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EphB4-IN-1
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Catalog No. T217956 Copy Product Info
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EphB4-IN-1 is a selective tyrosine kinase inhibitor of EphB4, exhibiting an IC50 value range of 0.16-0.30 μM. It binds to the ATP-binding site of EphB4 in the DFG-in conformation, creating four stable intermolecular hydrogen bonds. Additionally, EphB4-IN-1 inhibits kinases such as Src, Abl1, Lck, and EGFR and prevents the autophosphorylation of EphB4. This compound is applicable in cancer research, including studies on non-small cell lung cancer.
EphB4-IN-1
Cas No. 1394837-94-5
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | EphB4-IN-1 is a selective tyrosine kinase inhibitor of EphB4, exhibiting an IC50 value range of 0.16-0.30 μM. It binds to the ATP-binding site of EphB4 in the DFG-in conformation, creating four stable intermolecular hydrogen bonds. Additionally, EphB4-IN-1 inhibits kinases such as Src, Abl1, Lck, and EGFR and prevents the autophosphorylation of EphB4. This compound is applicable in cancer research, including studies on non-small cell lung cancer. |
| Targets & IC50 | EPHB4:016-0.3 μM |
| In vitro | EphB4-IN-1 (Compound 7) inhibits purified EphB4 kinase with an IC50 of 0.30 μM at an ATP concentration of 30 μM. In a radiolabeled ATP-based enzymatic assay using 1 μM ATP, it shows an IC50 of 0.16 μM against purified EphB4 kinase. It also inhibits Src, Abl1, Lck, and EGFR kinases with IC50 values of 0.338 μM, 0.864 μM, 1.38 μM, and 1.62 μM, respectively, but does not inhibit IGF1R, demonstrating higher affinity for EphB4 than these kinases. EphB4-IN-1 effectively inhibits EphB4 autophosphorylation in Ephrin-B2/Fc-stimulated MEF cells expressing exogenous human EphB4, with an IC50 of 0.93 μM. |
| Molecular Weight | 322.36 |
| Formula | C18H18N4O2 |
| Cas No. | 1394837-94-5 |
| Smiles | O=C1C2=C(C=3C(=NC=NC3N1C4=CC(O)=CC=C4C)N)CCCC2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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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.
Dose Conversion
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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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Related Tags: EphB4-IN-1 in vitro | EphB4-IN-1 formula | EphB4-IN-1 molecular weight
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