2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. VEGFR

VEGFR

Vascular endothelial growth factor receptor

VEGFR

Related Products

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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.

VEGFR Isoform Specific Products:

VEGFR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161695
    Angiogenesis inhibitor 6
    Angiogenesis inhibitor 6 (Compound 8) is a non-tyrosine kinase inhibitor with effective antiangiogenic properties. Angiogenesis inhibitor 6 has antitumor activity.
    Angiogenesis inhibitor 6
  • HY-168127
    VEGFR-2-IN-57
    		Inhibitor
    VEGFR-2-IN-57 (compound 6n) exhibited significant cytotoxicity in HUVEC cells (IC50 = 28.77 nM).
    VEGFR-2-IN-57
  • HY-136209
    SU5208
    		Inhibitor 99.48%
    SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2).
    SU5208
  • HY-139996
    Pomalidomide-C5-Dovitinib
    		Inhibitor
    Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD+ acute myeloid leukemia.
    Pomalidomide-C5-Dovitinib
  • HY-161995
    FGFR1/VEGFR2-IN-2
    		Inhibitor
    FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells.
    FGFR1/VEGFR2-IN-2
  • HY-150027
    Multi-kinase-IN-3
    		Inhibitor
    Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor. Multi-kinase-IN-3 shows inhibition activity against VEGFR-2 and PDGFRβ, with IC50 values of 58.3 and 55 nM, respectively.
    Multi-kinase-IN-3
  • HY-170551
    CA IX/VEGFR-2-IN-3
    		Inhibitor
    CA IX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. CA IX/VEGFR-2-IN-3 exhibits anticancer activity, inhibiting the growth of MCF-7 breast cancer cells (with an IC50 of 22.33 μM) and mouse fibroblast cell line 3T3 (where cell viability is less than 40% at a concentration of 100 μM). CA IX/VEGFR-2-IN-3 can be used for research in the field of cancer treatment.
    CA IX/VEGFR-2-IN-3
  • HY-10201S2
    Sorafenib-13C,d3
    		Inhibitor 98.35%
    Sorafenib-13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
    Sorafenib-<sup>13</sup>C,d<sub>3</sub>
  • HY-168279
    VEGF-IN-1
    		Inhibitor
    VEGF-IN-1 (compound 6) can reduce the release of VEGF in U87-MG cells and inhibit angiogenesis in vitro. VEGF-IN-1 can inhibit cell proliferation by inducing autophagy in tumor cells, with an IC50 value of 28.35 μM for U87-MG cells.
    VEGF-IN-1
  • HY-143491
    VS 8
    		Inhibitor
    VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells).
    VS 8
  • HY-13590
    CEP-7055
    		Inhibitor
    CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
    CEP-7055
  • HY-10201S1
    Sorafenib-d4
    		Inhibitor
    Sorafenib-d4 is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
    Sorafenib-d<sub>4</sub>
  • HY-168073
    EGFR/VEGFR2-IN-1
    		Inhibitor
    EGFR/VEGFR2-IN-1 (Compound 10e) is a VEGFR-2 and EGFR inhibitor (IC50: 0.26 and 0.14 μM respectively). EGFR/VEGFR2-IN-1 inhibits tubulin polymerization with an IC50 of 40.9 μM. EGFR/VEGFR2-IN-1 induces apoptosis. EGFR/VEGFR2-IN-1 can be used for research of antileukemia and antilymphoma.
    EGFR/VEGFR2-IN-1
  • HY-144795
    VEGFR-2-IN-14
    		Inhibitor
    VEGFR-2-IN-14 (Compound 5) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-14 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis.
    VEGFR-2-IN-14
  • HY-W342441
    Monosialoganglioside GM3 (bovine)
    		Inhibitor
    Monosialoganglioside GM3 (bovine) is a monosialoganglioside and an inhibitor of VEGFR2 and Akt. At a concentration of 20 μM, Monosialoganglioside GM3 inhibits angiogenesis and reduces the proliferation and migration of human umbilical vein endothelial cells (HUVECs) by inhibiting VEGFR2 and Akt phosphorylation. Ganglioside GM3 also inhibits ferroptosis, providing protective effects during the formation of abdominal aortic aneurysms. Additionally, Monosialoganglioside GM3 (bovine) acts as an inhibitor of insulin signaling, inducing the dissociation of the insulin receptor (IR)-Caveolin-1 complex from lipid microdomains and causing insulin resistance in adipocytes. Monosialoganglioside GM3 (bovine) can be used in cancer and metabolic disease research.
    Monosialoganglioside GM3 (bovine)
  • HY-106374
    Elpamotide
    		Inhibitor
    Elpamotide is an epitope peptide derived from VEGFR2. Elpamotide induces cytotoxic T lymphocytes (CTLs) to kill VEGFR2-expressing endothelial cells. Elpamotide has potential immunostimulatory and antineoplastic activities. Elpamotide can be used in the research of cancer, such as pancreatic cancer.
    Elpamotide
  • HY-163747
    VEGFR-2-IN-47
    		Inhibitor
    VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma .
    VEGFR-2-IN-47
  • HY-B0239S2
    Threo-Chloramphenicol-d6
    Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol[1]. 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[2][3][4].
    Threo-Chloramphenicol-d<sub>6</sub>
  • HY-163533
    CPD-002
    		Inhibitor
    CPD-002 is an inhibitor for vascular endothelial growth factor receptor 2 (VEGFR 2), that inhibits angiogenesis through inhibition of VEGFR2/PI3K/AKT signaling pathway. CPD-002 exhibits anti-inflammatory activity and attenuates rheumatoid arthritis.
    CPD-002
  • HY-160684
    GW701427A
    		Inhibitor
    GW701427A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.12 μM and 603 nM, respectively. GW701427A acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays.
    GW701427A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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