Afatinib dimaleate

Tocris Bioscience | Catalog # 6812

Potent dual specificity EGFR/HER2 inhibitor; active in vivo
Tocris Bioscience

Key Product Details

Description

Potent dual specificity EGFR/HER2 inhibitor; active in vivo

Alternative Names

BIBW2992
View all EGF Receptor Inhibitors »

Product Description

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.

Product Specifications for Afatinib dimaleate

Molecular Weight

718.08

Formula

C24H25ClFN5O3.2C4H4O4

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate

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.

Solubility

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 all 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

Calculators

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 4 publications citing the usage of this product.

Product Documents for Afatinib dimaleate

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for Afatinib dimaleate

For research use only

Citations for Afatinib dimaleate

Customer Reviews for Afatinib dimaleate (1)

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  • Easy to use!
    Name: Anonymous
    Species: Mouse
    Assay Type: In Vitro
    Cell Line/Tissue: B16F0
    Verified Customer | Posted 09/17/2022
    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.
    Afatinib dimaleate 6812

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