Ephrin-Receptor-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html Ephrin HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html ReceptorThe Eph receptor tyrosine kinase (RTK) family comprises the largest group of surface receptors and are cate

2、gorized into EphA orEphB subclasses based on sequence homology and preferential binding to their ephrin-A and ephrin-B ligands, respectively.In humans, nine EphA (EphA1-8,10) and five EphB (EphB1-4,6) receptors are expressed, along with five ephrin-A and three ephrin-Bligands. Unlike most RTKs, Eph

3、receptors interact with ligands that are often membrane-bound, allowing both “forward signaling” inthe receptor-bound cell and “reverse signaling” in the ephrin-bound cell. In addition to “forward signaling,” Eph receptors cansignal in the absence of ligand binding and kinase activation through cros

4、s-talk with other RTKs, such as HER2.Eph receptor tyrosine kinases and their ligands, the ephrins, play key roles in the regulation of migration and cell adhesion duringdevelopment, thereby influencing cell fate, morphogenesis and organogenesis. By now, many Eph receptors and ephrins have alsobeen f

5、ound to play important roles in the progression of cancer. Therefore, the Eph/ephrin system is considered a promisingtherapeutic target.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html Ephrin HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html HYPERLINK https:/www.Med

6、ChemE/Targets/Ephrin Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html Agonists

7、 HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Ephrin Receptor.html Antagonists HYPERLINK https:/www.MedChemE/123c4.html 123C4Cat

8、. No.: HY-P0177 HYPERLINK https:/www.MedChemE/ALW-II-41-27.html ALW-II-41-27(Eph receptor tyrosine kinase inhibitor) Cat. No.: HY-18007123C4 is a potent, selective and competitiveagonist of the receptor tyrosine kinase EPHA4,with a K value of 0.65 M.iALW-II-41-27 is a Eph family tyrosine kinaseinhib

9、itor with an IC of 11 nM for Eph2.50Purity: 99.05%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 99.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/ehp-inhibitor-2.html Eph HYPERLINK https:/www.MedChemE/ehp-inhibitor-2

10、.html HYPERLINK https:/www.MedChemE/ehp-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/ehp-inhibitor-2.html HYPERLINK https:/www.MedChemE/ehp-inhibitor-2.html 2 HYPERLINK https:/www.MedChemE/ehp-inhibitor-2.html HYPERLINK https:/www.MedChemE/JI-101.html JI-101Cat. No.: HY-131005 Cat. No.:

11、HY-16265Eph inhibitor 2 (Example 35) is a Eph familytyrosine kinase inhibitor.JI-101 is an orally available multi-kinaseinhibitor of VEGFR2, PDGFR and EphB4 withpotent anti-cancer activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.43%Clinical Data: Phase 2Size: 5 mg

12、, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/kyl-peptide.html KYL HYPERLINK https:/www.MedChemE/kyl-peptide.html HYPERLINK https:/www.MedChemE/kyl-peptide.html peptide HYPERLINK https:/www.MedChemE/kyl-peptide.html HYPERLINK https:/www.MedChemE/ml786-dihydrochloride.html ML786 HYPERLINK http

13、s:/www.MedChemE/ml786-dihydrochloride.html HYPERLINK https:/www.MedChemE/ml786-dihydrochloride.html dihydrochlorideCat. No.: HY-P2264 Cat. No.: HY-14979AKYL peptide, an antagonistic peptide, selectivelytargets EphA4 receptor. KYL peptide binds to theligand-binding domain of EphA4, effectivelyallevia

14、tes A-induced synaptic dysfunction andsynaptic plasticity defects in AD mice.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgML786 dihydrochloride is a potent and orallybioavailable Raf inhibitor, with IC s of 2.1,504.2, and 2.5 nM for V600EB-Raf, wt B-Raf,and C-Raf, respectively. M

15、L786 dihydrochloridealso inhibits Abl-1, DDR2, EPHA2, KDR, and RET(IC =98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/nvp-bhg712.html NVP-BHG712 HYPERLINK https:/www.MedChemE/nvp-bhg712.html HYPERLINK https:/www.MedChemE/nvp-bhg712-isomer.html NVP-BHG712 HYPE

16、RLINK https:/www.MedChemE/nvp-bhg712-isomer.html HYPERLINK https:/www.MedChemE/nvp-bhg712-isomer.html isomer(BHG712) Cat. No.: HY-13258ACat. No.: HY-13258NVP-BHG712 is an oral active EphB4 kinaseautophosphorylation inhibitor, with IC values of503.3 nM and 3.0 nM for EphA2 and EphB4,respectively.NVP-

17、BHG712 isomer, a regioisomer of NVP-BHG712,shows conserved non-bonded binding to EPHA2 andEPHB4.Purity: 99.78%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.46%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK h

18、ttps:/www.MedChemE/XL-647.html Tesevatinib HYPERLINK https:/www.MedChemE/XL-647.html HYPERLINK https:/www.MedChemE/unipr129.html UniPR129(XL-647; EXEL-7647; KD-019) Cat. No.: HY-13314Cat. No.: HY-123607Tesevatinib (XL-647; EXEL-7647; KD-019) is anorally available, multi-target tyrosine kinaseinhibitor; inhibits EGFR, ErbB2, KDR, Flt4 andEphB4 kinase with IC s of 0.3,