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Product Details
Synonyms Tovok; BIBW-2992
Product Type Chemical
Formula C24H25ClFN5O3
MW 486.0
CAS 439081-18-2
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO or ethanol.
Declaration Manufactured by SynKinase.
Other Product Data Target: EGFR - HER2 | Kinase Group: RTK | Substrate: Tyrosine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
Afatinib is an irreversible kinase inhibitor and binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) to inhibit tyrosine kinase autophosphorylation. This results in a downregulation of ErbB signaling and subsequent inhibition of proliferation of cell lines expressing wild-type EGFR, selected EGFR exon 19 deletion mutations, or exon 21 L858R mutations. It also inhibited in vitro proliferation of cell lines overexpressing HER2. Overall, tumor growth was inhibited by Afatinib very effectively with low nanomolar IC(50) values ranging from approximately 6nM to below 500nM.
Product References
  1. Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors: K.L. Stevens, et al.; Bioorg. Med. Chem. Lett. 19, 21 (2009)
  2. Irreversible protein kinase inhibitors: balancing the benefits and risks: T. Barf & A. Kaptein; J. Med. Chem. 55, 6243 (2012)
  3. Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR): R.A. Ward, et al.; J. Med. Chem. 56, 7025 (2013)
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