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A-770041 is an orally active and selective Lck inhibitor that inhibits concanavalin A-stimulated IL-2 production in whole blood and prevents cardiac allograft rejection. A-770041 reduces pulmonary fibrosis by inhibiting TGF-β production in regulatory T cells.
Description | A-770041 is an orally active and selective Lck inhibitor that inhibits concanavalin A-stimulated IL-2 production in whole blood and prevents cardiac allograft rejection. A-770041 reduces pulmonary fibrosis by inhibiting TGF-β production in regulatory T cells. |
Targets&IC50 | Lck:0.147 μM, FGR:14.1 μM, Src:9.1 μM, Fyn:44.1 μM |
In vitro | A-770041 selectively inhibited LCK with IC50=0.147 μM; A-770041 inhibited other SRC family kinases with SRC IC50=9.1 μM, FGR IC50=14.1 μM, and FYN IC50=44.1 μM. [1] A-770041 dose-dependently (0-30 μM; 2 h) inhibited anti-CD3-induced IL-2 production with an EC50 = 80 nM. [1] |
In vivo | Recipient animals were treated with vehicle control or 2.5 to 20 mg/kg/day of A-770041 in equally. Animals were treated for 14 days, and graft viability was assessed by abdominal palpation each day. A-770041 dosed at 2.5 mg/kg/day did not lengthen graft survival time. There was a dose-dependent increase in survival with doses of 5 and 10 mg/kg/day. At doses of 10 and 20 mg/kg/day of A-770041, 100% of transplanted grafts were still beating at 14 days. [1] |
Alias | A770041, A 770041 |
Molecular Weight | 621.73 |
Formula | C34H39N9O3 |
Cas No. | 869748-10-7 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 20 mg/mL(32.17 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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