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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V69628 | (E)-FeCP-oxindole | 884338-18-5 | (Z)-FeCP-oxindole is a selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR2) with IC50 of 200 nM. |
|
V69648 | (Rac)-SAR131675 | 1092539-44-0 | (Rac)-SAR131675 is the racemate of SAR131675. |
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V51006 | (Z)-Orantinib ((Z)-SU6668) | 210644-62-5 | (Z)-Orantinib ((Z)-SU6668) is a specific, interface-active and ATP-competitive Flk-1/KDR, PDGFRβ and FGFR1 sibling with IC50s of 2.1, 0.008 and 1.2 µM, respectively ( Z)-Olantinib is a potent anti-angiogenic and anti-tumor agent that induces regression of established tumors. |
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V69609 | 5α-Hydroxycostic acid | 132185-83-2 | 5α-Hydroxycostic acid is a eucalyptol-type sesquiterpene extracted from the herb Laggera alata. |
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V69624 | Abicipar pegol (AGN-150998; MP0112) | 1327278-94-3 | Abicipar pegol (AGN-150998, MP0112) is an anti-VEGF DARPin molecule. |
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V69629 | ABP 215 | 1438851-35-4 | ABP 215 (Bevacizumab-awwb) is a biosimilar to Bevacizumab, a humanized IgG1 monoclonal antibody (mAb) targeting VEGFA (VEGFR). |
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V69623 | Aflibercept (VEGF Trap) | 862111-32-8 | Aflibercept (VEGF Trap) is a soluble decoy VEGFR formed by fusion of the Ig domains of VEGFR1 and VEGFR2 with the Fc domain of human IgG1. |
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V69608 | Aflibercept (VEGF Trap; VEGF-TRAPR1R2; VEGF-trapR1) | 862111-32-8 | Aflibercept (VEGF Trap) is a soluble decoy VEGFR formed by fusion of the Ig domains of VEGFR1 and VEGFR2 with the Fc domain of human IgG1. |
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V67708 | AhR modulator-1 | 118174-38-2 | AhR modulator-1 (compound 6-MCDF) is a selective orally bioactive aryl hydrocarbon receptor (AhR) modulator. |
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V0194 | ALG1001 (Risuteganib; Luminate) | 1307293-62-4 | ALG1001 (discontinued,also known as Risuteganib andLuminate, developed by Allegro Ophthalmics) is a potent and selective small peptide with a sequence ofGly-Arg-Gly-Cya-Thr-Pro. |
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V69533 | Axitinib-13C,d3 (AG-013736-13C,d3) | 1261432-00-1 | Axitinib-13C,d3 is a 13C (carbon 13)-labeled and deuterated Axitinib. |
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V69627 | Axitinib-d3 (AG-013736-d3) | 1126623-89-9 | Axitinib-d3 is the deuterated form of Axitinib. |
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V69636 | Bevasiranib | 959961-96-7 | Bevasiranib is an siRNA that silences the gene that produces vascular endothelial growth factor (VEGF). |
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V69632 | Bevasiranib sodium | 849758-52-7 | Bevasiranib sodium is an siRNA that silences the gene that produces vascular endothelial growth factor (VEGF). |
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V69605 | Brolucizumab (DLX1008; ESBA 1008; RTH258) | 1531589-13-5 | Brolucizumab (DLX1008) is a single-chain anti-VEGF-A antibody fragment with low picomolar affinity (KD=1.05 pM). |
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V69626 | CBO-P11 | 612096-46-5 | CBO-P11 specifically binds to the VEGFR-2 receptor and serves as a targeting ligand for tumor angiogenesis. |
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V69621 | Conbercept (KH902) | 1227158-72-6 | Conbercept (KH902) is a monoclonal antibody (mAb) targeting VEGFRA fused to the IGHG1 Fc fragment. |
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V69455 | CP-547632 TFA | 2805804-54-8 | CP-547632 TFA is an orally bioactive, ATP-competitive inhibitor of VEGFR-2 and FGF kinases with IC50s of 11 nM and 9 nM, respectively. |
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V69613 | Dilpacimab (ABT165; PR1283233) | 1791420-09-1 | Dilpacimab (ABT165) is a potent dual variable domain immunoglobulin targeting the delta-like ligand 4 (DLL4) and VEGF pathways. |
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V69620 | Efdamrofusp alfa | 2375661-82-6 | Efdamrofusp alfa is a bispecific fusion protein. |
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