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Afatinib (BIBW 2992) is a novel irreversible dual EGFR and HER2 tyrosine kinase inhibitor. The potency of Afatinib (BIBW 2992) on the EGFR and HER2 kinases revealed IC50 values of 0.5 nM and 14 nM, respectively. Afatinib (BIBW 2992) 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.
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Source | Am J Cancer Res (2015). Figure 3. BIBW2992 |
| Method | Western Blot | |
| Cell Lines | HKESC-2 and EC-1 cell lines | |
| Concentrations | 0.1 μM | |
| Incubation Time | 24 h | |
| Results | In HKESC-2 and EC-1 cell lines, afatinib could suppress AKT phosphorylation in a dose and time dependent manner, in which the phosphorylation was almost completely abrogated when the cells were treated with concentrations around their corresponding IC50 (HKESC-2: 0.1 μM, EC-1: 1 μM) for 24 hours (Figure 3). |
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Source | Am J Cancer Res (2015). Figure 1. BIBW2992 |
| Method | ELISA | |
| Cell Lines | ESCC cell lines | |
| Concentrations | 0.1 μM | |
| Incubation Time | 48 and 72 h | |
| Results | All 5 ESCC cell lines were sensitive to afatinib, in which over 95% of growth inhibition was observed after 48 and 72 hours of treatment (Figure 1B). |
| Cell Experiment | |
|---|---|
| Cell lines | NSCLC cells H1666, H3255 and NCI-H1975 |
| Preparation method | Growth inhibition of lung cancer cell lines by BIBW2992 and other EGFR and/or HER2 inhibitors (a) Sensitivity of NSCLC cell lines that express EGFR WT, Exon 19 Del, L858R/ T790M and HER2 INS776V to BIBW2992 and erlotinib. Dose-dependent growth inhibition was determined by MTS assay. Only HCC827 cells are sensitive to erlotinib whereas NCIH1781 and NCI-H1975 cells are also sensitive to BIBW2992. Points, average of two independent experiments, each done in triplicate; bars, s.d. *A549 cells harbor a Kras G12S mutation. See also in Supplementary Table 4. (b) Inhibition of anchorage independent cell proliferation of various lung cancer cell lines treated with BIBW2992, lapatinib, canertinib, gefitinib or erlotinib. The IC50 values were determined as described. |
| Concentrations | 0~10µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | A431 cells mouse bearing tumor xenograft model |
| Formulation | 0.5% methyl cellulose-0.4% polysorbate-80 (Tween 80) |
| Dosages | 20 ml/kg body weight once daily |
| Administration | oral gavage |
| Molecular Weight | 485.94 |
| Formula | C24H25ClFN5O3 |
| CAS Number | 850140-72-6 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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