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) 对 PKCε、PKCβ2、ZAP-70、Btk 和 Itk 的作用较弱，IC₅₀ 值为 5.1 μM、11 μM、11.2 μM、15.5 μM 和 22.6 μM，分别为^[1]。

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

在抗原攻击前 30 分钟，将 Syk Inhibitor II (Compound 9a；10-100 mg/kg) 皮下给药至小鼠。Syk Inhibitor II 以剂量依赖性方式抑制过敏反应，ID₅₀ 值为 13.2 mg/kg^[1]。

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

340.30

C₁₄H₁₅F₃N₆O

726695-51-8

固体

White to off-white

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• [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]