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BIBW2992 (Afatinib) | EGFR, Her2 inhibitor

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Catalog #:

Product Description

BIBW2992 (Afatinib) is an orally-available, aminoquinazoline-acrylamide-based inhibitor with IC50 potency for EGFRwt, EGFR(L858R), EGFR(L858R/T790M), and HER2 at 0.5, 0.4, 10, and 14 nM, respectively. [1] Via its crotonamide functional group, BIBW2992 targets the ErbB family in an irreversible manner, providing a sustained, selective, and covalent inhibition that has been shown to be effective toward erlotinib-resistant tumors. [2]

In cellular assays, BIBW2992 inhibits phosphorylation of EGFR wild type (A431), EGFR (NCI-H1975), and HER2 (BT474) at EC50s of 8, 49, and 75 nM, respectively. [3]

BIBW2992 displays potent growth inhibition of EGFR/HER2 expressing lung cancer cell lines H1666, H3255, and NCI1975 at IC50 values of 60, 0.7, and 99 nM, respectively. [1]

Technical information:

Chemical Formula:   C24H25ClFN5O3
CAS #:   439081-18-2
Molecular Weight:   485.94
Purity:   > 98%
Appearance:   Off White
Chemical Name:   (S,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   BIBW2992, BIBW-2992, Afatinib, Tovok, Tomtovok

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. Li et al., BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene, 2008, 27(34), 4702-4711. Pubmed ID: 18408761
2. Boehringer Ingelheim backgrounder (BIBW2992, Afatinib), May, 2012.
3. Solca et al., Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker. J. Pharmacol. Exp. Ther. 2012, 343(2), 342-350. Pubmed ID: 22888144

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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