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Afatinib

Chemical Structure : Afatinib

CAS No.: 850140-72-6

Afatinib (BIBW-2992;BIBW2992;BIBW 2992)

Catalog No.: PC-42499Not For Human Use, Lab Use Only.

Afatinib (BIBW 2992) is an irreversible, dual EGFR/HER2 inhibitor with IC50 of 0.5/0.4/10/14 nM for wt EGFR/EGFR L858R/EGFR L858R+T790M/HER2 respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Afatinib (BIBW 2992) is an irreversible, dual EGFR/HER2 inhibitor with IC50 of 0.5/0.4/10/14 nM for wt EGFR/EGFR L858R/EGFR L858R+T790M/HER2 respectively.
Afatinib (BIBW 2992) shows high selectivity over HGFR, c-Src, β-InsRK,VEGFR2.
Afatinib (BIBW 2992) suppresses transformation in isogenic cell-based assays, inhibits survival of cancer cell lines and induces tumor regression in xenograft and transgenic lung cancer models.

Physicochemical Properties

M.Wt 485.9384
Formula C24H25ClFN5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, (2E)-

References

1. Li D, et al. Oncogene. 2008 Aug 7;27(34):4702-11.

2. Perera SA, et al. Proc Natl Acad Sci U S A. 2009 Jan 13;106(2):474-9.

3. Takezawa K, et al. Mol Cancer Ther. 2010 Jun;9(6):1647-56.

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