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^[1].

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.

417.42

C₂₂H₁₉N₅O₄

1192216-03-7

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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• [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]