Three protein-tyrosine kinases (VEGFR1, VEGFR2, and VEGFR3) and two non-protein kinase co-receptors (neuropilin-1 and neuropilin-2) make up the vascular endothelial growth factor (VEGF) family of receptors. The extracellular component of VEGFRs, which has seven immunoglobulin-like domains, one transmembrane domain, and a split tyrosine kinase domain, make up typical tyrosine kinase receptors (TKRs). VEGFR-1 binds to VEGF-A, -B, and PlGF; VEGFR-2 is activated by VEGF-A, -C, -D, and -E; and VEGFR-3 is particular to VEGF-C and -D.The consensus model for ligand-induced activation of RTKs states that VEGF binds to a cognate VEGFR to cause receptor dimerization, which then triggers the activation of protein kinases, autophosphorylation of tyrosine residues in the intracellular domains of the receptor, and the initiation of signaling pathways like PI3K/AKT and MAPK/ERK1/2. VEGFR signaling is tightly controlled at many different levels, including receptor expression levels, the availability and affinities of its various ligands for binding, the presence of VEGF-binding co-receptors, non-VEGF-binding auxiliary proteins, and inactivating tyrosine phosphatases, as well as the rate of receptor cellular uptake, extent of receptor degradation, and speed of recycling.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V69573 | Vanucizumab (Anti-Human VEGFA Recombinant Antibody; RO5520985) | 1448221-05-3 | Vanucizumab is a first-in-class bispecific IgG1 monoclonal antibody (mAb) that simultaneously blocks the interaction of VEGF-A and angiopoietin-2 (Ang-2) with their receptors. |
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V69637 | Vatalanib succinate (PTK787 succinate; ZK-222584 succinate; CGP-79787 succinate) | 212142-18-2 | Vatalanib (PTK787) succinate is a potent orally bioactive VEGFR inhibitor (antagonist) with IC50s of 37 nM for KDR, Flt-1, Flk, Flt-4, c-Kit, c-Fms and PDGFR-β, respectively. |
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V69617 | VEGFR-2-IN-10 | 2760792-40-1 | VEGFR-2-IN-10 has enhanced anti-angiogenic potency (IC50 = 0.7 μM) on VEGF-induced VEGFR2 phosphorylation without cytotoxicities. |
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V69643 | VEGFR-2-IN-13 | 2839104-01-5 | VEGFR-2-IN-13 (Compound 19a) is a potent inhibitor of VEGFR-2 with IC50 of 3.4 nM. |
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V69634 | VEGFR-2-IN-37 | 298207-77-9 | VEGFR-2-IN-37 (compound 12) is an inhibitor (blocker/antagonist) of VEGFR-2. |
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V69615 | VEGFR-2-IN-5 hydrochloride | 2700435-52-3 | VEGFR-2-IN-5 HCl is a VEGFR2 inhibitor. |
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V69635 | VEGFR-2-IN-6 | 444731-47-9 | VEGFR-2-IN-6 (example 64) is an inhibitor (blocker/antagonist) of VEGFR2 (regulator of angiogenesis), information is from example 64 of patent WO 02/059110. |
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V69647 | VEGFR-3-IN-1 | 2756668-73-0 | VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor (antagonist) with IC50 of 110.4 nM. |
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V69622 | VEGFR-IN-3 | 2874264-13-6 | VEGFR-IN-3 (compound 3f) is a VEGFR inhibitor. |
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V69644 | VEGFR2-IN-1 | 2765224-55-1 | VEGFR2-IN-1 is a potent and specific VEGFR2 inhibitor (IC50=19.8 nM). |
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V69646 | VEGFR2-IN-3 | 417717-09-0 | VEGFR2-IN-3 (compound 385) is a potent VEGFR2 inhibitor. |
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V69645 | Vulinacimab (HLX-06) | 2250342-36-8 | Vulinacimab (HLX-06) is an anti-VEGFR-2 monoclonal antibody (mAb). |
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V69619 | Ziv-aflibercept | 1609655-49-3 | Ziv-aflibercept is a soluble inhibitor of vascular endothelial growth factor (VEGF). |
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