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-10260S2
    Vandetanib-13C6
    Inhibitor
    Vandetanib-13C6 is a deuterated labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
    Vandetanib-<sup>13</sup>C<sub>6</sub>
  • HY-172112
    VEGFR-2-IN-64
    Inhibitor
    VEGFR-2-IN-64 (Compound 28) is the inhibitor for VEGFR2 with IC50 of 27.8 nM. VEGFR-2-IN-64 inhibits the proliferation of cancer cell A549, T-47D and Caco-2, exhibits anti-migration and anti-cloning activities in cell T-47D, induces apoptosis in T-47D.
    VEGFR-2-IN-64
  • HY-153158
    VEGFR2-IN-3
    Inhibitor
    VEGFR2-IN-3 (compound 385) is a potent VEGFR2 inhibitor.
    VEGFR2-IN-3
  • HY-162887
    VEGFR-2-IN-53
    Inhibitor
    VEGFR-2-IN-53 (Compound 15w) is a VEGFR-2 inhibitor with an IC50 of 4.34 μM. VEGFR-2-IN-53 induces apoptosis by inhibiting VEGFR-2 activity and preventing cell migration, thereby exhibiting anti-angiogenic effects. The IC50 value of VEGFR-2-IN-53 for inhibiting MCF-7 cell growth is 3.87 μM. VEGFR-2-IN-53 can be used in cancer research.
    VEGFR-2-IN-53
  • HY-P3995
    Scospondistatin
    Scospondistatin is an anti-angiogenic peptide that can inhibit proliferation and migration of human umbilical vein endothelial cells in vitro.
    Scospondistatin
  • HY-162557
    VEGFR-2-IN-45
    Inhibitor
    VEGFR-2-IN-45 (compound 3j) is a potent inhibitor of VEGFR-2, with the IC50 of 0.2 μM. VEGFR-2-IN-45 plays an important role in cancer research.
    VEGFR-2-IN-45
  • HY-15268
    PP487
    Inhibitor
    PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research.
    PP487
  • HY-50904S
    Nintedanib-d3
    Inhibitor
    Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib-d<sub>3</sub>
  • HY-155242
    VEGFR-2-IN-36
    Inhibitor
    VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM).
    VEGFR-2-IN-36
  • HY-18318
    Takeda-6D
    Inhibitor
    Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity.
    Takeda-6D
  • HY-122010
    NVP-AAD777
    Inhibitor
    NVP-AAD777 is a specific inhibitor of VEGFR-2, demonstrated in vivo by its effective suppression of phospho-VEGFR-2 (Tyr1175) signaling in rat lung tissues. Unlike the nonspecific VEGFR inhibitor SUG-5416, NVP-AAD777 did not induce emphysematous changes in the lungs after three weeks of treatment, even when combined with exposure to cigarette smoke. Additionally, there were no alterations observed in vascular density compared to control animals. This indicates NVP-AAD777's targeted action in inhibiting VEGFR-2 without adverse pulmonary effects, highlighting its potential therapeutic utility in managing conditions associated with aberrant VEGFR-2 signaling.
    NVP-AAD777
  • HY-162064
    T-1-MBHEPA
    Inhibitor
    T-1-MBHEPA is a potent inhibitor of VEGFR-2, with the IC50 value of 0.121±0.051 μM. T-1-MBHEPA has anti-tumor and anti-angiogenic effect.
    T-1-MBHEPA
  • HY-117991
    DW10075
    Inhibitor
    DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
    DW10075
  • HY-N0545S
    Taurocholic acid-13C2,15N sodium
    Agonist
    Taurocholic acid-13C2,15N (sodium) is the 13C- and 15N- labeled Taurocholic acid (sodium).
    Taurocholic acid-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N sodium
  • HY-164387
    Sutetinib
    Inhibitor
    Sutetinib 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 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
  • HY-142085
    Antiproliferative agent-20
    Inhibitor
    Antiproliferative agent-20 is a potent and orally active anticancer agent. Antiproliferative agent-20 exhibits antiproliferative and anti-angiogenic activities.
    Antiproliferative agent-20
  • HY-P10052
    CBO-P11
    Inhibitor
    CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. CBO-P11 is modified with a nearinfrared cyanine dye bearing an alkyne function, allowing both “click” coupling on azido-modified nanoparticles and fluorescence labelling.
    CBO-P11
  • HY-N2575R
    Hypocrellin A (Standard)
    Inhibitor
    Hypocrellin A (Standard) is the analytical standard of Hypocrellin A. This product is intended for research and analytical applications. Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml)[1][2][3][4][5][6][7][8][9].
    Hypocrellin A (Standard)
  • HY-146228
    HSP90-IN-13
    Inhibitor
    HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway.
    HSP90-IN-13
  • HY-P990543
    Anti-VEGFR2/KDR/CD309 Antibody (AT001)
    Inhibitor
    The Anti-VEGFR2/KDR/CD309 Antibody (AT001) is a humanized antibody expressed in CHO cells that targets VEGFR2/KDR/CD309. The Anti-VEGFR2/KDR/CD309 Antibody (AT001) contains a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-VEGFR2/KDR/CD309 Antibody (AT001) can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-VEGFR2/KDR/CD309 Antibody (AT001)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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