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-P991419
    MSB-0254
    Inhibitor
    MSB-0254 is a human monoclonal antibody (mAb) targeting VEGFR2/KDR/CD309. MSB-0254 inhibits the invasion, migration, and vascular mimetic (VM) formation of U251 and primary glioma cells. MSB-0254 inhibits the growth of U251 and GL261 cell transplanted tumors. MSB-0254 reduces the expression of CD34, VEGFR2, Ki67, MMP2, MMP9, and CD34/PAS. MSB-0254 can be used in advanced solid tumors research.
    MSB-0254
  • HY-175565
    Tubulin/VEGFR-2-IN-1
    Inhibitor
    Tubulin/VEGFR-2-IN-1 is a dual inhibitor of tubulin and VEGFR-2 (IC50 = 1.52 μM) with anti-angiogenic activity. Tubulin/VEGFR-2-IN-1 exhibits potent cytotoxicity against the cancer cells. Tubulin/VEGFR-2-IN-1 elevates ROS production, induces apoptosis and causes G0/G1 phase arrest in HepG-2 cells. Tubulin/VEGFR-2-IN-1 inhibits the migratory ability and the clonogenic ability in HepG-2 cells. Tubulin/VEGFR-2-IN-1 can be used for the study of cancer.
    Tubulin/VEGFR-2-IN-1
  • 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, 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-181493
    VEGFR-2-IN-81
    Inhibitor
    VEGFR-2-IN-81 is a thiazole-based isoquinolin-1(2H)-one derivative and an VEGFR-2 inhibitor with IC50 of 1.94 μM. VEGFR-2-IN-81 exhibits significant selective cytotoxicity against colorectal cancer cells (IC50 = 7.75 μM). VEGFR-2-IN-81 exerts anti-colorectal cancer effects by inducing apoptosis, elevating intracellular ROS levels and reducing mitochondrial transmembrane potential. VEGFR-2-IN-81 can be used for the research of colorectal cancer, lung cancer, breast cancer, liver cancer.
    VEGFR-2-IN-81
  • 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-P991418
    MW02
    Inhibitor
    MW02 is a human monoclonal antibody (mAb) targeting VEGFA. MW02 can be used in Wet age-related macular degeneration research.
    MW02
  • 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-P992511
    CS2009
    Inhibitor
    CS2009 is a trispecific antibody targeting PD-1, CTLA-4 and VEGFA. CS2009 blocks the interactions of PD-1/PD-L1, CTLA-4/CD80 and VEGFA/VEGFR2, mediates checkpoint inhibition, and suppresses tumor angiogenesis. CS2009 reactivates PD-1/CTLA-4 double-positive tumor-infiltrating T lymphocytes, induces T cell activation, enhances tumor growth inhibition, promotes vascular normalization, improves T lymphocyte infiltration, and converts the immunosuppressive tumor microenvironment into an immunocompetent one. CS2009 can be used for the research of various advanced solid tumors.
    CS2009
  • HY-10501B
    (Z)-SU14813
    (Z)-SU14813 is an analog of SU14813 (HY-10501). SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
    (Z)-SU14813
  • 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-P11775
    Peptide HRH
    Ligand
    Peptide HRH is a polypeptide that specifically binds to VEGF receptors. Peptide HRH inhibits VEGF-stimulated endothelial cell proliferation. Peptide HRH inhibits angiogenesis and suppresses corneal neovascularization. Peptide HRH can be used in anti-angiogenesis related studies.
    Peptide HRH
  • HY-178968
    VEGFR-2-IN-76
    Inhibitor
    VEGFR-2-IN-76 (Compound GL-3) is a potent VEGFR-2 inhibitor with an IC50 value of 5.44 μM. VEGFR-2-IN-76 can be used for cancer research.
    VEGFR-2-IN-76
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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