Bioactivity | Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect[1]. | ||||||||||||
Invitro | Syk Inhibitor II (compound 9a) shows less potent against PKCε, PKCβ2, ZAP-70, Btk, and Itk with IC50 values of 5.1 µM, 11 µM, 11.2 µM, 15.5 µM, and 22.6 µM, respectively[1]. | ||||||||||||
In Vivo | 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 ID50 value of 13.2 mg/kg[1]. | ||||||||||||
Name | Syk Inhibitor II | ||||||||||||
CAS | 726695-51-8 | ||||||||||||
Formula | C14H15F3N6O | ||||||||||||
Molar Mass | 340.30 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |