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-168493
    FLT3/VEGFR2-IN-1
    		Inhibitor
    FLT3/VEGFR2-IN-1 (Compound 26) is a FLT3/VEGFR2/HDAC inhibitor with IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM for FLT3, VEGFR2, and HDAC1, respectively. FLT3/VEGFR2-IN-1 can inhibit the phosphorylation of STAT3 and ERK1/2 and the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 has anti-tumor activity and can be used for the research of acute myeloid leukemia.
    FLT3/VEGFR2-IN-1
  • HY-146368
    PROTAC VEGFR-2 degrader-1
    		Inhibitor
    PROTAC VEGFR-2 degrader-1（PROTAC-1）, a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM).
    PROTAC VEGFR-2 degrader-1
  • HY-149630
    VEGFR2/HDAC1-IN-1
    		Inhibitor
    VEGFR2/HDAC1-IN-1 (compound 13) is a potent VEGFR-2/HDAC dual inhibitor, with IC50s of 57.83 nM and 9.82 nM, respectively. VEGFR2/HDAC1-IN-1 arrests the cell cycle at the S and G2 phases, and induces apoptosis in HeLa cells. VEGFR2/HDAC1-IN-1 exhibits anti-angiogenic effect.
    VEGFR2/HDAC1-IN-1
  • HY-19471
    (rac)-ZK-304709
    		Inhibitor
    (rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET.
    (rac)-ZK-304709
  • HY-149674
    VEGFR-2/c-Met-IN-1
    		Inhibitor
    VEGFR-2/c-Met-IN-1 is a dual inhibitoe of VEGFR-2 and c-Met with IC50s of 138 nM and 74 nM, respectively. VEGFR-2/c-Met-IN-1 has antitumor activity.
    VEGFR-2/c-Met-IN-1
  • HY-157965
    ZINC09875266
    		Inhibitor
    ZINC09875266 is a dual inhibitor targeting VEGFR2 and FAK that can be used in cancer research.
    ZINC09875266
  • HY-161855
    VEGFR-2-IN-50
    		Inhibitor
    VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer, with an IC50 value of 0.33 μM. VEGFR-2-IN-50 (Compound 10f) has growth inhibitory activity on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, which is expected to be used in the study of breast cancer diseases.
    VEGFR-2-IN-50
  • HY-146229
    VEGFR-2-IN-25
    		Inhibitor
    VEGFR-2-IN-25 (compound 5d) is a highly potent VEGFR-2 inhibitor with an IC50 value of 12.1 nM. VEGFR-2-IN-25 can be used for researching anticancer.
    VEGFR-2-IN-25
  • HY-172272
    DSPE-PEG1000-A7R
    DSPE-PEG1000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors.
    DSPE-PEG1000-A7R
  • HY-163881
    VEGFR-IN-5
    		Inhibitor
    VEGFR-IN-5 (compound 9k) is a potent inhibitor of VEGFR2, with the IC50 of 8.4 nM and an acceptable oral bioavailability. VEGFR-IN-5 inhibits migration and invasion of human umbilical vein endothelial cells (HUVEC) cells and induces apoptosis.
    VEGFR-IN-5
  • HY-10368
    EGFR/VEGFR2-IN-4
    		Inhibitor
    EGFR/VEGFR2-IN-4 (Compound 19) is the irreversible inhibitor for EGFR and VEGFR-2 with IC50 of 18.7 nM and 102.3 nM, under the presence of 1 μM ATP.
    EGFR/VEGFR2-IN-4
  • HY-P991417
    LYN00101
    		Inhibitor
    LYN00101 is a human monoclonal antibody (mAb) targeting VEGFA. LYN00101 can be used in Cervical cancer, Colorectal cancer, Gastric cancer and Ovarian cancer research.
    LYN00101
  • HY-134000
    Emodic acid
    Emodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, ERK and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells.
    Emodic acid
  • HY-143293
    VEGFR-IN-3
    		Inhibitor
    VEGFR-IN-3 (compound 3f) is a VEGFR inhibitor. VEGFR-IN-3 inhibits OVCAR-4 and MDA-MB-468 cancer cells growth with IC50s of 0.29 and 0.35 μM, respectively. VEGFR-IN-3 can be used for the research of cancer.
    VEGFR-IN-3
  • HY-111326
    Naphazoline
    		Inhibitor 99.74%
    Naphazoline (Naphthazoline) is a potent α-adrenergic receptor agonist. Naphazoline reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline can be used for non-bacterial conjunctivitis research.
    Naphazoline
  • HY-163740
    VEGFR-2-IN-46
    		Inhibitor
    VEGFR-2-IN-46 (compound 4d) is a potent VEGFR-2 inhibitor with an EC50 value of 67.0 nM. VEGFR-2-IN-46 shows cytotoxicity and induces cell cycle arrest at the G2/M phase. VEGFR-2-IN-46 induces necrosis and apoptosis.
    VEGFR-2-IN-46
  • HY-104075
    R916562
    		Inhibitor
    R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
    R916562
  • HY-168170
    EGFR/VEGFR2-IN-2
    		Inhibitor
    EGFR/VEGFR2-IN-2 (compound 4b) is an dual inhibitor VEGFR-2 and EGFR..
    EGFR/VEGFR2-IN-2
  • HY-P991141
    Inlecitug
    		Ligand
    Inlecitug is a chimeric monoclonal antibody targeting human KDR (kinase insert domain receptor). Inlecitug specifically binds to KDR, blocking the binding of vascular endothelial growth factor (VEGF) to KDR and inhibiting angiogenesis, thus exerting antitumor activity. Inlecitug is promising for research of cancers.
    Inlecitug
  • HY-149512
    FGFR1/VEGFR2-IN-1
    		Inhibitor
    FGFR1/VEGFR2-IN-1 (compound 2b) is an FGFR1/VEGFR2 inhibitor. FGFR1/VEGFR2-IN-1 can be used for cancer research.
    FGFR1/VEGFR2-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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