ephrinreceptor

UniPR505 is a potent EphA2 antagonist (IC50: 0.95 µM), a novel 3α-carbamoyloxy derivative with antiangiogenic properties.

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.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

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].

UniPR1449 is an EphA2 receptor antagonist with a KD of 3.8±2.4 μM, which is significant in cancer pathophysiology [1].

123C4 is a potent, selective, and competitive agonist of the receptor tyrosine kinase EPHA4 (Ki=0.65 μM)[1].

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.

ALW-II-41-27 (Eph receptor tyrosine kinase inhibitor), an Eph receptor tyrosine kinase inhibitor, is used for cancer therapy.

ALW-II-49-7 is a selective and potent inhibitor of EphB2 kinase, with an EC50 value of 40 nM in cell.

UniPR500, a derivative of UniPR129, is a competitive antagonist for the EphA2 receptor, with a Ki of 0.78 μM. It reduces the binding of biotinylated Ephrin-A1 to EphA2 in a dose-dependent manner, exhibiting an IC50 value of 1.1 μM.

PKMYT1-IN-8 (Compound 137) is an inhibitor of PKMYT1, with an IC50 value of 9 nM. It also inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2, exhibiting IC50 values of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. Additionally, PKMYT1-IN-8 suppresses the proliferation of cancer cells OVCAR3 with a GI50 of 2.02 μM.

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.

Eph inhibitor 2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.

AWL-II-38.3 is a highly potent EphA3 inhibitor with potent kinase inhibitory activity against EphA3 but no significant cellular activity against Src family kinases or b-raf.

Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.

Ehp-inhibitor-2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.

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.

Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ​​of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.

NVP-BHG712 isomer shows conserved non-bonded binding to EPHA2 and EPHB4.

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).