Afatinib BIBW 2992 BIBW2992
Afatinib is a new generation of oral small molecule tyrosine kinase inhibitor (TKI) and is the first irreversible ErbB family blocker that acts on the entire ErbB family, including EGFR. Unlike the first-generation reversible EGFR TKI, afatinib binds irreversibly to EGFR, thereby shutting down the cancer cell signaling pathway and inhibiting tumor growth.
Product name | Afatinib (BIBW 2992) | Cas Number | 39081-18-2 |
Moculer formula | C24H25N5O3FCl | Moculer weigh | 485.944 |
Appearance and traits | white powder | Density | 1.380g/cm3 |
Melting point | 100 - 102 °C | Boiling point | 676.917 at 760 mmHg |
Flash point | 363.186°C | Refractive index | 1.668 |
Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively. Afatinib (BIBW 2992) is the second-generation potent and irreversible dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinase.
1 Local advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) gene-sensitive mutations, previously untreated with EGFR tyrosine kinase inhibitor (TKI)
2 Local advanced or metastatic squamous type of non-small cell lung cancer (NSCLC) with or without disease progression during platinum chemotherapy.
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