TX1-85-1 is an inhibitor of the epidermal growth factor receptor tyrosine kinase ErbB3 (IC50 = 23 nM).1 It also binds to ErbB2, Lyn, and several other Src family kinases in a live cell chemical proteomics assay when used at a concentration of 2 ?M. TX1-85-1 inhibits phosphorylation of Akt and ERK1/2 in ErbB3-dependent HCC2935 and OVCAR-8 cells when used at concentrations of 5 and 2 ?M, respectively. However, it does not inhibit proliferation of ErbB3-dependent PC9 GR4, HCC827 GR8, or OVCAR-8 cells (EC50s = ≥10 ?M).
1.Xie, T., Lim, S.M., Westover, K.D., et al.Pharmacological targeting of the pseudokinase Her3Nat. Chem. Biol.10(12)1006-1012(2014)