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-164387A
    Sutetinib maleate
    		Inhibitor
    Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo.
    Sutetinib maleate
  • HY-149407
    Multi-kinase-IN-4
    		Inhibitor
    Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
    Multi-kinase-IN-4
  • HY-144796
    VEGFR-2-IN-15
    		Inhibitor
    VEGFR-2-IN-15 (Compound 14b) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-15 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis.
    VEGFR-2-IN-15
  • HY-169409
    VEGFR-2-IN-59
    		Inhibitor
    VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property.
    VEGFR-2-IN-59
  • HY-P990542
    Anti-VEGFR2/KDR/CD309 Antibody
    		Inhibitor
    Anti-VEGFR2/KDR/CD309 Antibody is a humanized antibody expressed in CHO, targeting VEGFR2/KDR/CD309. The Anti-VEGFR2/KDR/CD309 Antibody is equipped with muIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For isotype control of the Anti-VEGFR2/KDR/CD309 Antibody, refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-VEGFR2/KDR/CD309 Antibody
  • HY-161859
    VEGFR-2/STAT-3-IN-1
    		Inhibitor
    VEGFR-2/STAT-3-IN-1 (Compound 9f) is a dual inhibitor for VEGFR-2 (IC50=26.3 nM) and STAT-3 (IC50=5.63 nM). VEGFR-2/STAT-3-IN-1 inhibits the proliferation of cancer cells PANC1 and PC3 with IC50 of 0.14 and 0.10 µM. VEGFR-2/STAT-3-IN-1 induces apoptosis in PC3.
    VEGFR-2/STAT-3-IN-1
  • HY-10981S2
    Lenvatinib-15N,d4
    		Inhibitor
    Lenvatinib-15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
    Lenvatinib-<sup>15</sup>N,d<sub>4</sub>
  • HY-P10521
    Apolipoprotein KV domain (67-77)
    		Inhibitor
    Apolipoprotein KV domain (67-77) is an 11-amino acid peptide identified from the KV domain of human apolipoprotein a (ApoA) with antiangiogenic and antitumor activities. Apolipoprotein KV domain (67-77) targets the angiogenic c-Src/ERK pathway by blocking activation signals received from vascular endothelial growth factor (VEGF). Apolipoprotein KV domain (67-77) can be used in cancer research.
    Apolipoprotein KV domain (67-77)
  • HY-142518
    EGFR-IN-26
    		Inhibitor
    EGFR-IN-26 is a EGFR inhibitor extracted from patent WO2019162323A1 compound I-028. EGFR-IN-26 can be used for the research of cancer.
    EGFR-IN-26
  • HY-155694
    hCA/VEGFR-2-IN-1
    		Inhibitor
    hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual Carbonic Anhydrase(CA) IX/XII with Ki values of 4.7 nM and 8.3 nM for hCA XII and hCA IX, respectively. hCA/VEGFR-2-IN-1 (compound 13a) is a potent VEGFR-2 inhibitor with IC50 values 26.3 nM. hCA/VEGFR-2-IN-1 has anticancer activity.
    hCA/VEGFR-2-IN-1
  • HY-149475
    VEGFR-2-IN-33
    		Inhibitor
    VEGFR-2-IN-33 (Compound 4d) is a VEGFR inhibitor (IC50: 61.04 nM). VEGFR-2-IN-33 inhibits HepG2 cell proliferation with an IC50 of 4.31 nM. VEGFR-2-IN-33 can be used for research of hepatocellular carcinoma (HCC).
    VEGFR-2-IN-33
  • HY-146492
    VEGFR-2/BRAF-IN-2
    		Inhibitor
    VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase.
    VEGFR-2/BRAF-IN-2
  • HY-U00002A
    ZD-4190 hydrochloride
    		Inhibitor
    ZD-4190 hydrochloride is a potent VEGFR inhibitor with anti-tumor activity. ZD-4190 hydrochloride can delay the growth of MDA-MB-435 tumors by inhibiting tumor cell proliferation and angiogenesis.
    ZD-4190 hydrochloride
  • HY-144805
    VEGFR-2-IN-18
    		Inhibitor
    VEGFR-2-IN-18 (Compound 15d) is a potent VEGFR-2 inhibitor with an IC50 of 60 nM. VEGFR-2-IN-18 induces cell apoptosis. VEGFR-2-IN-18 shows antitumor activities.
    VEGFR-2-IN-18
  • HY-P4253A
    Arginyl-Glutamine TFA
    		Inhibitor
    Arginyl-Glutamine TFA is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy.
    Arginyl-Glutamine TFA
  • HY-110272
    Vatalanib succinate
    		Inhibitor
    Vatalanib (PTK787) succinate is a potent and orally active VEGFR inhibitor with IC50s of 37 nM, 77 nM, 270 nM, 660 nM, 730 nM, 1400 nM, and 580 nM for KDR, Flt-1, Flk, Flt-4, c-Kit, c-Fms, and PDGFR-β, respectively.
    Vatalanib succinate
  • HY-P990397
    Anti-DCBLD2/ESDN Antibody (FA19-1)
    		Inhibitor
    The Anti-DCBLD2/ESDN Antibody (FA19-1) is a humanized antibody expressed in CHO cells that targets DCBLD2/ESDN. The Anti-DCBLD2/ESDN Antibody (FA19-1) contains a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-DCBLD2/ESDN Antibody (FA19-1) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-DCBLD2/ESDN Antibody (FA19-1)
  • HY-170846
    FGFRs-IN-1
    		Inhibitor
    FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model.
    FGFRs-IN-1
  • HY-155464
    VEGFR-2/AURKA-IN-1
    		Chemical
    VEGFR-2/AURKA-IN-1 (compound 5e) is a thiazolidin-4-one derivative with antiglioma activity (IC50: 6.43 μM, LN229). VEGFR-2/AURKA-IN-1 has affinity for AURKA and VEGFR-2 and is a potential ligand. VEGFR-2/AURKA-IN-1 causes DNA strand breaks and exhibits cytotoxic and anticancer potential.
    VEGFR-2/AURKA-IN-1
  • HY-151969
    VEGFR-2-IN-30
    		Inhibitor
    VEGFR-2-IN-30 is a VEGFR-2 inhibitor (IC50: 66 nM). VEGFR-2-IN-30 also inhibits PDGFR, EGFR and FGFR1 with IC50s of 180, 98, 82 nM respectively. VEGFR-2-IN-30 arrests cancer cell at S-phase and induces early and late apoptosis.
    VEGFR-2-IN-30
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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