A-770041

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

A-770041 是一种选择性口服活性 Src 家族 Lck 抑制剂，也是参与 T 细胞信号转导的另一种 Src 家族激酶。

A-770041 is selective and orally active Src-family Lck inhibitor, and the other Src family kinase involved in T-cell signaling. A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, IC50 value: 147 nM Target: Lck.

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.

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.

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Tyrosine Kinase

Src

Lck

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869748-10-7

621.73

C34H39N9O3

>98% (HPLC)

DMSO: 100 mg/mL (160.84 mM)

CC(N(CC1)CCN1C(CC1)CCC1n(c1ncnc(N)c11)nc1-c(cc1)cc(OC)c1NC(c1cc(cccc2)c2n1C)=O)=O

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(-20℃)

With Ice Pack

≥ 2 years