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Tyrphostin AG 528

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Catalog No. T4528Cas No. 133550-49-9
Alias Tyrphostin B66, AG 528

Tyrphostin AG 528 (Tyrphostin B66) is an inhibitor of EGFR (IC50: 4.9 μM) and ErbB2 (IC50: 2.1 μM).

Tyrphostin AG 528

Tyrphostin AG 528

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🥰Excellent
Purity: 99.64%
Catalog No. T4528Alias Tyrphostin B66, AG 528Cas No. 133550-49-9
Tyrphostin AG 528 (Tyrphostin B66) is an inhibitor of EGFR (IC50: 4.9 μM) and ErbB2 (IC50: 2.1 μM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$50In StockIn Stock
25 mg$113In StockIn Stock
50 mg$196In StockIn Stock
100 mg$298In StockIn Stock
200 mg$443In StockIn Stock
1 mL x 10 mM (in DMSO)$39In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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.
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Purity:99.64%
Appearance:Solid
Color:Yellow
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Product Introduction

Tyrphostin AG 528 AI Summary
Tyrphostin AG 528 exhibits a wide range of bioactivities, including significant inhibitory effects against key proteins involved in cancer and infectious diseases. It has shown inhibitory activity against epidermal growth factor receptor (EGFR) with an IC50 value of 12022.64 nM and against protein kinase HER-2 with an IC50 value of 4897.79 nM, suggesting its potential as a targeted therapy for cancers driven by EGFR and HER-2 signaling pathways. Additionally, it inhibits polyGAT phosphorylation, HER1 and ERBB2 autophosphorylation, and HER14 cell proliferation without EGF. In the field of infectious diseases, Tyrphostin AG 528 demonstrates antiplasmodial activity against Plasmodium falciparum with IC50 values ranging from 2511.89 nM to 15848.93 nM, indicating its potential in treating malaria. It also exhibits antiviral properties, including inhibition of the SARS-CoV-2 3CL-Pro protease by 5.9% at 20 µM and reducing SARS-CoV-2 induced cytotoxicity in VERO-6 cells by 0.53% at 10 µM for 48 hours. Furthermore, Tyrphostin AG 528 inhibits various other bioactivities such as ATPase activity of Tag, L3MBTL1, JMJD2A-Tudor Domain, GCN5L2, SV40 T antigen, and Histone Lysine Methyltransferase G9a. It also exhibits inhibitory actions on polymerases Iota and Eta, Flap endonuclease 1 (FEN1), TGF-b, WRN Helicase, Pin1, tyrosyl-DNA phosphodiesterase 1 (TDP1), and induces DNA re-replication in cancer cells. Additionally, it displays potential for antimalarial drug development by inhibiting AMA1-RON and shows activity against the SARS-CoV-2 virus. These diverse bioactivities make Tyrphostin AG 528 a promising candidate for further investigation in oncology, infectious diseases, and other therapeutic areas..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Tyrphostin AG 528 (Tyrphostin B66) is an inhibitor of EGFR (IC50: 4.9 μM) and ErbB2 (IC50: 2.1 μM).
Targets&IC50
EGFR:4.9 μM, ErbB2:2.1 μM
SynonymsTyrphostin B66, AG 528
Chemical Properties
Molecular Weight306.32
FormulaC18H14N2O3
Cas No.133550-49-9
SmilesOc1ccc(\C=C(\C#N)C(=O)N2CCc3ccccc23)cc1O
Relative Density.1.416 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (179.55 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.53 mM), Sonication is recommended.
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
1mg5mg10mg50mg
1 mM3.2646 mL16.3228 mL32.6456 mL163.2280 mL
5 mM0.6529 mL3.2646 mL6.5291 mL32.6456 mL
10 mM0.3265 mL1.6323 mL3.2646 mL16.3228 mL
20 mM0.1632 mL0.8161 mL1.6323 mL8.1614 mL
50 mM0.0653 mL0.3265 mL0.6529 mL3.2646 mL
100 mM0.0326 mL0.1632 mL0.3265 mL1.6323 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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