Afatinib dimaleate

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Description: Potent dual specificity EGFR/HER2 inhibitor; active in vivo
Alternative Names: BIBW2992
Chemical Name: (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate
Purity: ≥98% (HPLC)
Citations (1)
Reviews (1)
Literature (1)

Biological Activity for Afatinib dimaleate

Afatinib dimaleate is a potent dual specificity EGFR/HER2 inhibitor (IC50 are 0.4, 0.5, 10, 14, 1 nM for EGFRL858R, EGFRwt, EGFR L858R/T790M, ErbB2 (HER2) and ErbB4 (HER4), respectively). 100-fold more active than Gefitinib in L858R-T790M EGFR double mutant cell line. Irreversibly binds EGFR and HER2. Suppresses the kinase activity of wild-type and activated EGFR and HER2 mutants, including erlotinib-resistant isoforms. Induces tumor regression in xenograft and transgenic lung cancer models.

Compound Libraries for Afatinib dimaleate

Afatinib dimaleate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Afatinib dimaleate

M. Wt 718.08
Formula C24H25ClFN5O3.2C4H4O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 850140-73-7
PubChem ID 15606394
Smiles CN(C/C=C/C(NC1=CC2=C(N=CN=C2NC3=CC(Cl)=C(C=C3)F)C=C1O[C@H]4CCOC4)=O)C.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Afatinib dimaleate

Solvent Max Conc. mg/mL Max Conc. mM
water 14.36 20 with gentle warming
DMSO 35.9 50

Preparing Stock Solutions for Afatinib dimaleate

The following data is based on the product molecular weight 718.08. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 2.79 mL 13.93 mL 27.85 mL
2.5 mM 0.56 mL 2.79 mL 5.57 mL
5 mM 0.28 mL 1.39 mL 2.79 mL
25 mM 0.06 mL 0.28 mL 0.56 mL

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Product Datasheets for Afatinib dimaleate

References for Afatinib dimaleate

References are publications that support the biological activity of the product.

Li et al (2008) BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 27 4702 PMID: 18408761

If you know of a relevant reference for Afatinib dimaleate, please let us know.

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Keywords: Afatinib dimaleate, Afatinib dimaleate supplier, BIBW2992, dual, specificity, EGFR, HER2, inhibitors, inhibits, potent, 6812, Tocris Bioscience

1 Citation for Afatinib dimaleate

Citations are publications that use Tocris products. Selected citations for Afatinib dimaleate include:

Jürgen et al (2022) Intranasal delivery of a small-molecule ErbB inhibitor promotes recovery from acute and late-stage CNS inflammation. JCI Insight 7 PMID: 35393953

Do you know of a great paper that uses Afatinib dimaleate from Tocris? Please let us know.

Reviews for Afatinib dimaleate

Average Rating: 5 (Based on 1 Review.)

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Easy to use!.
By Anonymous on 09/17/2022
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: B16F0

I treated the mouse cell line with Afatinib, and detected the downstream EGFR tyrosine kinase activity by Western blot. The results were quantified and normalized to the vehicle-treated group.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.