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-162557
    VEGFR-2-IN-45
    Inhibitor
    VEGFR-2-IN-45 (compound 3j) is a potent inhibitor of VEGFR-2, with the IC50 of 0.2 μM. VEGFR-2-IN-45 plays an important role in cancer research.
    VEGFR-2-IN-45
  • HY-15268
    PP487
    Inhibitor
    PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research.
    PP487
  • HY-50904S
    Nintedanib-d3
    Inhibitor
    Nintedanib-d3 is the 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-d<sub>3</sub>
  • HY-W751179
    Midostaurin-13C6
    Midostaurin-13C6 (PKC412-13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
    Midostaurin-<sup>13</sup>C<sub>6</sub>
  • HY-155242
    VEGFR-2-IN-36
    Inhibitor
    VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM).
    VEGFR-2-IN-36
  • HY-18318
    Takeda-6D
    Inhibitor
    Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity.
    Takeda-6D
  • HY-122010
    NVP-AAD777
    Inhibitor
    NVP-AAD777 is a specific inhibitor of VEGFR-2, demonstrated in vivo by its effective suppression of phospho-VEGFR-2 (Tyr1175) signaling in rat lung tissues. Unlike the nonspecific VEGFR inhibitor SUG-5416, NVP-AAD777 did not induce emphysematous changes in the lungs after three weeks of treatment, even when combined with exposure to cigarette smoke. Additionally, there were no alterations observed in vascular density compared to control animals. This indicates NVP-AAD777's targeted action in inhibiting VEGFR-2 without adverse pulmonary effects, highlighting its potential therapeutic utility in managing conditions associated with aberrant VEGFR-2 signaling.
    NVP-AAD777
  • HY-162064
    T-1-MBHEPA
    Inhibitor
    T-1-MBHEPA is a potent inhibitor of VEGFR-2, with the IC50 value of 0.121±0.051 μM. T-1-MBHEPA has anti-tumor and anti-angiogenic effect.
    T-1-MBHEPA
  • HY-117991
    DW10075
    Inhibitor
    DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
    DW10075
  • HY-N0545S
    Taurocholic acid-13C2,15N sodium
    Agonist
    Taurocholic acid-13C2,15N (sodium) is the 13C- and 15N- labeled Taurocholic acid (sodium).
    Taurocholic acid-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N sodium
  • HY-142085
    Antiproliferative agent-20
    Inhibitor
    Antiproliferative agent-20 is a potent and orally active anticancer agent. Antiproliferative agent-20 exhibits antiproliferative and anti-angiogenic activities.
    Antiproliferative agent-20
  • HY-P10052
    CBO-P11
    Inhibitor
    CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. CBO-P11 is modified with a nearinfrared cyanine dye bearing an alkyne function, allowing both “click” coupling on azido-modified nanoparticles and fluorescence labelling.
    CBO-P11
  • HY-N2575R
    Hypocrellin A (Standard)
    Inhibitor
    Hypocrellin A (Standard) is the analytical standard of Hypocrellin A. This product is intended for research and analytical applications. 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)[1][2][3][4][5][6][7][8][9].
    Hypocrellin A (Standard)
  • HY-146228
    HSP90-IN-13
    Inhibitor
    HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway.
    HSP90-IN-13
  • HY-P990543
    Anti-VEGFR2/KDR/CD309 Antibody (AT001)
    Inhibitor
    The Anti-VEGFR2/KDR/CD309 Antibody (AT001) is a humanized antibody expressed in CHO cells that targets VEGFR2/KDR/CD309. The Anti-VEGFR2/KDR/CD309 Antibody (AT001) contains a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for the Anti-VEGFR2/KDR/CD309 Antibody (AT001) can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-VEGFR2/KDR/CD309 Antibody (AT001)
  • HY-W706452
    Cabozantinib-d4 S-malate
    Cabozantinib-d4 (S-malate) (XL184-d4 (S-malate); BMS-907351-d4 (S-malate)) is the deuterium labeled Cabozantinib (S-malate) (HY-12044). Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
    Cabozantinib-d<sub>4</sub> S-malate
  • HY-155684
    SA-PA
    Inhibitor
    SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues.
    SA-PA
  • HY-P99516
    Vulinacimab
    Inhibitor
    Vulinacimab (HLX-06) is an anti-VEGFR-2 monoclonal antibody (mAb). Vulinacimab can be used in the research of cancers. VEGFR-2, overexpressed in certain tumors, is critical in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells.
    Vulinacimab
  • HY-145849
    VEGFR2-IN-1
    Inhibitor
    VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition.
    VEGFR2-IN-1
  • HY-170662
    VEGFR-2-IN-62
    Inhibitor
    VEGFR-2-IN-62 (Compound 3f) is an effective VEGFR-2 inhibitor with an IC50 value of 0.0557 μM. VEGFR-2-IN-62 can inhibit cell proliferation and induce apoptosis, and can be used in cancer research.
    VEGFR-2-IN-62
Cat. No. Product Name / Synonyms Species Source
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