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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- No. CAS: 1192216-03-7
- Fòrmula: C22H19N5O4
- Peso molecular:417.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
EPHB4 5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | IC50 |
2.7 μM
Compound: 3
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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
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[PMID: 23253074] |
| Hs-578T | GI50 |
562 nM
Compound: 3
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Cytotoxicity against human Hs578T cells by SRB assay
Cytotoxicity against human Hs578T cells by SRB assay
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[PMID: 23253074] |
| K562 | GI50 |
309 nM
Compound: 3
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Cytotoxicity against human K562 cells by SRB assay
Cytotoxicity against human K562 cells by SRB assay
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[PMID: 23253074] |
| MEF | IC50 |
130 nM
Compound: 3
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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
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[PMID: 23253074] |
| SNB-75 | GI50 |
128 nM
Compound: 3
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Cytotoxicity against human SNB75 cells by SRB assay
Cytotoxicity against human SNB75 cells by SRB assay
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[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
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No. CAS 1192216-03-7
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Peso molecular 417.42
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Fòrmula C22H19N5O4
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SMILES
CN(C1=C2N3C(N(C4=C(OC)C=CC=C4)C(C5=CC(O)=CC=C5C)=C3)=N1)C(NC2=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EphB4-IN-2 Related Classifications
HY-10654 Related Classifications
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