| Identification | Back Directory | [Name]
5-Pyrimidinecarboxamide, 2-[(2-aminoethyl)amino]-4-[[3-(trifluoromethyl)phenyl]amino]-, hydrochloride, hydrate (1:2:2) | [CAS]
1965323-05-0 | [Synonyms]
Syk Inhibitor II dihydrochloride dihydrate
5-Pyrimidinecarboxamide, 2-[(2-aminoethyl)amino]-4-[[3-(trifluoromethyl)phenyl]amino]-, hydrochloride, hydrate (1:2:2) | [Molecular Formula]
C14H18ClF3N6O2 | [MOL File]
1965323-05-0.mol | [Molecular Weight]
394.78 |
| Hazard Information | Back Directory | [Uses]
Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect[1]. | [in vivo]
Syk Inhibitor II (Compound 9a; 10-100 mg/kg) dihydrochloride dihydrate is subcutaneously administered to mice 30 min before antigen challenge. Syk Inhibitor II inhibits the anaphylaxis reaction dose-dependently with an ID50 value of 13.2 mg/kg[1]. | [IC 50]
Syk: 41 nM (IC50); serotonin: 460 nM (IC50); PKCε: 5.1 μM (IC50); PKCβ2: 11 μM (IC50); ZAP-70: 11.2 μM (IC50); Btk: 15.5 μM (IC50); Itk: 22.6 μM (IC50) | [References]
[1] Hiroyuki Hisamichi, et al. Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure-activity relationships of pyrimidine-5-carboxamide derivatives. Bioorg Med Chem. 2005 Aug 15;13(16):4936-51. DOI:10.1016/j.bmc.2005.05.033 |
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