Biological Activity:

BIBW2992 (Afatinib) is a highly potent and selective irreversible EGFR inhibitor, inhibiting EGFR^wt, EGFR^L858R, EGFR^L858R/T790M and HER2 with IC₅₀ of 0.5 nM, 0.4 nM, 10 nM, 14 nM, respectively. BIBW2992 suppresses transformation in isogenic cell-based assays, inhibits survival of cancer cell lines, exhibits potent effects on both EGFR and HER2 phosphorylation, and induces tumor regression in xenograft and transgenic lung cancer models, with superior activity over erlotinib. BIBW2992 is currently undergoing Phase III clinical trials for non-small cell lung carcinoma (NSCLC) and breast cancer.

How to Use:

In vitro:  BIBW2992 was used at 1-10 µM final concentration in vitro and in cellular assays.

In vivo: BIBW2992 was orally dosed to mice at 20 mg/kg once per day, or in combination with 2 mg/kg of Rapamycin to significantly reduce the tumor volume. Formulation: 0.5% methylcellulose/0.4% Tween-80.

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