EphB4-IN-1
EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC50 values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 1394837-94-5
- Formula: C18H18N4O2
- Molecular Weight:322.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
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Biological Activity
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EPHB4 016-0.3 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MEF | IC50 |
0.93 μM
Compound: 7
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Inhibition of human full length EphB4 expressed in MEF cells assessed as inhibition of human ephrin B2/FC chimera-stimulated receptor autophosphorylation
Inhibition of human full length EphB4 expressed in MEF cells assessed as inhibition of human ephrin B2/FC chimera-stimulated receptor autophosphorylation
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[PMID: 24900387] |
EphB4-IN-1 (Compound 7) inhibits purified EphB4 kinase with an IC50 of 0.30 μM (30 μM ATP)[1].
EphB4-IN-1 inhibits purified EphB4 kinase with an IC50 of 0.16 μM in a radioactive ATP-based enzymatic assay with 1 μM ATP[1].
EphB4-IN-1 inhibits purified Src, Abl1, Lck, and EGFR kinases with IC50 values of 0.338 μM, 0.864 μM, 1.38 μM, and 1.62 μM respectively, does not inhibit IGF1R, and has higher affinity for EphB4 than these five kinases[1].
EphB4-IN-1 inhibits EphB4 autophosphorylation in Ephrin-B2/Fc-stimulated MEF cells expressing exogenous human EphB4 with an IC50 of 0.93 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1394837-94-5
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Molecular Weight 322.36
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Formula C18H18N4O2
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SMILES
O=C1C2=C(CCCC2)C3=C(N1C4=CC(O)=CC=C4C)N=CN=C3N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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