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: 0.147 μM (Lck), 9.1 μM (Src), 14.1 μM (Fgr), 44.1 μM (Fyn)^[1]

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].

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

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].

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

621.73

Solid

C₃₄H₃₉N₉O₃

869748-10-7

NC1=C2C(N([[email protected]@H]3CC[[email protected]@H](N4CCN(C(C)=O)CC4)CC3)N=C2C5=CC=C(NC(C6=CC7=C(C=CC=C7)N6C)=O)C(OC)=C5)=NC=N1

Room temperature in continental US; may vary elsewhere.

• [1]. Stachlewitz RF, et al.A-770041, a novel and selective small-molecule inhibitor of Lck, prevents heart allograft rejection.J Pharmacol Exp Ther. 2005 Oct;315(1):36-41.  [Content Brief]

  [2]. Andrew Burchat, et al. Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection Bioorganic & Medicinal Chemistry Letters Volume 16, Issue 1, 1 January 2006, Pages 118-122  [Content Brief]