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-14575
    Nastorazepide hemicalcium
    Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer. Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
    Nastorazepide hemicalcium
  • HY-P990147
    Anti-Mouse VEGFR-2 Antibody (DC101-Mouse IgG2a)
    Inhibitor
    Anti-Mouse VEGFR-2 Antibody (DC101-CP132) is a mouse-derived IgG2a, κ type antibody inhibitor, targeting to mouse VEGFR-2.
    Anti-Mouse VEGFR-2 Antibody (DC101-Mouse IgG2a)
  • HY-15492A
    AG-13958 (mono(hydrochloride))
    Inhibitor
    AG-13958 monohydrochloride, a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD).
    AG-13958 (mono(hydrochloride))
  • HY-144754
    VEGFR-2-IN-13
    Inhibitor
    VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor with an IC50 of 3.4 nM. VEGFR-2-IN-13 disrupts the HepG2 cell cycle by arresting the G2/M phase and induces apoptosis.
    VEGFR-2-IN-13
  • HY-151458
    VEGFR-2/DHFR-IN-1
    Inhibitor
    VEGFR-2/DHFR-IN-1 (compound 8b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.384 and 7.881 μM, respectively. VEGFR-2/DHFR-IN-1 shows good antibacterial activities against Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA and MRSA with MIC values of 16, 16, 16, 8, and 16 μg/mL, respectively. VEGFR-2/DHFR-IN-1 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 2.97-7.12 μM. VEGFR-2/DHFR-IN-1 can be used for the research of cancer.
    VEGFR-2/DHFR-IN-1
  • HY-10331AR
    Regorafenib monohydrate (Standard)
    Inhibitor
    Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate 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 monohydrate shows very robust antitumor and antiangiogenic activity.
    Regorafenib monohydrate (Standard)
  • HY-170776
    AXL/Angiokinase-IN-1
    Inhibitor
    AXL/Angiokinase-IN-1 (compound 11b) is an AXL/triple angiokinase inhibitor, IC50=3.75 nM (AXL expression). AXL/Angiokinase-IN-1 inhibits epithelial-mesenchymal transition (EMT) in Bxpc-3, blocking lung cancer cell metastasis. AXL/Angiokinase-IN-1 also inhibits vascular and fibroblast functions, promoting apoptosis (apoptosis) in cancer cells and fibroblasts. AXL/Angiokinase-IN-1 features low toxicity and good metabolic stability.
    AXL/Angiokinase-IN-1
  • HY-P991416
    BAT5906
    Inhibitor
    BAT5906 is a human monoclonal antibody (mAb) targeting VEGFA. BAT5906 can be used in Wet age-related macular degeneration and Diabetic macular oedema research.
    BAT5906
  • HY-156452
    T-1-MCPAB
    Inhibitor
    T-1-MCPAB is a VEGFR-2 inhibitor (IC50=0.135 µM) that effectively inhibits MCF7 migration. T-1-MCPAB can be used in cancer research.
    T-1-MCPAB
  • HY-173365
    VEGFR-2-IN-67
    Inhibitor
    VEGFR-2-IN-67 (Compound 6b) is an inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2). Its IC50 values for MDA-231 and MCF-7 cell lines are 5.91 µM and 7.16 µM respectively, and its inhibitory effect on VEGFR-2 is comparable to that of Sorafenib (HY-10201) (IC50 is 53.63 nM). VEGFR-2-IN-67 exerts significant anti-cancer activity through mechanisms such as inducing Apoptosis (the early apoptosis rate reaches 57.20%), arresting the cell cycle at the G1 phase, upregulating pro-apoptotic markers and downregulating Bcl-2. VEGFR-2-IN-67 can be used for research in the field of cancer.
    VEGFR-2-IN-67
  • HY-172272A
    DSPE-PEG2000-A7R
    DSPE-PEG2000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors.
    DSPE-PEG2000-A7R
  • HY-147926
    VEGFR-2-IN-28
    Inhibitor
    VEGFR-2-IN-28 (compound 12c) is a potent VEGFR-2 inhibitor with IC50 value of 0.83 µM. VEGFR-2-IN-28 induces apoptosis and has anticancer activity.
    VEGFR-2-IN-28
  • HY-14979A
    ML786 dihydrochloride
    Inhibitor
    ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
    ML786 dihydrochloride
  • HY-P991415
    ASKG-712
    Antagonist
    ASKG-712 (AM712) is a recombinant anti-VEGF humanized monoclonal antibody and Ang-2 antagonist peptide fusion protein. ASKG-712 can be used in Wet age-related macular degeneration and Diabetic macular oedema research.
    ASKG-712
  • HY-151459
    VEGFR-2/DHFR-IN-2
    Inhibitor
    VEGFR-2/DHFR-IN-2 (compound 5b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.623 and 9.085 μM, respectively. VEGFR-2/DHFR-IN-2 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 3.59-8.38 μM. VEGFR-2/DHFR-IN-2 can be used for the research of cancer.
    VEGFR-2/DHFR-IN-2
  • HY-10260S2
    Vandetanib-13C6
    Inhibitor
    Vandetanib-13C6 is a 13C labeled Vandetanib (HY-10260). Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
    Vandetanib-<sup>13</sup>C<sub>6</sub>
  • HY-172112
    VEGFR-2-IN-64
    Inhibitor
    VEGFR-2-IN-64 (Compound 28) is the inhibitor for VEGFR2 with IC50 of 27.8 nM. VEGFR-2-IN-64 inhibits the proliferation of cancer cell A549, T-47D and Caco-2, exhibits anti-migration and anti-cloning activities in cell T-47D, induces apoptosis in T-47D.
    VEGFR-2-IN-64
  • HY-153158
    VEGFR2-IN-3
    Inhibitor
    VEGFR2-IN-3 (compound 385) is a potent VEGFR2 inhibitor.
    VEGFR2-IN-3
  • HY-162887
    VEGFR-2-IN-53
    Inhibitor
    VEGFR-2-IN-53 (Compound 15w) is a VEGFR-2 inhibitor with an IC50 of 4.34 μM. VEGFR-2-IN-53 induces apoptosis by inhibiting VEGFR-2 activity and preventing cell migration, thereby exhibiting anti-angiogenic effects. The IC50 value of VEGFR-2-IN-53 for inhibiting MCF-7 cell growth is 3.87 μM. VEGFR-2-IN-53 can be used in cancer research.
    VEGFR-2-IN-53
  • HY-P3995
    Scospondistatin
    Scospondistatin is an anti-angiogenic peptide that can inhibit proliferation and migration of human umbilical vein endothelial cells in vitro.
    Scospondistatin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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