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Description

A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1R (insulin-like growth factor-1 receptor) kinase autophosphorylation (IC50 = 400 nM). Also inhibits the phosphorylation of PTK substrate poly (Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC50 = 60 nM, 113 nM, and 2.4 µ,M respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC50 = 76 µ,M). Inhibition is competitive with respect to the substrate binding site of IGF-1R kinase. Also inhibits the authophosphorylation of IGF-1R and the activation of PKB and ERK2 in NIH-3T3 cells over-expressing IGF-1R., A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1 receptor kinase (IC50 = 400 nM). Reaction is competitive with respect to IGF-1R substrate. Also inhibits the phosphorylation of PTK substrate poly(Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC50 = 60 nM, 113 nM, 370 nM, and 2.4 µ,M, respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC50 = 76 µ,M).