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Submit ReviewAfatinib dimaleate
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)
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 |
| InChI Key | USNRYVNRPYXCSP-JUGPPOIOSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
Citations for Afatinib dimaleate
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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.
Literature in this Area
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