BIBW2992 (Tovok)

1 mg. Purity >99%. CAS# 439081-18-2. BIBW-2992 is a potent, irreversible combined EGFR/HER2 inhibitor both in vitro and in vivo. The potency of BIBW-2992 on the EGFR and HER2 kinases revealed IC50 values of 0.5 nM and 14 nM, respectively. BIBW-2992 is highly selective for these kinases and no additional inhibition of other kinases has been observed. BIBW2992, an anilino-quinazoline designed to irreversibly bind EGFR and HER2, potently suppresses the kinase activity of wild-type and activated EGFR and HER2 mutants, including erlotinib-resistant isoforms. Consistent with this activity, BIBW2992 suppresses transformation in isogenic cell-based assays, inhibits survival of cancer cell lines and induces tumor regression in xenograft and transgenic lung cancer models, with superior activity over erlotinib. These findings encourage further testing of BIBW2992 in lung cancer patients harboring EGFR or HER2 oncogenes. Soluble in DMSO. Store cool and dry at -20C. Protect from light.