Afatinib dimaleate |CAS:850140-73-7 Probechem Biochemicals

Chemical Structure : Afatinib dimaleate

CAS No.: 850140-73-7

Afatinib dimaleate (BIBW 2992MA2;BIBW-2992;BIBW2992;BIBW 2992;Afatinib)

Catalog No.: PC-42500Not For Human Use, Lab Use Only.

Afatinib (BIBW 2992) dimaleate 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.

Packing	Price	Stock
50 mg	$88	In stock
100 mg	$120	In stock
200 mg	$168	In stock
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Biological Activity

Afatinib (BIBW 2992) dimaleate 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 shows high selectivity over HGFR, c-Src, β-InsRK,VEGFR2.
Afatinib 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	718.0827
Formula	C32H33ClFN5O11
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	DMSO: ≥ 35 mg/mL
Chemical Name/SMILES	2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, (2E)-, (2Z)-2-butenedioate (1:2) (9CI)

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.

Afatinib dimaleate (BIBW 2992MA2;BIBW-2992;BIBW2992;BIBW 2992;Afatinib)

Biological Activity

Physicochemical Properties

References

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