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-N0883
    Gamabufotalin
    Inhibitor 99.96%
    Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.
    Gamabufotalin
  • HY-15511
    Tyrphostin A9
    Inhibitor 99.87%
    Tyrphostin A9, a PDGFR inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. Tyrphostin A9 has anti-influenza virus activities.
    Tyrphostin A9
  • HY-P9951A
    Ranibizumab (anti-VEGF)
    Inhibitor 98.08%
    Ranibizumab (RG-6321) (anti-VEGF) is a humanized anti-VEGF monoclonal antibody fragment and can recognize all VEGF-A isoforms (VEGF110, VEGF121, and VEGF165). Ranibizumab (anti-VEGF) slows vision loss in vivo and is used for wet age-related macular degeneration (AMD) research.
    Ranibizumab (anti-VEGF)
  • HY-10337
    Brivanib
    Inhibitor 99.92%
    Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2/KDR/Flk-1 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
    Brivanib
  • HY-10248
    RAF265
    Inhibitor 99.80%
    RAF265 is a potent and orally active RAF/VEGFR2/KDR/Flk-1 inhibitor.
    RAF265
  • HY-15391
    Lucitanib
    Inhibitor 98.94%
    Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
    Lucitanib
  • HY-124593
    PTC299
    Inhibitor 99.89%
    PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.
    PTC299
  • HY-13314
    Tesevatinib
    Inhibitor 99.21%
    Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2/KDR/Flk-1 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity.
    Tesevatinib
  • HY-N2575
    Hypocrellin A
    Inhibitor 99.73%
    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).
    Hypocrellin A
  • HY-N0316
    Mollugin
    Inhibitor 99.48%
    Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway.
    Mollugin
  • HY-112292A
    GW806742X hydrochloride
    Inhibitor 98.77%
    GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2/KDR/Flk-1 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis.
    GW806742X hydrochloride
  • HY-10501
    SU14813
    Inhibitor 99.63%
    SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2/KDR/Flk-1, VEGFR1/Flt-1, PDGFRβ and KIT.
    SU14813
  • HY-10517
    Orantinib
    Inhibitor 99.21%
    Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
    Orantinib
  • HY-109019
    Vorolanib
    Inhibitor 99.88%
    Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
    Vorolanib
  • HY-18303
    AMG-47a
    Inhibitor 99.34%
    AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
    AMG-47a
  • HY-10372
    PP121
    Inhibitor 98.67%
    PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2/KDR/Flk-1, Src, PDGFR, respectively.
    PP121
  • HY-13068
    Golvatinib
    Inhibitor 99.89%
    Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2/KDR/Flk-1 kinases with IC50s of 14 and 16 nM, respectively.
    Golvatinib
  • HY-10333
    BMS-690514
    Inhibitor 99.07%
    BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
    BMS-690514
  • HY-12038
    Ki8751
    Inhibitor 98.15%
    Ki8751 is a potent VEGFR2/KDR/Flk-1 inhibitor with an IC50 of 0.9 nM.
    Ki8751
  • HY-10527
    Telatinib
    Inhibitor 99.60%
    Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
    Telatinib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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