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-15458A
    (S)-SAR131675
    Inhibitor 99.72%
    (S)-SAR131675 is the S-enantiomer of SAR131675 (HY-15458), a potent and selective VEGFR3 inhibitor and a click chemistry reagent.
    (S)-SAR131675
  • HY-18309
    MET kinase-IN-4
    Inhibitor 99.46%
    MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer.
    MET kinase-IN-4
  • HY-13785
    ZM 306416
    Inhibitor 99.80%
    ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.
    ZM 306416
  • HY-U00437
    Pz-1
    Inhibitor 99.90%
    Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases.
    Pz-1
  • HY-N10521
    6'-Sialyllactose
    Inhibitor 99.51%
    6'-Sialyllactose promotes the growth of beneficial bacteria (such as Bifidobacterium and lactobacillus) and inhibits the proliferation of harmful bacteria. 6'-Sialyllactose exhibits anti-inflammatory and anti-angiogenic activities. 6'-Sialyllactose promotes the muscle health.
    6'-Sialyllactose
  • HY-12572
    TIE-2/VEGFR-2 kinase-IN-2
    Inhibitor 99.79%
    TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research.
    TIE-2/VEGFR-2 kinase-IN-2
  • HY-N3127
    Orobol
    99.28%
    Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ).
    Orobol
  • HY-153556
    GW297361
    Inhibitor 98.13%
    GW297361 is an oxindole CDK inhibitor that elicits a Pho85-selective response in cells. GW297361 inhibits yeast Cdk1 and Pho85 with IC50s of 20 nM and 400 nM in vitro, respectively.
    GW297361
  • HY-17617
    Nastorazepide
    99.95%
    Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide
  • HY-16025
    EOC317
    Inhibitor 98.05%
    EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.
    EOC317
  • HY-10207
    Dovitinib lactate
    Inhibitor 99.75%
    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα, respectively.
    Dovitinib lactate
  • HY-13737
    R1530
    Inhibitor 99.06%
    R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence.
    R1530
  • HY-100394
    NVP-BAW2881
    Inhibitor 98.54%
    NVP-BAW2881 (BAW2881) is a potent and selective VEGFR2 inhibitor with an IC50 of 9 nM.
    NVP-BAW2881
  • HY-136477
    Pentagamavunon-1
    Inhibitor 99.84%
    Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
    Pentagamavunon-1
  • HY-10987
    ENMD-2076 Tartrate
    Inhibitor 99.42%
    ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
    ENMD-2076 Tartrate
  • 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-12423A
    Pamufetinib mesylate
    Inhibitor 99.17%
    Pamufetinib (TAS-115) mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
    Pamufetinib mesylate
  • 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-101931
    hVEGF-IN-1
    Inhibitor 99.26%
    hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression.
    hVEGF-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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