VEGFR
VEGF is one of the key regulators of angiogenesis, vasculogenesis, and developmental hematopoiesis. It is a mitogen and survival factor for vascular endothelial cells while also promoting vascular endothelial cell and monocyte motility[1]. Binding of growth factors to the ectodomain of their transmembrane receptors leads to receptor dimerization, protein kinase activation, trans-autophosphorylation, and initiation of signaling pathways. The VEGF family of receptors (RTK class IV, VEGF receptor family) consists of three protein–tyrosine kinases (VEGFR1, VEGFR2, and VEGFR3) and two non-protein kinase co-receptors (neuropilin-1 and 2)[2]. Targeting VEGF receptors proved to be a successful therapeutic approach for disorders with non-physiologic angiogenesis including age-related macular degeneration of the eye, diabetic retinopathy, rheumatoid arthritis, tumor growth and metastasis1.
[1] Vascular endothelial growth factor (VEGF) signaling during tumor progression. A comprehensive review of the discovery of the VEGF family of ligands and receptors. R. Roskoski Jr. Crit. Rev. Oncol. Hematol. 2007, 62, 179–213.
[2] VEGF receptor protein–tyrosine kinases: Structure and regulation. Mini Review. R. Roskoski Jr. Biochem. Biophys. Res. Com. 2008, 375, 287–291.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 1638 | ABT 869 | PDGFR, c-KIT and VEGFR tyrosine kinase inhibitor | €85.00 | |
| 1653 | AEE 788 | EGFR, ErbB2 and VEGFR tyrosine kinase inhibitor | €95.00 | |
| 1414 | AG 013736 | PDGFR,c-KIT and VEGFR tyrosine kinase inhibitor | €65.00 | |
| 1768 | AMG 706 | Multiple receptor tyrosine kinase inhibitor | €105.00 | |
| 2849 | Apatinib | Inhibitor of VEGFR2 | €125.00 | |
| 1850 | BMS 540215 | Inhibitor of VEGFR (subtype 2 and 3 selective) | €110.00 | |
| 2837 | BMS 605541 | Potent, selective, orally active, and ATP-competitive VEGFR2 inhibitor | Recently added | €90.00 |
| 1864 | Brivanib alaninate | Prodrug of BMS 540215; Inhibitor of VEGF | €105.00 | |
| 1819 | Cabozantinib S-malate | Inhibitor of multiple receptor tyrosine kinases, specifically MET and VEGFR2 | €85.00 | |
| 1461 | Cediranib | VEGFR tyrosine kinase inhibitor | €70.00 | |
| 1662 | CP 547632 | VEGFR2 tyrosine kinase inhibitor | €105.00 | |
| 1942 | E 3810 dihydrochloride | Dual VEGFR/FGFR tyrosine kinase inhibitor | €95.00 | |
| 1959 | Golvatinib | Potent and orally available inhibitor of c-MET (HGFR) and VEGFR2 | €95.00 | |
| 1420 | GW 786034 | PDGFR, c-KIT and VEGFR tyrosine kinase inhibitor | €70.00 | |
| 1963 | LY 573636 | Anti-tumor agent; causes growth arrest and apoptosis | €95.00 | |