A-770041

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^[1][2]. IC50 & Target:IC50: 0.147 μM (Lck), 9.1 μM (Src), 14.1 μM (Fgr), 44.1 μM (Fyn)^[1] In Vitro: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^[1].
A-770041 (0-30 μM; 2 h) dose-dependently inhibits anti-CD3 induced IL-2 production with an EC₅₀ value of 80 nM^[1]. In Vivo:A-770041 (2.5 mg/kg; i.g. once) inhibits concanavalin A-induced IL-2 in vivo^[1].
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^[1].