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-173232
    VEGFR-2-IN-66
    Inhibitor
    VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 value of 0.509 µM and an IC50 value of 7.48 μM for inhibiting the proliferation of MCF-7 cells. VEGFR-2-IN-66 exerts its anti-cancer activity by arresting the cell cycle, inducing apoptosis, and regulating gene expression, and can be used in the research of the breast cancer field.
    VEGFR-2-IN-66
  • HY-147714
    FGFR3-IN-2
    Inhibitor
    FGFR3-IN-2 (compound 18b) is a potent and selective FGFR3 inhibitor, with IC50s of 4.1 nM and 570 nM for FGFR3 and VEGFR2, respectively. FGFR3-IN-2 can be used for the research of bladder cancer.
    FGFR3-IN-2
  • HY-10208S1
    Pazopanib-13C,d3
    Pazopanib-13C,d3 is the deuterium and 13C labeled Pazopanib[1]. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
    Pazopanib-<sup>13</sup>C,d<sub>3</sub>
  • HY-163403
    VEGFR-2-IN-43
    Inhibitor
    VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research.
    VEGFR-2-IN-43
  • HY-P990540
    Anti-VEGFB Antibody (CSL346)
    Anti-VEGFB Antibody (CSL346) is a CHO-expressed human antibody that targets VEGFB. Anti-VEGFB Antibody (CSL346) contains huIgG4SP heavy chain and huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-VEGFB Antibody (CSL346) can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-VEGFB Antibody (CSL346)
  • HY-10201S4
    Sorafenib-d3 tosylate
    Inhibitor
    Sorafenib-d3 (Donafenib) tosylate is the 13C- and deuterium labeled Sorafenib. Sorafenib-d3tosylate is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib-d<sub>3</sub> tosylate
  • HY-123050
    (Rac)-SAR131675
    Inhibitor
    (Rac)-SAR131675 is the racemate of SAR131675. SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM.
    (Rac)-SAR131675
  • HY-168597
    FGFR1/VEGFR2-IN-3
    Inhibitor
    FGFR1/VEGFR2-IN-3 (Compound 8m) is a dual inhibitor of FGFR1/VEGFR2. FGFR1/VEGFR2-IN-3 exhibits anti-proliferative and anti-migratory activities against cancer cells, and is capable of inducing cell apoptosis.
    FGFR1/VEGFR2-IN-3
  • HY-144804
    VEGFR-2-IN-17
    Inhibitor
    VEGFR-2-IN-17 (Compound 15a) is a potent VEGFR-2 inhibitor with an IC50 of 67.25 nM. VEGFR-2-IN-17 shows antitumor activities.
    VEGFR-2-IN-17
  • HY-Y0121R
    Ethyl cinnamate (Standard)
    Inhibitor
    Ethyl cinnamate (Standard) is the analytical standard of Ethyl cinnamate. This product is intended for research and analytical applications. Ethyl cinnamate, an orally active chemical constituent of the rhizome of Kaempferia galanga, exhibits anti-cancer, nematocidal, sedative and vasorelaxant activities. Ethyl cinnamate is a fragrance ingredient used as a food flavor and additive for cosmetic products. Ethyl cinnamate is also an excellent clearing reagent for mammalian tissues. Ethyl cinnamate suppresses tumor growth through anti-angiogenesis by attenuating VEGFR2 signal pathway in colorectal cancer. Ethyl cinnamate inhibits the tonic contractions induced by high K+ and phenylephrine (PE) with respective IC50 values of 0.30 mM and 0.38 mM in rat aorta.
    Ethyl cinnamate (Standard)
  • HY-156638
    TIE-2/VEGFR-2 kinase-IN-5
    Inhibitor
    TIE-2/VEGFR-2 kinase-IN-5 is an anti-angiogenic agent. TIE-2/VEGFR-2 kinase-IN-5 also is a potent TIE-2 and VEGFR-2 tyrosine kinase inhibitor with pIC50 values of 7.78 nM and 8.11 nM, respectively. TIE-2/VEGFR-2 kinase-IN-5 can be used for the research of angiogenesis.
    TIE-2/VEGFR-2 kinase-IN-5
  • HY-146491
    VEGFR-2/BRAF-IN-1
    Inhibitor
    VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase.
    VEGFR-2/BRAF-IN-1
  • HY-158027
    B-Raf IN 17
    Inhibitor
    B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer.
    B-Raf IN 17
  • HY-12044R
    Cabozantinib (S-malate) (Standard)
    Inhibitor
    Cabozantinib (S-malate) (Standard) is the analytical standard of Cabozantinib (S-malate). This product is intended for research and analytical applications. Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
    Cabozantinib (S-malate) (Standard)
  • HY-N0135R
    Tanshinone IIA (Standard)
    Inhibitor
    Tanshinone IIA (Standard) is the analytical standard of Tanshinone IIA. This product is intended for research and analytical applications. Tanshinone IIA (Tan IIA) is one of the main compositions in the root of Salvia miltiorrhiza Bunge. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.
    Tanshinone IIA (Standard)
  • HY-155610
    VEGFR-2-IN-32
    Inhibitor
    VEGFR-2-IN-32 (Comp 3a) is an inhibitor of VEGFR-2 with an IC50 of 8.93 nM. VEGFR-2-IN-32 has cytotoxic activity against PC-3 cells with an IC50 of 1.22 μM. VEGFR-2-IN-32 can be used for anti-prostate cancer research.
    VEGFR-2-IN-32
  • HY-149024
    VEGFR-2-IN-23
    Inhibitor
    VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cell cycle arrest at G1 phase.
    VEGFR-2-IN-23
  • HY-160687
    GW549390X
    Inhibitor
    GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.26 μM and 1.2 μM, respectively. GW549390X can bind to the ATP pocket of FLuc through the aniline side chain and is an ATP-competitive inhibitor of Fluc. GW549390X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, with potential implications for Fluc reporter assays.
    GW549390X
  • HY-10260S
    Vandetanib-d6
    Inhibitor
    Vandetanib-d6 is the deuterium 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)[1].
    Vandetanib-d<sub>6</sub>
  • HY-157960
    VEGFR-2-IN-42
    Inhibitor
    VEGFR-2-IN-42 (compound 8c) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-42 shows anti-proliferative effect against MCF7 cells with the IC50 of 25 µM.
    VEGFR-2-IN-42
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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