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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V2092 | AAL-993 | 269390-77-4 | AAL-993 is a novel, orally bioavailable and highly potent VEGFR inhibitor that inhibits VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively. |
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V3414 | ACC-789 | 300842-64-2 | ACC-789, also known as ZK-202650 and NVP-ACC789 is a novel, potent, selective and orally bioavailable inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively. |
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V2156 | AMG-Tie2-1 | 870223-96-4 | AMG-Tie2-1 is an inhibitor (blocker/antagonist) of intimal endothelial cell kinase 2 (Tie2) with IC50 of 1 nM. |
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V85007 | Anti-Mouse VEGFR-2 Antibody (DC101) | ||
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V0496 | AZD2932 | 883986-34-3 | AZD2932 (AZD-2932), a new quinazoline ether, is a novel, potent, high affinity and mutil-targeted tyrosine kinase inhibitor with potential anticancer activity. |
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V2674 | BFH772 | 890128-81-1 | BFH772 (also known as BFH-772)is a novel andpotent orallybioavailableVEGFR2 inhibitor thattargets VEGFR2 kinase with IC50 of 3 nM. |
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V85453 | BHEP | ||
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V12626 | BIBF-1202 | 894783-71-2 | BIBF-1202 (BIBF1202; BIBF 1202) is the carboxylate metabolite of Nintedanib (formerly BIBF-1120; Vargatef), which is an approved anticancer medication acting as an orally bioavailable triple angiokinase (VEGFR, PDGFR, FGFR) inhibitor. |
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V0501 | BMS-794833 | 1174046-72-0 | BMS-794833 (BMS794833; BMS 794833) is an ATP competitive multi-kinase (Met/VEGFR2) inhibitor with potential anticancer activity. |
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V5272 | CP-547632 (PAN-90806) | 252003-65-9 | CP-547632 (PAN-90806), a novel isothiazole, is a novel, orally bioavailable and ATP-competitive inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. |
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V31207 | CP-547632 hydrochloride (PAN-90806) | 252003-71-7 | CP-547632 HCl (PAN90806), a novel isothiazole, is a orally-bioavailable and ATP-competitive inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. |
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V0528 | ENMD-2076 Tartrate | 1291074-87-7 | ENMD-2076Tartrate, the tartrate salt ofENMD-981693 (MKC-1693), is a novel, potent andorally bioactive multi-kinase inhibitorwith potential antineoplastic activity. |
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V79199 | hCA/VEGFR-2-IN-2 | 2971782-66-6 | hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual (bifunctional) inhibitor of cancer-associated hCA IX/XII and VEGFR-2. |
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V79040 | hCA/VEGFR-2-IN-3 | 2971782-73-5 | hCA/VEGFR-2-IN-3 (compound 8j) is an indolinylbenzenesulfonamide and a potential dual (bifunctional) inhibitor of cancer-associated hCA IX/XII and VEGFR-2. |
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V79440 | hCA/VEGFR-2-IN-4 | 2971782-83-7 | hCA/VEGFR-2-IN-4 (compound 15b) is an indolinonylbenzenesulfonamide and a potential dual (bifunctional) inhibitor of cancer-associated hCA IX/XII and VEGFR-2. |
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V32431 | hVEGF-IN-1 | 1637443-98-1 | hVEGF-IN-1, a quinazoline analogue, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilizes the G-quadruplex structure. |
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V2149 | JK-P3 | 942655-44-9 | JK-P3 is novel inhibitor of VEGFR-2. JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50 = 7.8 μM). |
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V0502 | Ki8751 | 228559-41-9 | Ki8751 (Ki-8751), aquinolyloxyphenyl-urea analog,is a novel,cell-permeableand selective inhibitor of VEGFR2 (Flk-1)with potential anticancer activity. |
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V0527 | KRN 633 | 286370-15-8 | KRN 633 (KRN-633) is a novel, potent, selective, cell-permeable, reversible,and ATP-competitive inhibitor of VEGFR1/2/3 with potential antitumor activity. |
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V0499 | LY2874455 | 1254473-64-7 | LY2874455 (LY-2874455; LY 2874455) is a novel and highly potent pan-FGFR inhibitor with potential anticancer activity. |
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