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Ephrin Receptor

Eph receptors (Ephs, after erythropoietin-producing human hepatocellular receptors) are a group of receptors that are activated in response to binding with Eph receptor-interacting proteins (Ephrins). Ephs form the largest known subfamily of receptor tyrosine kinases (RTKs). Both Eph receptors and their corresponding ephrin ligands are membrane-bound proteins that require direct cell-cell interactions for Eph receptor activation. Eph/ephrin signaling has been implicated in the regulation of a host of processes critical to embryonic development including axon guidance, formation of tissue boundaries, cell migration, and segmentation. Additionally, Eph/ephrin signaling has recently been identified to play a critical role in the maintenance of several processes during adulthood including long-term potentiation, angiogenesis, and stem cell differentiation and cancer.

  • AWL-II-38.3
    T385111135205-94-5
    AWL-II-38.3 is a highly effective inhibitor of EphA3, a receptor for ephrin-A. It demonstrates potent kinase inhibitory activity against EphA3 and does not show significant cellular activity against Src-family kinases or b-raf [1] [2].
    • $74
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  • Tesevatinib
    TQ0166781613-23-8
    Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).
    • $109
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  • UniPR505
    T733682938227-14-4In house
    UniPR505 is a potent EphA2 antagonist (IC50: 0.95 µM), a novel 3α-carbamoyloxy derivative with antiangiogenic properties.
    • $518
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  • KYL acetate(676657-00-4 free base)
    TP1895L1
    KYL acetate is an EphA4 receptor tyrosine kinase inhibitor (Kd = 0.8 μM); inhibits EphA4-EphrinA5 interactions (IC50 = 6.34 μM). Prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. Exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively). Neuroprotective.
    • $133
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  • AZ12672857
    T9650945396-55-4In house
    AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. AZ12672857 inhibits cell proliferation of Src transfected 3T3 cells with IC50 of 2 nM and autophosphorylation of EphB4 in transfected CHO-K1 cells with IC50 of 9 nM.
    • $64
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  • Dasatinib monohydrate
    T1448L863127-77-9
    Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.
    • $33
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    TargetMol | Citations Cited
  • Sitravatinib
    T43491123837-84-2
    Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.
    • $47
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    TargetMol | Citations Cited
  • UniPR1447
    T808971809170-68-0
    UniPR1447 is a dual antagonist for both EphA2 and EphB2 receptors, exhibiting an IC50 value of 6.6 μM against EphA2-ephrin-A1 binding [1].
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  • UniPR1449
    T80896
    UniPR1449 is an EphA2 receptor antagonist with a KD of 3.8±2.4 μM, which is significant in cancer pathophysiology [1].
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  • Eph inhibitor 2
    T5451861249-59-4
    Eph inhibitor 2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.
    • $87
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  • Tivozanib
    T2456475108-18-0
    Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.
    • $34
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  • ALW-II-49-7
    T677361135219-23-6
    ALW-II-49-7 is a selective and potent inhibitor of EphB2 kinase with an EC50 value of 40 nM in cell.
    • $65
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  • 123C4
    TP15612034159-30-1
    123C4 is a novel, potent, and selective agonist of the tyrosine kinase EphA4 receptor.
    • $147
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  • ALW-II-41-27
    T43441186206-79-0
    ALW-II-41-27 (Eph receptor tyrosine kinase inhibitor), an Eph receptor tyrosine kinase inhibitor, is used for cancer therapy.
    • $63
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  • JI-101
    T3476900573-88-8
    JI-101 (CGI-1842) is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4).
    • $31
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  • NVP-BHG712
    T6348940310-85-0
    NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
    • $31
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  • NVP-BHG712 isomer
    T194872245892-85-5
    NVP-BHG712 isomer shows conserved non-bonded binding to EPHA2 and EPHB4.
    • $36
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  • Ehp-inhibitor-2
    T5452861249-77-6
    Ehp-inhibitor-2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.
    • $39
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