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-169516
    VEGFR-2-IN-65
    Inhibitor
    VEGFR-2-IN-65 (Compound 07) is a VEGFR-2 inhibitor. VEGFR-2-IN-65 has H-bond interactions with Cys180. VEGFR-2-IN-65 inhibits tube formation in HUVECs.
    VEGFR-2-IN-65
  • HY-165603
    Si5-N14
    Inhibitor
    Si5-N14 is a key component of siloxane-incorporated lipid nanoparticles (SiLNP), possessing pro-vascular repair and anti-tumor activities. In the transgenic GFP mouse model, Si5-N14 can mediate CRISPR-Cas9 editing. In the Lewis lung carcinoma (LLC) tumor-bearing mouse model, Si5-N14 can knock out the expression of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) to exert an anti-tumor effect. In a mouse model of lung injury induced by viral infection, the delivery of Fibroblast Growth Factor-2 (FGF-2) mRNA via Si5-N14 can promote vascular repair, increase blood oxygen levels, and improve lung function. Si5-N14 shows promise for research in the fields of oncology, pneumonia, and cardiovascular diseases.
    Si5-N14
  • HY-15769A
    WHI-P180 hydrochloride
    Inhibitor
    WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
    WHI-P180 hydrochloride
  • HY-111326AR
    Naphazoline nitrate (Standard)
    Inhibitor
    Naphazoline (nitrate) (Standard) is the analytical standard of Naphazoline (nitrate). This product is intended for research and analytical applications. Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline nitrate can be used for non-bacterial conjunctivitis research.
    Naphazoline nitrate (Standard)
  • HY-10338R
    Foretinib (Standard)
    Inhibitor
    Foretinib (Standard) is the analytical standard of Foretinib. This product is intended for research and analytical applications. Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
    Foretinib (Standard)
  • HY-160686
    GSK248233A
    Inhibitor
    GSK248233A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 1.03 μM and 2 nM, respectively. GSK248233A also shows activity against the AGC family. GSK248233A acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays.
    GSK248233A
  • HY-13314R
    Tesevatinib (Standard)
    Inhibitor
    Tesevatinib (Standard) is the analytical standard of Tesevatinib. This product is intended for research and analytical applications. 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 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity.
    Tesevatinib (Standard)
  • HY-164529
    SJ-C1044
    Inhibitor
    SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer.
    SJ-C1044
  • HY-108226
    Regorafenib N-oxide and N-desmethyl (M5)
    Inhibitor
    Regorafenib N-oxide and N-desmethyl (M5) (N-Desmethyl regorafenib N-oxide) is an active metabolite of Sorafenib (HY-10201) and can be metabolized by CYP3A4.
    Regorafenib N-oxide and N-desmethyl (M5)
  • HY-10977R
    Tivozanib (Standard)
    Inhibitor
    Tivozanib (Standard) is the analytical standard of Tivozanib. This product is intended for research and analytical applications. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy.
    Tivozanib (Standard)
  • HY-116590
    (±)-Glaziovine
    Inhibitor
    (±)-Glaziovine, a proaporphine alkaloid, has anxiolytic activity. (±)-Glaziovine can be used for neuropharmacological research.
    (±)-Glaziovine
  • HY-11106R
    Nintedanib esylate (Standard)
    Inhibitor
    Nintedanib esylate (Standard) is the analytical standard of Nintedanib esylate. This product is intended for research and analytical applications. Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib esylate (Standard)
  • HY-13718A
    Oglufanide disodium
    Inhibitor
    Oglufanide (H-Glu-Trp-OH) disodium is a dipeptide immunomodulator isolated from calf thymus. Oglufanide disodium inhibits vascular endothelial growth factor (VEGF). Oglufanide disodium can stimulate the immune response to hepatitic C virus (HCV) and intracellular bacterial infections. Oglufanide disodium shows antitumor and anti-angiogenesis activities.
    Oglufanide disodium
  • HY-10331R
    Regorafenib (Standard)
    Inhibitor
    Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
    Regorafenib (Standard)
  • HY-169627
    VEGFR-IN-7
    Inhibitor
    VEGFR-IN-7 (Compound 2) is a VEGFR inhibitor, showing inhibition of angiogenesis to a lesser extent. VEGFR-IN-7 is promising for research of cardiovascular diseases.
    VEGFR-IN-7
  • HY-169520
    VEGFR/PDGFR-IN-1
    Inhibitor
    VEGFR/PDGFR-IN-1 (Compound 1) is the inhibitor for VEGFR with an IC50 of 0.4 μM. VEGFR/PDGFR-IN-1 inhibits angiogenesis in HUVEC cell, exhibiting potential in tumor growth and metastasis inhibition.
    VEGFR/PDGFR-IN-1
  • HY-15467
    ZM323881
    Inhibitor
    ZM323881 is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
    ZM323881
  • HY-13068R
    Golvatinib (Standard)
    Inhibitor
    Golvatinib (Standard) is the analytical standard of Golvatinib. This product is intended for research and analytical applications. Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
    Golvatinib (Standard)
  • HY-10208S2
    Pazopanib-d3
    Inhibitor
    Pazopanib-d3 (GW786034-d3) is deuterium 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-d<sub>3</sub>
  • HY-10337R
    Brivanib (Standard)
    Inhibitor
    Brivanib (Standard) is the analytical standard of Brivanib. This product is intended for research and analytical applications. Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
    Brivanib (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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