BIBW 2992 is an anilino-quinazoline that irreversibly inhibits EGFR and HER2 kinase activity in cell-free in vitro kinase assays (IC50s = 0.5 and 14 nM, respectively). It demonstrates potent activity against mutant forms of EGFR and HER2, including erlotinib-resistant isoforms (IC50 = 10 nM), and displays weak activity when evaluated against a panel of 52 additional tyrosine and serine/threonine kinases. BIBW 2992 suppresses transformation in isogenic cell-based assays, inhibits survival of cancer cell lines, and at 20 mg/kg, induces tumor regression in xenograft and transgenic lung cancer models.
