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编 号:F282966
分子式:C14H17Cl2F3N6O
分子量:413.23
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生物活性:
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect.

体内研究:
Syk Inhibitor II (Compound 9a; 10-100 mg/kg) dihydrochloride 在抗原攻击前 30 分钟皮下给药,以剂量依赖方式抑制过敏反应,ID50 值为13.2 mg/kg。Animal Model:ICR mice
Dosage:10, 30, 100 mg/kg
Administration:S.c.; 30 min before antigen challenge
Result:Inhibited the anaphylaxis reaction dose-dependently with an ID50 value of 13.2 mg/kg.

体外研究:
Syk Inhibitor II (compound 9a) dihydrochloride 对 PKCε、PKCβ2、ZAP-70、Btk 和 Itk 的作用较弱,IC50 值分别为 5.1 μM、11 μM、11.2 μM、15.5 μM 和 22.6 μM。
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