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-W653842
    Taurocholic acid-d8 sodium
    		Agonist
    Taurocholic acid-d8 (sodium) is deuterium labeled Taurocholic acid (sodium). Taurocholic acid sodium (Sodium taurocholate) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid sodium has immunoregulation effect.
    Taurocholic acid-d<sub>8</sub> sodium
  • HY-10260S1
    Vandetanib-d4
    		Inhibitor
    Vandetanib-d4 is the deuterium labeled Vandetanib. Vandetanib (ZD6474) 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)[1][2].
    Vandetanib-d<sub>4</sub>
  • HY-152120
    (±)-Aiphanol
    		Inhibitor
    (±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak.(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 μM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active.
    (±)-Aiphanol
  • HY-169296
    IMPDH2-IN-4
    IMPDH2-IN-4 (compound 2d), a Mycophenolic acid (HY-B0421) analogue, is a selective IMPDH2 inhibitor with a Ki of 1.8 μM. IMPDH2-IN-4 exhibits good cytotoxic activity against osteosarcoma cancer cell lines. IMPDH2-IN-4 possesses a high affinity for VEGFR-2, CDK2, and IMPDH.
    IMPDH2-IN-4
  • HY-173124
    CDK2/FLT4/PDGFRA-IN-1
    		Inhibitor
    CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3) and PDGFRA, with IC50s of 1.672, 0.554, and 0.629 μM, respectively. CDK2/FLT4/PDGFRA-IN-1 exhibits potent antiproliferative effects against cancer cells (lung EBC-1, pancreatic ductal adenocarcinoma AsPC-1, colorectal HT-29 cells). CDK2/FLT4/PDGFRA-IN-1 can also induce apoptosis in cancer cells.
    CDK2/FLT4/PDGFRA-IN-1
  • HY-168104
    VEGFR-2-IN-55
    		Inhibitor
    VEGFR-2-IN-55 (Compound 30) is a potent VEGFR-2 kinase inhibitor with an IC50 value of 1.24 nM . VEGFR-2-IN-55 has antitumor activity.
    VEGFR-2-IN-55
  • HY-157546
    VEGFR-2-IN-40
    		Inhibitor
    VEGFR-2-IN-40 is a VEGFR-2 inhibitor. VEGFR-2-IN-40 boosts early and late apoptosis. VEGFR-2-IN-40 decreases the levels immunomodulatory proteins TNF-α and IL-6 while showing a four-fold rise in an apoptotic marker caspase-3.
    VEGFR-2-IN-40
  • HY-146884
    MET kinase-IN-3
    		Inhibitor
    MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines.
    MET kinase-IN-3
  • HY-160685
    GW809897X
    		Inhibitor
    GW809897X is a dual inhibitor of Fluc and VEGFR with IC50 of 0.58 μM and 65 nM, respectively. GW809897X is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential impact on Fluc reporter assays.
    GW809897X
  • HY-158328A
    CA IX/VEGFR-2-IN-2
    		Inhibitor
    CA IX/VEGFR-2-IN-2 (compound 5e) is a dual-targeted inhibitor. CA IX/VEGFR-2-IN-2 shows strong inhibitory effects on both CA IX (Ki=3.1 μM) and VEGFR-2 (IC50=32.1 nM). CA IX/VEGFR-2-IN-2 can be used for the study of pancreatic (PANC1), breast cancer (MCF7) and prostate cancer (PC3) .
    CA IX/VEGFR-2-IN-2
  • HY-139822
    VEGFR-2-IN-10
    		Inhibitor
    VEGFR-2-IN-10 exhibits increased antiangiogenic potency (IC50 = 0.7 μM) against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects.
    VEGFR-2-IN-10
  • HY-149675
    VEGFR-2/c-Met-IN-2
    		Inhibitor
    VEGFR-2/c-Met-IN-2 (compound 3e) is a VEGFR-2/c-Met inhibitor, with IC50 values of 83 and 48 nM, respectively. VEGFR-2/c-Met-IN-2 exhibits cytotoxic activity against HCT-116 cell line (IC50: 3.403 µM).
    VEGFR-2/c-Met-IN-2
  • HY-168655
    EGFR/VEGFR2-IN-3
    		Inhibitor
    EGFR/VEGFR2-IN-3 (compound 9) is a potent EGFR and VEGFR-2 inhibitor with IC50 values of 0.129, 0.142, 3.428 µM for EGFR, VEGFR-2, COX-2, respectively. EGFR/VEGFR2-IN-3 shows cytotoxicity. EGFR/VEGFR2-IN-3 induces apoptosis and cell cycle arrest at G2/M phase.
    EGFR/VEGFR2-IN-3
  • HY-116452
    YLT192
    		Inhibitor
    YLT192 is an orally active and highly bioavailable VEGFR2 inhibitor with potent anti-angiogenic activity and anti-tumor efficacy. YLT192 significantly inhibited the kinase activity of VEGFR2 and inhibited the proliferation, migration, invasion and tube formation of human umbilical cord vascular endothelial cells. YLT192 also inhibited VEGF-induced VEGFR2 phosphorylation and its downstream signaling regulators. YLT192 also showed the ability to inhibit angiogenesis in vivo in zebrafish embryo models and alginate-coated tumor cell experiments. YLT192 can directly inhibit the proliferation of cancer cells and induce their apoptosis.
    YLT192
  • HY-144803
    VEGFR-2-IN-16
    		Inhibitor
    VEGFR-2-IN-16 (Compound 15b) is a potent VEGFR-2 inhibitor with an IC50 of 86.36 nM. VEGFR-2-IN-16 shows antitumor activities.
    VEGFR-2-IN-16
  • HY-172787
    FGFR4-IN-23
    		Inhibitor
    FGFR4-IN-23 (compound 48c) is a FGFR4 inhibitor with an IC50 value of 2.9 nM against FGFR4WT kinase. FGFR4-IN-23 inhibits the phosphorylation of FGFR4, AKT and MAPK.
    FGFR4-IN-23
  • HY-150026
    Multi-kinase-IN-2
    		Inhibitor
    Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.
    Multi-kinase-IN-2
  • HY-P10550
    VGB4
    		Antagonist
    VGB4 is a VEGF-A and VEGF-B antagonist peptide that duplicates two binding domains of VEGF-B (loop 1 and loop3) and are linked together by the receptor-binding domain of VEGF-A (loop3). VGB4 has significant anti-angiogenic and anti-tumor activities and can regulate tumor growth and metastasis through multiple mechanisms. VGB4 could be used in anti-tumor research.
    VGB4
  • HY-151945
    TRK II-IN-1
    		Inhibitor
    TRK II-IN-1 is a potent type II TRK inhibitor, with IC50s of 3.3, 6.4, 4.3 and 9.4 nM, for TRKA/B/C and TRKAG667C, respectively. TRK II-IN-1 also inhibits FLT3, RET, and VEGFR2 with IC50s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers.
    TRK II-IN-1
  • HY-P99476
    ABP 215
    		Inhibitor
    ABP 215 (Bevacizumab-awwb), a Bevacizumab (Bevacizumab (HY-P9906)) biosimilar, is a humanized IgG1 monoclonal antibody targeting VEGFA (VEGFR.html" class="link-product" target="_blank">VEGFR). ABP 215 has anticancer effects, and can be used metastatic colorectal cancer (mCRC) research.
    ABP 215
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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