| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.147 μM (Lck), 9.1 μM (Src), 14.1 μM (Fgr), 44.1 μM (Fyn) | ||||||||||||
| Invitro | 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]. Animal Model: | ||||||||||||
| Name | A-770041 | ||||||||||||
| CAS | 869748-10-7 | ||||||||||||
| Formula | C34H39N9O3 | ||||||||||||
| Molar Mass | 621.73 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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 |