SYK INHIBITOR II
| 中文名称 | SYK INHIBITOR II |
|---|---|
| 中文同义词 | 化合物SYK INHIBITOR II;2-((2-氨基乙基)氨基)-4-((3-三氟甲基)苯基)氨基)嘧啶-5-甲酰胺 |
| 英文名称 | Syk Inhibitor II |
| 英文同义词 | ATP-competitive,Serotonin Receptor,antigen,inhibit,Spleen tyrosine kinase,Syk Inhibitor II,Anti-allergic,pyrimidine-carboxamide,Inhibitor,Syk,5-HT Receptor,5-hydroxytryptamine Receptor;5-Pyrimidinecarboxamide, 2-[(2-aminoethyl)amino]-4-[[3-(trifluoromethyl)phenyl]amino]-;2-((2-Aminoethyl)amino)-4-((3-(trifluoromethyl)phenyl)amino)pyrimidine-5-carboxamide |
| CAS号 | 726695-51-8 |
| 分子式 | C14H15F3N6O |
| 分子量 | 340.3 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 726695-51-8.mol |
| 结构式 |  |
SYK INHIBITOR II 性质
| 熔点 | 270-272 °C (decomp)(Solv: water (7732-18-5); ethanol (64-17-5)) |
|---|---|
| 沸点 | 541.6±60.0 °C(Predicted) |
| 密度 | 1.455±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMF：25mg/mL；二甲基亚砜：15mg/mL |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 14.04±0.50(Predicted) |
| 颜色 | 白色至米白色 |
|
serotonin 460 nM (IC 50 ) |
Syk 41 nM (IC 50 ) |
PKCε 5.1 μM (IC 50 ) |
PKCβ2 11 μM (IC 50 ) |
ZAP-70 11.2 μM (IC 50 ) |
Btk 15.5 μM (IC 50 ) |
Itk 22.6 μM (IC 50 ) |
Syk Inhibitor II (compound 9a) shows less potent against PKCε, PKCβ2, ZAP-70, Btk, and Itk with IC 50 values of 5.1 µM, 11 µM, 11.2 µM, 15.5 µM, and 22.6 µM, respectively.
Syk Inhibitor II (Compound 9a; 10-100 mg/kg) is subcutaneously administered to mice 30 min before antigen challenge. Syk Inhibitor II inhibits the anaphylaxis reaction dose-dependently with an ID 50 value of 13.2 mg/kg.