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Tovok; BIBW-2992

Chemical

C24H25ClFN5O3

486.0

439081-18-2

≥95%

Solid.

Soluble in DMSO or ethanol.

Manufactured by SynKinase.

Target: EGFR - HER2 | Kinase Group: RTK | Substrate: TyrosineClick here for Original Manufacturer Product DatasheetOur product description may differ slightly from the original manufacturers product datasheet.

ULXXDDBFHOBEHA-CWDCEQMOSA-N

AMBIENT

+4°C

-20°C

Stable for at least 2 years after receipt when stored at -20°C.

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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

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)

Irreversible protein kinase inhibitors: balancing the benefits and risks: T. Barf & A. Kaptein; J. Med. Chem. 55, 6243 (2012)

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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