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

VEGFR

Vascular endothelial growth factor receptor

VEGFR

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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.

VEGFR Isoform Specific Products:

VEGFR Isoform Comparison
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-P991626
    VGX200
    		Inhibitor
    VGX200 is a monoclonal antibody against vascular endothelial growth factor D (VEGFD).
    VGX200
  • HY-182306
    VEGFR-2 ligand-2
    		Ligand
    VEGFR-2 ligand-1, Sorafenib (HY-10201) derivative, is a vascular endothelial growth factor receptor 2 (VEGFR2) ligand. VEGFR-2 ligand-1 binds to the ATP-binding pocket of VEGFR2, forms hydrophobic contacts and hydrogen bonds with key binding-site residues. VEGFR-2 ligand-1 can be used for the research angiogenesis-related pathologies.
    VEGFR-2 ligand-2
  • HY-10208S1
    Pazopanib-13C,d3
    Pazopanib-13C,d3 is the deuterium and 13C labeled Pazopanib. 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.
    Pazopanib-<sup>13</sup>C,d<sub>3</sub>
  • HY-181766
    EGFR/VEGFR2-IN-11
    		Inhibitor
    EGFR/VEGFR2-IN-11 is an EGFR/VEGFR2 inhibitor with IC50 values of 0.62 μM (human EGFR), 2.26 μM (human VEGFR-2), 17.38 μM (human COX-2), and 19.31 μM (human tubulin). EGFR/VEGFR2-IN-11 inhibits COX-2 activity and tubulin polymerization. EGFR/VEGFR2-IN-11 induces cell cycle arrest and apoptosis. EGFR/VEGFR2-IN-11 exerts selective and antiproliferative activity against human cancer cells. EGFR/VEGFR2-IN-11 can be used for the research of colon carcinoma, breast carcinoma, leukemia, lymphoma, glioblastoma.
    EGFR/VEGFR2-IN-11
  • 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-10201S4
    Sorafenib-d3 tosylate
    		Inhibitor
    Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib 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-182032
    VEGFR-2-IN-83
    		Inhibitor
    VEGFR-2-IN-83 is a VEGFR-2 kinase inhibitor with an IC50 of 0.037 μM. VEGFR-2-IN-83 induces G0/G1 cell cycle arrest and apoptosis in breast cancer cells, and increases the production of reactive oxygen species (ROS). VEGFR-2-IN-83 is applicable to relevant research on breast cancer.
    VEGFR-2-IN-83
  • HY-184141
    EYE1090
    		Inhibitor
    EYE1090 is an orally active VEGFR2 inhibitor with an IC50 of 3 nM. EYE1090 inhibits angiogenesis, endothelial migration, VEGFR2-induced retinal leakage, and reduces choroidal neovascularization lesion size in mice. EYE1090 can be used for the research of age-related macular degeneration, diabetic retinopathy, choroidal neovascularization.
    EYE1090
  • 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-P992082
    Anti-Human/Rat VEGF Antibody (A.4.6.1)
    		Inhibitor
    Anti-Human/Rat VEGF Antibody (A.4.6.1) is an antibody targeting human and rat vascular endothelial growth factor (VEGF) that potently inhibits tumor growth in various animal models. Anti-Human/Rat VEGF Antibody (A.4.6.1) is the parent antibody of Bevacizumab (HY-P9906), and it exhibits high affinity and high selectivity for binding to human VEGF. The isotype control for Anti-Human/Rat VEGF Antibody (A.4.6.1) is Mouse IgG1 kappa, Isotype Control (HY-P99977).
    Anti-Human/Rat VEGF Antibody (A.4.6.1)
  • HY-175553
    VEGFR-2-IN-72
    		Inhibitor
    VEGFR-2-IN-72 is a selective VEGFR-2 inhibitor with an IC50 of 22.2 nM. VEGFR-2-IN-72 exhibits anticancer activity against HepG2 and Hep3B human HCC cell lines with IC50s of 15.7 and 2.4 μM. VEGFR-2-IN-72 can cause a mild blockage of the cell cycle and induce cell aopoptosis. VEGFR-2-IN-72 can used for the study of hepatocellular carcinoma (HCC).
    VEGFR-2-IN-72
  • HY-179485
    EGFR/VEGFR2-IN-10
    		Inhibitor
    EGFR/VEGFR2-IN-10 is a selective EGFR, VEGFR2 and COX2 inhibitor with IC50s of 8.5, 68 and 158 nM, respectively. EGFR/VEGFR2-IN-10 induces G1-phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8, and elevates caspase-9 protein levels, confirming activation of the intrinsic apoptotic pathway. EGFR/VEGFR2-IN-10 demonstrates exceptional therapeutic potential by simultaneously inhibiting tumor proliferation, angiogenesis, and inflammation pathways while maintaining a favorable selectivity profile. EGFR/VEGFR2-IN-10 can be used as a research tool for cervical, liver, colon, and breast cancer studies.
    EGFR/VEGFR2-IN-10
  • 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-178005
    EGFR-IN-174
    		Inhibitor
    EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer.
    EGFR-IN-174
  • 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-181776
    c-Met-IN-31
    		Inhibitor
    c-Met-IN-31 is a c-Met inhibitor with an IC50 value of 0.021 μM. c-Met-IN-31 also inhibits VEGFR-2 and EGFR activities, with IC50 values ​​of 0.32 μM and 9.3 μM, respectively. c-Met-IN-31 inhibits cancer cell proliferation. c-Met-IN-31 suppresses neovascularization in the chick chorioallantoic membrane (CAM) assay, exhibiting in vivo anti-angiogenic activity. c-Met-IN-31 can be used in research related to breast cancer and lung cancer.
    c-Met-IN-31
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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