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-10065S
    Axitinib-13C,d3
    Inhibitor
    Axitinib-13C,d3 is a 13C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50 values of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
    Axitinib-<sup>13</sup>C,d<sub>3</sub>
  • HY-125741
    GW768505A free base
    Inhibitor 98.66%
    GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC50 of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity.
    GW768505A free base
  • HY-108443
    DMH4
    Inhibitor 98.98%
    DMH4 is a potent and selective inhibitor of VEGFR2 with an IC50 of 0.16 µM.
    DMH4
  • HY-18179
    AZD2932
    Inhibitor 99.04%
    AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.
    AZD2932
  • HY-152293
    EVT801
    Inhibitor
    EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models. EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    EVT801
  • HY-10517A
    (Z)-Orantinib
    Inhibitor 99.44%
    (Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
    (Z)-Orantinib
  • HY-109020
    Acrizanib
    Inhibitor 99.84%
    Acrizanib (LHA510) is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-VEGFR-2.
    Acrizanib
  • HY-12423
    Pamufetinib
    Inhibitor 98.28%
    Pamufetinib (TAS-115) is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
    Pamufetinib
  • HY-15769
    WHI-P180
    Inhibitor 99.84%
    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
  • HY-108798
    Ziv-aflibercept
    Inhibitor
    Ziv-aflibercept is a soluble inhibitor of vascular endothelial growth factor (VEGF). Ziv-aflibercept is an adaptive variant of Aflibercept (HY-108801), Ziv-aflibercept has a low PH value and high osmotic pressure when compared to Aflibercept. Ziv-aflibercept has potential applications in metastatic colorectal carcinoma and retinal diseases.
    Ziv-aflibercept
  • HY-15992S
    BIBF 1202-13C,d3
    Inhibitor 99.70%
    BIBF 1202-13C,d3 is the 13C- and deuterium labeled BIBF 1202. BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.
    BIBF 1202-<sup>13</sup>C,d<sub>3</sub>
  • HY-13023
    AMG-Tie2-1
    Inhibitor 99.5%
    AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) with an IC50 of 1 nM. AMG-Tie2-1 is a VEGFR2 inhibitor with an IC50 of 3 nM.
    AMG-Tie2-1
  • HY-18625A
    VEGFR-2-IN-5 hydrochloride
    Inhibitor 99.51%
    VEGFR-2-IN-5 hydrochloride is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 69.
    VEGFR-2-IN-5 hydrochloride
  • HY-N6794
    10Z-Hymenialdisine
    Inhibitor
    10Z-Hymenialdisine ((Z)-Hymenialdisine) is a natural bioactive pyrrole alkaloid. 10Z-Hymenialdisine is a pan kinase inhibitor, and has anticancer activities.
    10Z-Hymenialdisine
  • HY-10065S1
    Axitinib-d3
    98.03%
    Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively[1].
    Axitinib-d<sub>3</sub>
  • HY-50904S1
    Nintedanib-13C,d3
    Inhibitor ≥99.0%
    Nintedanib-13C,d3 is the 13C- and 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-<sup>13</sup>C,d<sub>3</sub>
  • HY-100315
    XL 999
    Inhibitor 99.01%
    XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC50 values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer.
    XL 999
  • HY-B0239R
    Chloramphenicol (Standard)
    Inhibitor
    Chloramphenicol (Standard) is the analytical standard of Chloramphenicol. This product is intended for research and analytical applications. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research.
    Chloramphenicol (Standard)
  • HY-18926
    VEGFR2-IN-7
    Inhibitor 99.79%
    VEGFR2-IN-7 (compound E) is an inhibitor of VEGFR2. VEGFR2-IN-7 can used in study cancers.
    VEGFR2-IN-7
  • HY-119757
    Tyrphostin AG1433
    Inhibitor 99.08%
    Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.
    Tyrphostin AG1433
Cat. No. Product Name / Synonyms Species Source
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