Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Afatinib [850140-72-6]

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Cat# NB-64-10870-5mg

Size : 5mg

Marca : Neo Biotech

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Afatinib

(Synonyms: BIBW 2992, Afatinib free base) Copy Product Info

Synonyms: BIBW 2992, Afatinib free base

Catalog No. T21312 Copy Product Info

Purity: 99.90%

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.

Cas No. 850140-72-6

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.90%

Color:White

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):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

Chemical Properties

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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.0579 mL	10.2893 mL	20.5787 mL	102.8934 mL
5 mM	0.4116 mL	2.0579 mL	4.1157 mL	20.5787 mL
10 mM	0.2058 mL	1.0289 mL	2.0579 mL	10.2893 mL
20 mM	0.1029 mL	0.5145 mL	1.0289 mL	5.1447 mL
50 mM	0.0412 mL	0.2058 mL	0.4116 mL	2.0579 mL
100 mM	0.0206 mL	0.1029 mL	0.2058 mL	1.0289 mL

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.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

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.

Stock Solution Preparation:

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.

Preparation of the In Vivo Formulation:

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.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

SLMT-1NIH-3T3 cellsNCI-H1975HKESC-2HKESC-1HER2H3255H1666ESCCEGFREC-1c-Met/HGFRBIBW-2992BIBW2992AutophagyAfatinibA431

Related Tags: Afatinib chemical structure | Afatinib in vivo | Afatinib in vitro | Afatinib formula | Afatinib molecular weight