产品
编 号:F488984
分子式:C34H39N9O3
分子量:621.73
产品类型
结构图
CAS No: 869748-10-7
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产品详情
生物活性:
A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection.
体内研究:
A-770041 (2.5 mg/kg; i.g. once) inhibits concanavalin A-induced IL-2 in vivo.A-770041 (2.5-20 mg/kg/day; for 14 days) dose-dependently increases the survival rate with doses of 5 and 10 mg/kg/day, and survives 100% of transplanted grafts until 14 days with doses of 10 and 20 mg/kg/day.Animal Model:Male Lewis rats
Dosage:2.5 mg/kg
Administration:Intragastric administration; 2.5 mg/kg once
Result:Showed an inhibition of concanavalin A-induced IL-2 with an in vivo EC50 value of 78 nM.
体外研究:
A-770041 selective inhibits Lck with an IC50 value of 0.147 μM, and inhibits other Src family kinase Src, Fgr, Fyn with IC50s of 9.1, 14.1 and 44.1 μM, respectively.A-770041 (0-30 μM; 2 h) dose-dependently inhibits anti-CD3 induced IL-2 production with an EC50 value of 80 nM.