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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V69467 | ENMD-2076 Tartrate | 1453868-32-0 | ENMD-2076 Tartrate is a multi-target kinase inhibitor that can suppress Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, and PDGFRα with IC50s of 1.86, 14, 58.2, 15.9, 92.7, and 70.8, respectively. |
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V69639 | EVT801 | 1412453-70-3 | EVT801 is an orally bioactive and selective VEGFR-3 inhibitor (IC50=11 nM) with anti-tumor effects. |
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V69604 | Faricimab (RG7716) | 1607793-29-2 | Faricimab is a bispecific antibody targeting angiopoietin-2 and vascular endothelial growth factor-A (VEGF-A). |
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V69640 | hVEGF-IN-2 | 186610-88-8 | hVEGF-IN-2 (compound 19) is a selective VEGF (Flk-1) receptor tyrosine kinase inhibitor (antagonist) with IC50 of 2.5 μM. |
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V69611 | Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) | 1024603-92-6 | Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is a humanized anti-VEGFR-1 IgG1 monoclonal antibody (mAb). |
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V51582 | Isolinderalactone | 957-66-4 | Isolactone suppresses the growth and angiogenic activity of human apoptotic cell blastoma by inhibiting VEGFR2 activation in endothelial cells. |
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V69614 | Ivonescimab (AK112) | 2428381-53-5 | Ivonescimab (AK112) is a PD-1/VEGF bispecific antibody. |
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V69633 | KLTWQELYQLKYKGI | 917760-16-8 | KLTWQELYQLKYKGI (QK) is a VEGF mimetic peptide that binds to VEGF receptors and competes with VEGF. |
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V69610 | Olinvacimab (TTAC-0001) | 2095504-49-5 | Olinvacimab (TTAC-0001) is a human anti-VEGFR2 monoclonal antibody (mAb). |
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V69631 | Parsatuzumab (Anti-EGFL7; RG 7414) | 1312797-14-0 | Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody (mAb) that binds to EGFL7 as an immunomodulator. |
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V69612 | Pegaptanib sodium (EYE001; NX1838) | 222716-86-1 | Pegaptanib sodium is an RNA aptamer targeting vascular endothelial growth factor (VEGF)-165. |
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V69618 | Protein LMWP | 121052-30-0 | Protein LMWP is a cell-penetrable peptide with vascular endothelial growth factor (VEGF) inhibitory activity. |
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V69642 | Pulocimab | 2428381-49-9 | Pulocimab is an anti-VEGFR2 monoclonal antibody (mAb). |
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V69606 | Ranibizumab (ranibizumab; RG-6321) | 347396-82-1 | Ranibizumab (RG-6321) is a humanized anti-VEGF monoclonal antibody (mAb) fragment that recognizes all VEGF-A isoforms (VEGF110, VEGF121, and VEGF165). |
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V69641 | Rhamnazin | 552-54-5 | Rhamnazin is an orally bioactive VEGFR2 signaling pathway inhibitor (antagonist) with IC50 of 4.68 μM for VEGFR2 kinase. |
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V69630 | Sotiburafusp alfa (Sotiburafusp alpha) | 2637466-37-4 | Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment fused to humanized IgG1-kappa anti-PD-L1 heavy chain variant L352>A through the peptide linker 101GGSGSGGSGGSGGS115. |
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V69625 | Sozinibercept (OPT 302; VGX-300) | 2568358-31-4 | Sozinibercept (OPT 302; VGX-300) is a soluble form of VEGFR-3, which can effectively inhibit the activity of the angiogenic factor VEGF-C/D, inhibit angiogenesis and vascular leakage. |
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V69638 | Suvemcitug | 1610010-57-5 | Suvemcitug is an IgG1κ antibody targeting VEGF developed from African hare (Oryctolagus cuniculus). |
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V69616 | Tarcocimab (OG1953) | 2408661-40-3 | Tarcocimab (OG1953) is a humanized anti-VEGFA monoclonal antibody (mAb) (IgG1 type). |
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V69494 | TRKII-IN-1 | 2904690-41-9 | TRK II-IN-1 is a potent type II TRK inhibitor (antagonist) with IC50s of 3.3, 6.4, 4.3 and 9.4 nM against TRKA/B/C and TRKAG667C, respectively. |
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