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

VEGFR

Vascular endothelial growth factor receptor

VEGFR

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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-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-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-P991625
    VX70
    VX70 is a humanized monoclonal antibody inhibitor targeting VEGF-A. VX70 can be used for cancers research.
    VX70
  • 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-175848
    NSC 850745
    		Inhibitor
    NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC50 values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer.
    NSC 850745
  • HY-B0239S2
    Threo-Chloramphenicol-d6
    Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol. 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.
    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
  • HY-15334
    CEP-5214
    		Inhibitor
    CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability.
    CEP-5214
  • HY-180292
    Tubulin/VEGFR-2-IN-2
    		Inhibitor
    Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma.
    Tubulin/VEGFR-2-IN-2
  • HY-177612A
    AGN-745 sodium
    		Inhibitor
    AGN-745 sodium is a chemically modified siRNA targeted to VEGFR-1. It is used for the study of Macular degeneration.
    AGN-745 sodium
  • HY-147779
    VEGFR-2-IN-20
    		Inhibitor
    VEGFR-2-IN-20 (Compound 7) is a potent inhibitor of VEGFR. VEGFR-2-IN-20 has the potential for the research of cancer diseases.
    VEGFR-2-IN-20
  • HY-135216
    Antiproliferative agent-54
    		Inhibitor
    Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC50 of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC50 of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats.
    Antiproliferative agent-54
  • HY-168126
    VEGFR-2-IN-56
    		Inhibitor
    VEGFR-2-IN-56 (compund 12e) is a potent VEGFR-2 inhibitor (IC50=45.9 nM).
    VEGFR-2-IN-56
  • HY-146230
    VEGFR-2-IN-26
    		Inhibitor
    VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells.
    VEGFR-2-IN-26
  • HY-156635
    TIE-2/VEGFR-2 kinase-IN-3
    		Inhibitor
    TIE-2/VEGFR-2 kinase-IN-3, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC50 values of 6.9 nM and 3.5 nM, respectively. TIE-2/VEGFR-2 kinase-IN-3 can be used for the research of angiogenesis.
    TIE-2/VEGFR-2 kinase-IN-3
  • HY-175635
    EGFR/VEGFR2-IN-6
    		Inhibitor
    EGFR/VEGFR2-IN-6 (Compound 3k) is a dual-functional inhibitor of EGFR and VEGFR2 with IC50s of 10.53 and 3.37 μM for EGFR and VEGFR2, respectively. EGFR/VEGFR2-IN-6 has significant anti-proliferation activity against breast cancer cells, and induces G0/G1 cell cycle arrest and cell apoptosis, especially early apoptosis. EGFR/VEGFR2-IN-6 can be used for cancers research.
    EGFR/VEGFR2-IN-6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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