Afatinib dimaleate

Product Description

Afatinib dimaleate is a potent dual specificity EGFR/HER2 inhibitor (IC₅₀ are 0.4, 0.5, 10, 14, 1 nM for EGFR^L858R, EGFR^wt, 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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

• Li BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 2008 PMID: 18408761