A selective dual inhibitor of EGFR/HER2
Related Products
Alternative(s)
21567Afatinib (maleate)
Labeled Version(s)
22552Afatinib-d6
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Afatinib

Item No. 11492

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
CAS Number
850140-72-6
Synonyms
  • BIBW 2992
Molecular Formula
C24H25ClFN5O3
Formula Weight
485.9
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 11 mg/ml
λmax
254, 343 nm
SMILES
N(C=1C2=C(C=C(O[C@H]3CCOC3)C(NC(/C=C/CN(C)C)=O)=C2)N=CN1)C4=CC(Cl)=C(F)C=C4
InChi Code
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
InChi Key
ULXXDDBFHOBEHA-CWDCEQMOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    Afatinib is an irreversible inhibitor of epidermal growth factor receptor (EGFR) and ErbB2 (IC50s = 0.5 and 14 nM, respectively).1 It increases the cytotoxicity of adriamycin in a concentration-dependent manner in multidrug-resistant A549T lung cancer cells overexpressing P-glycoprotein.2 Afatinib (20 mg/kg) reduces tumor growth in ErbB2-amplified NCI-N87 and NUGC4 gastric cancer mouse xenograft models.3 Formulations containing afatinib have been used in the treatment of non-small cell lung cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Eskens, F.A.L.M., Mom, C.H., Planting, A.S.T., et al. A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours. Br. J. Cancer 98(1), 80-85 (2008).

    2. Zhang, Y., Wang, C.-Y., Duan, Y.-J., et al. Afatinib decreases P-glycoprotein expression to promote adriamycin toxicity of A549T cells. J. Cell. Biochem. 119(1), 414-423 (2018).

    3. Yoshioka, T., Shien, K., Namba, K., et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 109(4), 1166-1176 (2018).