |
SMILES: | C1=CC(=CC(=C1)O)NC2=NC(=NC=C2F)NC3=CC(=CC=C3)O |
Formula: | C16H13FN4O2 |
M.Wt: | 312.3 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM. |
In Vitro: | R112 blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action was immediate, and the inhibition was reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 potently, completely, and rapidly abrogated all mast cell activation cascades triggered by IgE receptor cross-linking.[1] |