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Afatinib dimaleate

An inhibitor of EGFR and HER2
Catalog #: B3072
SKU-Size Size Price Qty
B3072-50 50 mg
B3072-250 250 mg
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Product Details

Alternate Name Gilotrif; (2E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(((3S)-tetrahydrofuran-3-yl)oxy)quinazolin- 6-yl)-4-(dimethylamino)but-2-enamide bis(hydrogen (2Z)-but-2-enedioate); (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate; (E)-4-Dimethylamino-But-2-Enoic Acid-(4-(3-Chloro-4-Fluoro-Phenylamino)-7-((S)-Tetra-Hydrofuran-3-Yloxy)-Quinazolin-6Yl)-Amide Dimaleate; BIBW 2992MA2; Tovok
Appearance White to off-white powder
CAS # 850140-73-7
Molecular Formula C₃₂H₃₃ClFN₅O₁₁
Molecular Weight 718.08
Purity ≥95%
Solubility ~ 50 mg/ml in water
InChi InChI=1S/C24H25ClFN5O3.2C4H4O4/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;2*5-3(6)1-2-4(7)8/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29);2*1-2H,(H,5,6)(H,7,8)/b4-3+;2*2-1-/t16-;;/m0../s1
PubChem CID 15606394
MDL Number MFCD25974239
Handling Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Storage Conditions -20°C
Shipping Conditions RT
USAGE For Research Use Only! Not For Use in Humans.


Afatinib is an irreversible dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinase. It shows IC₅₀ values of 0.5 nM and 14 nM for EGFR kinase and HER2 kinase respectively. It inhibits EGF-induced EGFR phosphorylation and cellular proliferation in cell lines such as EGFR-overexpressing and HER2-expressing cell lines A431, NIH-3T3-HER2, NCI-N87 and BT-474. It causes tumour regression in mice carrying EGFR-overexpressing and HER2-expressing A431 xenografts, EGFR-overexpressing and HER2-expressing MDA-MB-453 xenografts, NCI-N87 gastric and SKOV-3 ovarian models.

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