Afatinib dimaleate

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Cat.No. 6812 - Afatinib dimaleate | C24H25ClFN5O3.2C4H4O4 | CAS No. 850140-73-7
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)
Literature (4)

Biological Activity

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.

Technical Data

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

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

Preparing Stock Solutions

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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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

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