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^[1].

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.

322.36

C₁₈H₁₈N₄O₂

1394837-94-5

O=C1C2=C(CCCC2)C3=C(N1C4=CC(O)=CC=C4C)N=CN=C3N

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• [1]. Zhao H, et al. Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics. ACS Med Chem Lett. 2012;3(10):834-838. Published 2012 Aug 23.  [Content Brief]