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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.
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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||14.36||20 with gentle warming|
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|
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.
Keywords: Afatinib dimaleate, Afatinib dimaleate supplier, BIBW2992, dual, specificity, EGFR, HER2, inhibitors, inhibits, potent, 6812, Tocris Bioscience
Citations are publications that use Tocris products.
Currently there are no citations for Afatinib dimaleate. Do you know of a great paper that uses Afatinib dimaleate from Tocris? Please let us know.
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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.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.