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Synonyms: BIBW 2992, Afatinib free base
| 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):0.4 nM, EGFR (L858R/T790M):10 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] |
| Synonyms | BIBW 2992, Afatinib free base |
| Molecular Weight | 485.94 |
| Formula | C24H25ClFN5O3 |
| Cas No. | 850140-72-6 |
| Smiles | N(C=1C2=C(C=C(O[C@H]3CCOC3)C(NC(/C=C/CN(C)C)=O)=C2)N=CN1)C4=CC(Cl)=C(F)C=C4 |
| Relative Density. | 1.380 g/cm3 |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 242 mg/mL (498 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.5 mg/mL (9.26 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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