Afatinib dimaleate

Irreversible blocker of three members of the ErbB family (ErbB1, ErbB2/HER2, and ErbB4) with IC50 in nanomolar range. The compound binds covalently to cysteine 797 residue in HER2 and blocks downstream cellular signalling, inhibits cellular growth and promotes apoptosis. Afatinib has been used for the treatment of tyrosine kinase inhibitor-resistant tumours with mutations in ErbB genes, especially for deletions in exon 19 and single nucleotide substitutions in exon 21. It has been used for treatment of non-small cell lung cancer (NSCLC), breast cancer, pancreatic cancer, colorectal cancer, etc.

Technical Data

CAS号: 850140-73-7
产品编码: BA162012
MDL号: MFCD25974239
分子式: C24H25ClFN5O3·C8H8O8
分子量: 718.08


  • Li D et al (2008). BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 27(34):4702-11.
  • Hirsh V (2011). Afatinib (BIBW 2992) development in non-small-cell lung cancer. Future Oncol. 7(7):817-25.
  • Pan Y et al (2012). SKLB1206, a novel orally available multikinase inhibitor targeting EGFR activating and T790M mutants, ErbB2, ErbB4, and VEGFR2, displays potent antitumor activity both in vitro and in vivo. Mol Cancer Ther 11(4):952-62.
  • Solca et al., 2012. Target binding properties and cellular activity of afatinib (BBW 2992), an irreversible ErbB family blocker. J Pharmacol Exp Ther 343:342–350.
  • Modjtahedi et al., 2014. A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer. Naunyn Schmiedebergs Arch Pharmacol 387(6):505-21.



Further Information


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