1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. VEGFR

VEGFR

Vascular endothelial growth factor receptor

VEGFRs consist of three subtypes, the fms-like tyrosine kinase Flt-1 (VEGFR1/Flt-1), the kinase domain region, also referred to as fetal liver kinase (VEGFR2/KDR/Flk-1), and Flt-4 (VEGFR3). Each receptor has seven immunoglobulinlike domains in the extracellular domain, a single transmembrane region, and a consensus tyrosine kinase sequence interrupted by a kinase insert domain. VEGFR1 and 2 are expressed on vascular endothelial cells, whereas VEGFR3 is expressed on lymphatic endothelial. The VEGF family members VEGF-A, -B, -C, -D, -E, and PlGF, and the human immunodeficiency (HIV) Tat protein bind in specific patterns to three related receptor protein tyrosine kinases, VEGFR1, 2, and 3, and induce the formation of homo- and heteromeric receptor complexes. Binding of VEGF to VEGFR causes dimerization and autophosphorylation of the receptor. Intracellular proteins such as VEGFR-associated protein (VRAP), PLC, and Sck that associate with specific tyrosine residues of VEGFR are phosphorylated upon receptor activation. Several signal transduction pathways are activated by the binding of VEGF to its receptor, leading to increased proliferation, survival, permeability, and migration of cells.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101990
    IMS2186
    Inhibitor 99.81%
    IMS2186 is an anti-choroidal neovascularization (CNV) agent that inhibits angiogenesis upstream of VEGF. IMS2186 can arrest cancer cell cycle in G2/M phase, thus exerting anti-proliferation and anti-angiogenesis effects. IMS2186 has no intraocular toxicity and reduces the amount of eye leakage and diseased cells.
    IMS2186
  • HY-161586
    Chloramphenicol/BSA
    Inhibitor
    Chloramphenicol/BSA is the antigen-adjuvant conjugate formed by the coupling of Chloramphenicol (HY-B0239) with Bovine Serum Albumin (BSA). By conjugating the antigen with a protein adjuvant, the production of antigen-specific antibodies in vaccine models can be enhanced. The conjugate does not affect protein folding or disrupt major epitopes, and it can enhance cross-presentation and the generation of antigen-specific T cells.
    Chloramphenicol/BSA
  • HY-164413
    CLM3
    Inhibitor
    CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways.
    CLM3
  • HY-157324
    EGFR-IN-94
    Inhibitor
    EGFR-IN-94 (compound 5a) is a EGFR inhibitor with IC50 of 0.086?μM, and also has IC50 of 0.107μM and 2.52 μM for VEGFR-2 and Topo II, respectively. EGFR-IN-94 induces cell apoptosis and arrests cell cycle at the S phase in HepG-2 cells .
    EGFR-IN-94
  • HY-168114
    Multi-kinase inhibitor 3
    Inhibitor
    Multi-kinase inhibitor 3 (compound 12) is a potent and orally active multikinase inhibitor with IC50 values of 1.59, 1.23, 1.19, 0.59, 0.22, 1.15 nM for FLT1/VEGFR1, KDR/VEGFR2, FLT4/VEGFR3, FLT3, PDGFRα, PDGFRβ, respectively. Multi-kinase inhibitor 3 shows antiproliferative activity. Multi-kinase inhibitor 3 shows anticancer activity.
    Multi-kinase inhibitor 3
  • HY-155760
    hCA/VEGFR-2-IN-3
    Inhibitor
    hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells.
    hCA/VEGFR-2-IN-3
  • HY-P990318
    Alacizumab
    Inhibitor
    Alacizumab is a CHO-expressed humanized antibody that targets VEGFR2/KDR/CD309. Alacizumab contains huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 144.08 kDa. The isotype control for Alacizumab can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Alacizumab
  • HY-10981S1
    Lenvatinib-d5
    Inhibitor
    Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
    Lenvatinib-d<sub>5</sub>
  • HY-P10833
    C-VGB3
    Antagonist
    C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer.
    C-VGB3
  • HY-158233
    Apoptotic agent-4
    Inhibitor
    Apoptotic agent-4 (Compound 9) is a apoptosis inducer. Apoptotic agent-4 inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 inhibits cancer cell proliferation and arrests the cell at both the G2/M and Pre-G1 phases.
    Apoptotic agent-4
  • HY-164387A
    Sutetinib maleate
    Inhibitor
    Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo.
    Sutetinib maleate
  • HY-149407
    Multi-kinase-IN-4
    Inhibitor
    Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
    Multi-kinase-IN-4
  • HY-144796
    VEGFR-2-IN-15
    Inhibitor
    VEGFR-2-IN-15 (Compound 14b) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-15 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis.
    VEGFR-2-IN-15
  • HY-169409
    VEGFR-2-IN-59
    Inhibitor
    VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property.
    VEGFR-2-IN-59
  • HY-P990542
    Anti-VEGFR2/KDR/CD309 Antibody
    Inhibitor
    Anti-VEGFR2/KDR/CD309 Antibody is a humanized antibody expressed in CHO, targeting VEGFR2/KDR/CD309. The Anti-VEGFR2/KDR/CD309 Antibody is equipped with muIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For isotype control of the Anti-VEGFR2/KDR/CD309 Antibody, refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-VEGFR2/KDR/CD309 Antibody
  • HY-161859
    VEGFR-2/STAT-3-IN-1
    Inhibitor
    VEGFR-2/STAT-3-IN-1 (Compound 9f) is a dual inhibitor for VEGFR-2 (IC50=26.3 nM) and STAT-3 (IC50=5.63 nM). VEGFR-2/STAT-3-IN-1 inhibits the proliferation of cancer cells PANC1 and PC3 with IC50 of 0.14 and 0.10 µM. VEGFR-2/STAT-3-IN-1 induces apoptosis in PC3.
    VEGFR-2/STAT-3-IN-1
  • HY-10981S2
    Lenvatinib-15N,d4
    Inhibitor
    Lenvatinib-15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
    Lenvatinib-<sup>15</sup>N,d<sub>4</sub>
  • HY-P10521
    Apolipoprotein KV domain (67-77)
    Inhibitor
    Apolipoprotein KV domain (67-77) is an 11-amino acid peptide identified from the KV domain of human apolipoprotein a (ApoA) with antiangiogenic and antitumor activities. Apolipoprotein KV domain (67-77) targets the angiogenic c-Src/ERK pathway by blocking activation signals received from vascular endothelial growth factor (VEGF). Apolipoprotein KV domain (67-77) can be used in cancer research.
    Apolipoprotein KV domain (67-77)
  • HY-142518
    EGFR-IN-26
    Inhibitor
    EGFR-IN-26 is a EGFR inhibitor extracted from patent WO2019162323A1 compound I-028. EGFR-IN-26 can be used for the research of cancer.
    EGFR-IN-26
  • HY-155694
    hCA/VEGFR-2-IN-1
    Inhibitor
    hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual Carbonic Anhydrase(CA) IX/XII with Ki values of 4.7 nM and 8.3 nM for hCA XII and hCA IX, respectively. hCA/VEGFR-2-IN-1 (compound 13a) is a potent VEGFR-2 inhibitor with IC50 values 26.3 nM. hCA/VEGFR-2-IN-1 has anticancer activity.
    hCA/VEGFR-2-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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