Afatinib dimaleate

Name: Afatinib dimaleate
Brand: Tocris Bioscience
SKU: 6812
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 6812

(1)

Citations (3)

COA / SDS

Potent dual specificity EGFR/HER2 inhibitor; active in vivo

Key Product Details

Description:	Potent dual specificity EGFR/HER2 inhibitor; active in vivo
Alternative Names:	BIBW2992
Chemical Name:	(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide dimaleate
Purity:	≥98% (HPLC)
Molecular Weight:	718.08

View Full Technical Details for Afatinib dimaleate

Technical Data
Citations / Reviews (1)

Biological Activity for Afatinib dimaleate

Afatinib dimaleate is a potent dual specificity EGFR/HER2 inhibitor (IC₅₀ are 0.4, 0.5, 10, 14, 1 nM for EGFR^L858R, EGFR^wt, 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.

Compound Libraries for Afatinib dimaleate

Afatinib dimaleate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Afatinib dimaleate

M. Wt	718.08
Formula	C₂₄H₂₅ClFN₅O₃.2C₄H₄O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Afatinib dimaleate

	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 will affect the solvent volumes required to prepare stock solutions.

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

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Reconstitution Calculator

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References for Afatinib dimaleate

References are publications that support the biological activity of the product.

Li BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 2008 PMID: 18408761