CL-387785 (EKI785, WAY-EKI785) is a specific, irreversible, covalent EGFR inhibitor with IC50 of 0.37 nM.
CL-387785 blocks EGF-stimulated autophosphorylation of EGFR in A431 cells (IC50=5 nM).
CL-387785 inhibits cell proliferation (IC50= 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-ErbB2, and profoundly blocks the growth of a tumor that overexpresses EGFR in nude mice; orally active.
