171179-37-6

BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀ = 8 pM).¹ It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR.¹

1. Rewcastle, G.W., Palmer, B.D., Bridges, A.J., et al. Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor J. Med. Chem. 39(4),918-928(1996).