产品描述:
A-770041 is an inhibitor of LCK kinase (IC50 = 0.147 µM).{61165} It is selective for LCK over other Src family tyrosine kinases including Src, Fyn, Fgr, HCK, and Tie2 (IC50s = 9.05, 44.1, 14.1, 1.22, and >50 µM, respectively). A-770041 induces dephosphorylation of LCK by SHP-1, inactivating LCK, in IgE/antigen-stimulated bone marrow-derived mast cells (BMMCs).{58868} It inhibits IL-2 production induced by an anti-CD3 antibody and phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) in isolated human whole blood (EC50 = 80 nM) and by concanavalin A (Item No. 14951) in rats.{61166} A-770041 (10 mg/kg) prevents acute rejection and increases graft survival in a rat model of heterotopic heart transplantation. It also inhibits the growth of CTV-1 human acute myeloid leukemia cells (IC50 = 224 nM) and sensitizes U2OSMR and KHOSR2 multidrug resistant human osteosarcoma cells to paclitaxel (Item No. 10461) and doxorubicin (Item No. 15007).{61167,61168}