Syk Inhibitor II 

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

340.30

C₁₄H₁₅F₃N₆O

726695-51-8

Solid

White to off-white

O=C(C1=CN=C(NCCN)N=C1NC2=CC=CC(C(F)(F)F)=C2)N

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]