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Afatinib

Afatinib
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Purity:99.9%
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Afatinib

Catalog No. T21312Cas No. 850140-72-6
Afatinib (BIBW 2992) is an irreversible inhibitor of the EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M, and HER2) with IC50s of 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$30In Stock
10 mg$47In Stock
25 mg$78In Stock
50 mg$117In Stock
100 mg$147In Stock
200 mg$187In Stock
500 mg$316In Stock
1 mL x 10 mM (in DMSO)$48In Stock
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Product Introduction

Bioactivity
Description
Afatinib (BIBW 2992) is an irreversible inhibitor of the EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M, and HER2) with IC50s of 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.
Targets&IC50
EGFR:0.5 nM, EGFR (L858R/T790M):10 nM, EGFR (L858R):0.4 nM, HER2:14 nM
In vitro
METHODS: NSCLC cells NCI-H1975, NCI-H1781, HCC827 and A549 were treated with Afatinib (0.0001-10 µM) for 72 h. Cell viability was measured by MTS assay.
RESULTS: Afatinib inhibited the survival of tumor cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR. Afatinib is also effective against NSCLC cell lines expressing HER2 776insV (NCI-H1781) or EGFR E746_A750del (HCC827), but is inactive against A549 cells expressing wild-type EGFR and HER2 but also harboring the oncogenic Kras G12S point mutation. [1]
METHODS: BEAS-2B cells overexpressing wild-type or mutant HER2 were treated with Afatinib (0.1 µM) for 6 h, and target protein expression levels were measured by Western Blot.
RESULTS: Afatinib treatment inhibited the phosphorylation of HER2, EGFR and AKT. [2]
In vivo
METHODS: To assay antitumor activity in vivo, Afatinib (20 mg/kg, 1.8% HP-beta-CD + 5% acetic acid (10%) + aqueous Natrosol (0.5%)) was administered by gavage to NMRI-nu/nu mice bearing A431 xenografts once daily for 25 days.
RESULTS: Afatinib resulted in significant tumor regression with a cumulative treatment/control tumor volume ratio (T/C ratio) of 2% and downregulation of EGFR and AKT phosphorylation. [1]
AliasAfatinib free base, BIBW 2992
Chemical Properties
Molecular Weight485.94
FormulaC24H25ClFN5O3
Cas No.850140-72-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 45 mg/mL (92.6 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0579 mL10.2893 mL20.5787 mL102.8934 mL
5 mM0.4116 mL2.0579 mL4.1157 mL20.5787 mL
10 mM0.2058 mL1.0289 mL2.0579 mL10.2893 mL
20 mM0.1029 mL0.5145 mL1.0289 mL5.1447 mL
50 mM0.0412 mL0.2058 mL0.4116 mL2.0579 mL

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