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Art. -Nr.: HY-10654

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EphB4-IN-2

EphB4-IN-2 is a tyrosine kinase inhibitor targeting the Eph family and Src family. EphB4-IN-2 binds to the ATP-binding site of the kinase domain of EphB4, and exhibits high affinity for tyrosine kinases with threonine as the gatekeeper residue, such as Abl, Lck and Src. EphB4-IN-2 can be used in research related to tumor-associated angiogenesis.

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CAS. Nr.: 1192216-03-7
Formel: C₂₂H₁₉N₅O₄
Molecular Weight:417.42

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

EphB4-IN-2 Chemical Structure

CAS. Nr.: 1192216-03-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EPHB4

5 nM (IC₅₀)

Alle Ephrin Receptor Isoform-spezifische Produkte anzeigen :

EphB
EphA

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	IC₅₀	2.7 μM Compound: 3	Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining	[PMID: 23253074]
Hs-578T	GI₅₀	562 nM Compound: 3	Cytotoxicity against human Hs578T cells by SRB assay Cytotoxicity against human Hs578T cells by SRB assay	[PMID: 23253074]
K562	GI₅₀	309 nM Compound: 3	Cytotoxicity against human K562 cells by SRB assay Cytotoxicity against human K562 cells by SRB assay	[PMID: 23253074]
MEF	IC₅₀	130 nM Compound: 3	Inhibition of human myc-tagged full length EphB4 expressed in MEF cells assessed as inhibition of ephrinB2-Fc-induced autophosphorylation incubated for 90 mins prior to ephrinB2-Fc-induction measured after 2 hrs by sandwich ELISA Inhibition of human myc-tagged full length EphB4 expressed in MEF cells assessed as inhibition of ephrinB2-Fc-induced autophosphorylation incubated for 90 mins prior to ephrinB2-Fc-induction measured after 2 hrs by sandwich ELISA	[PMID: 23253074]
SNB-75	GI₅₀	128 nM Compound: 3	Cytotoxicity against human SNB75 cells by SRB assay Cytotoxicity against human SNB75 cells by SRB assay	[PMID: 23253074]

In Vitro

EphB4-IN-2 (compound 66) potently inhibits recombinant EphB4 kinase activity in FRET-based enzymatic assays with an IC₅₀ of 5 nM; it also inhibits this target in [γ-33P] ATP-based enzymatic assays, with an IC₅₀ of 1.6 nM. This compound exhibits potent inhibitory effects on 9 out of 10 tested recombinant Eph receptor kinases, with corresponding IC₅₀ values falling within the low nanomolar range of 1.1-15 nM, and only shows weak inhibitory activity against EphA7, with an IC₅₀ of 1118 nM.
EphB4-IN-2 (1 μM; 30 minutes) potently inhibits recombinant EphA2, EphB3, Src, Lck and Yes1 kinases, exhibits moderate activity against CSK, BTK and HER-4, and shows only very low activity against most other tested kinases^[1].
EphB4-IN-2 (1 μM) binds with high affinity to 15 kinases with small gatekeeper residues among the 49 tested recombinant kinases, and these kinases mainly belong to the Eph, Src and Abl families^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1192216-03-7
Molecular Weight 417.42
Formel C₂₂H₁₉N₅O₄
SMILES

CN(C1=C2N3C(N(C4=C(OC)C=CC=C4)C(C5=CC(O)=CC=C5C)=C3)=N1)C(NC2=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Lafleur K, et al. Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). J Med Chem. 2009;52(20):6433-6446. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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EphB4-IN-2

Alle Ephrin Receptor Isoform-spezifische Produkte anzeigen