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-P3990
    Coibamide A
    		Inhibitor
    Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts.
    Coibamide A
  • HY-179497
    FLT3-IN-37
    		Inhibitor
    FLT3-IN-37 (Compound 6z) is a potent inhibitor of FLT3-ITD, with IC50 values of 1.5 and 3.4 nM for FLT3-ITD and TEL-VEGFR2, respectively. FLT3-IN-37 exhibits high selectivity for wild-type FLT3 (WT) and c-Kit. FLT3-IN-37 inhibits FLT3 phosphorylation and downregulates the expression of p-Akt, p-STAT5, and p-ERK. FLT3-IN-37 exerts anti-leukemia effects by blocking the cell cycle and inducing apoptosis (apoptosis). FLT3-IN-37 can be used for research on acute myeloid leukemia (AML).
    FLT3-IN-37
  • HY-184162
    HSP110-IN-1
    		Inhibitor
    HSP110-IN-1 is a HSP110 inhibitor. HSP110-IN-1 binds to HSP110, inhibits the activity of STAT3, and downregulates the expression of downstream genes VEGF, MMP7 and MMP9. HSP110-IN-1 abrogates IL-6-induced epithelial-mesenchymal transition and inhibits the proliferation of colorectal cancer cells. HSP110-IN-1 remodels the tumor microenvironment by inducing a pro-inflammatory phenotype, regulates macrophages, induces PD-L1 expression, and enhances anti-PD-L1 antibody-mediated tumor regression. HSP110-IN-1 can be used in studies related to colorectal cancer.
    HSP110-IN-1
  • HY-155685
    SA-VA
    		Inhibitor
    SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase.
    SA-VA
  • HY-50905S
    Dovitinib-d8
    		Inhibitor
    Dovitinib-d8 is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.
    Dovitinib-d<sub>8</sub>
  • HY-13314A
    Tesevatinib tosylate
    		Inhibitor
    Tesevatinib (XL-647) tosylate is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib tosylate significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib tosylate also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib tosylate can inhibit tumor proliferation and exhibits antitumor activity.
    Tesevatinib tosylate
  • HY-181775
    VEGFR-2/c-Met/EGFR-IN-1
    		Inhibitor
    VEGFR-2/c-Met/EGFR-IN-1 is a VEGFR-2/c-Met/EGFR inhibitor with IC50 values of 0.014 μM, 0.072 μM, and 0.94 μM, respectively. c-Met-IN-27 inhibits neovascularization in the chick chorioallantoic membrane (CAM) assay and exhibits in vivo anti-angiogenic activity. c-Met-IN-27 can be used in angiogenesis-related research.
    VEGFR-2/c-Met/EGFR-IN-1
  • HY-175019
    VEGFR-2-IN-70
    		Inhibitor
    VEGFR-2-IN-70 is a potent VEGFR-2 inhibitor with an IC50 of 18.04 nM. VEGFR-2-IN-70 exhibits cytotoxicity against A549 and MCF-7 cancer cells with IC50 values of 0.43 μM and 3.8 μM, respectively. VEGFR-2-IN-70 induces G1 cell cycle arrest and apoptosis in lung cancer cells. VEGFR-2-IN-70 is useful in cancer research.
    VEGFR-2-IN-70
  • HY-146367
    VEGFR-2-IN-19
    		Inhibitor
    VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent.
    VEGFR-2-IN-19
  • HY-179350
    EG01449 Free acid
    		Inhibitor
    EG01449 Free acid is a quinoline-based antagonist of Neuropilin-1 (NRP1) with an Kd of 0.6 µM. EG01449 Free acid competitively inhibits the binding of VEGFA to NRP1 with an IC50 of 362 nM. EG01449 Free acid prevents VEGFA-induced pain by inhibiting NRP1-dependent signaling and reducing sodium currents in sensory neurons. EG01449 Free acid can be used for the research of nociceptive pain.
    EG01449 Free acid
  • HY-170590
    VEGFR-2-IN-61
    		Inhibitor
    VEGFR-2-IN-61 (Compound 7b) is an inhibitor for VEGFR-2 with an IC50 of 2.83 µM. VEGFR-2-IN-61 inhibits the proliferation of multi cancer cells (IC50 for MCF-7 is 2.12 μM). VEGFR-2-IN-61 inhibits the cell migration, induces oxidative stress and apoptosis in MCF-7.
    VEGFR-2-IN-61
  • HY-170549
    VEGFR-2-IN-60
    		Inhibitor
    VEGFR-2-IN-60 (compound 5c) is a potent VEGFR-2 inhibitor with an IC50 of 1.07 nM. VEGFR-2-IN-60 exhibits cytotoxic activity against HCC1806, Hela, and A549 cell lines.
    VEGFR-2-IN-60
  • HY-N10330
    7-Hydroxyneolamellarin A
    		Inhibitor
    7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer.
    7-Hydroxyneolamellarin A
  • HY-165386
    TU-100
    		Inhibitor
    TU-100 is a Japanese herbal medicine. TU-100 exhibits anti-cancer effects by regulating cancer-associated fibroblasts (CAFs) in the TME. TU-100 can antagonize the M2 polarization phenotype of macrophages in the tumor microenvironment by suppressing the TLR4/NF-κB/STAT3 axis. TU-100 can inhibit the high expression of MMP-2, COX-2, and VEGF in TAMs.
    TU-100
  • HY-148316
    hVEGF-IN-2
    		Inhibitor
    hVEGF-IN-2 (compound 19) is a selective VEGF (Flk-1) receptor tyrosine kinases (RTK) inhibitor with an IC50 value of 2.5 μM. hVEGF-IN-2 inhibits PDGF RTK activity with an IC50 value of 33.1 μM. hVEGF-IN-2 can be used for the development of RTK-specific agents.
    hVEGF-IN-2
  • HY-146236
    VEGFR-2-IN-27
    		Inhibitor
    VEGFR-2-IN-27 (compound 7a) is a highly potent VEGFR-2 inhibitor with an IC50 value of 14.8 nM. VEGFR-2-IN-27 can be used for researching anticancer.
    VEGFR-2-IN-27
  • HY-117807
    A-176120
    		Inhibitor
    A-176120 is a selective inhibitor of farnesyl transferase (IC50=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC50=423 nM), GGTaseII (IC50=3000 nM), and SSase (IC50>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion.
    A-176120
  • HY-P991429
    THR-317
    		Inhibitor
    THR-317 is a human monoclonal antibody (mAb) targeting PLGF. THR-317 can be used in Diabetic retinopathy research.
    THR-317
  • HY-124122
    BPTQ
    		Inhibitor
    BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases.
    BPTQ
  • HY-116721
    AG-28262
    		Inhibitor
    AG-28262 is a VEGFR inhibitor. AG-28262 has anti-angiogenesis activity.
    AG-28262
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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