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-108444A
    (E)-FeCP-oxindole
    Inhibitor
    (Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM.
    (E)-FeCP-oxindole
  • HY-135671
    AhR modulator-1
    Inhibitor
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.
    AhR modulator-1
  • HY-P10797
    TAT-N24
    Inhibitor
    TAT-N24 is a cell-permeable TAT peptide as a p55PIK signaling inhibitor. TAT-N24 is effective for corneal neovascularization (CNV) and ocular inflammation by inhibiting the HIF-1α/NF-κB signaling pathway in corneal suture (CS). TAT-N24 also inhibits corneal neovascularization.
    TAT-N24
  • HY-163723
    EGFR-IN-116
    Inhibitor
    EGFR-IN-116 (compound 14D) is an anticancer agent. EGFR-IN-116 against EGFR has the IC50 values​of EGFR, VEGFR-2 and Topo II are 0.103 μM, 0.069 μM and 19.74 μM, respectively.
    EGFR-IN-116
  • HY-175820
    AGW-11
    Inhibitor
    AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer.
    AGW-11
  • HY-120200
    YF-452
    Inhibitor
    YF-452 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2). YF-452 remarkably inhibits the migration, invasion and tube-like structure formation of human umbilical vein endothelial cells (HUVECs) with little toxicity. YF-452 inhibits VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal regulated kinase (ERK), focal adhesion kinase (FAK) and Src. YF-452 is a potential antiangiogenic agent candidate for cancer research.
    YF-452
  • HY-162509
    YS07
    Inhibitor
    YS07 is a potent VEGFR-2 inhibitor. Molecular dynamics simulation study revealed sustained interactions of YS07 with key amino acids of VEGFR-2 at a run time of 100 ns. YS07 can be used for anticancer research.
    YS07
  • HY-163471
    PDGFRα/β/VEGFR-2-IN-1
    Inhibitor
    PDGFRα/β/VEGFR-2-IN-1 (6f), a multiple PDGFRα/ and VEGFR-2 tyrosine kinase inhibitor, particularly targets PDGFRα, PDGFRβ, and VEGFR-2 kinases with Nano molar concentrations.
    PDGFRα/β/VEGFR-2-IN-1
  • HY-178453
    VEGFR-2-IN-74
    Inhibitor
    VEGFR-2-IN-74 (compound 55) is a potent VEGFR-2 inhibitor (IC50 = 0.035 µM). VEGFR-2-IN-74 exhibits good anti proliferative activity and can induce apoptosis in various cancer cells, such as A549 (IC50 = 2.67 µM) and HCT116 (IC50 = 10.87 µM) cells. VEGFR-2-IN-74 has low toxicity to normal cells. VEGFR-2-IN-74 shows significant anti angiogenic effects in chicken embryo models. VEGFR-2-IN-74 can be used in the research of cancer.
    VEGFR-2-IN-74
  • HY-176805
    TGP-377
    Activator
    TGP-377 is a potent miR-377 inhibitor that specifically and effectively enhances VEGFA expression by targeting the non-coding microRNA that regulates VEGFA expression.
    TGP-377
  • 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-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-183778
    Antiangiogenic agent 9
    Inhibitor
    Antiangiogenic agent 9 is an antiangiogenic agent and also a VEGFR-2 inhibitor. Antiangiogenic agent 9 induces apoptosis of breast cancer cells by activating caspase-3 (apoptosis). Antiangiogenic agent 9 exhibits antiproliferative activity against breast cancer cells. Antiangiogenic agent 9 can be used for the research of breast cancer.
    Antiangiogenic agent 9
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.