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-P11198
    AC-P19M
    Inhibitor
    AC-P19M is an anticancer peptide. AC-P19M induces apoptosis by disrupting the cell membrane of cancer cells. AC-P19M reverses epithelial-mesenchymal transition (EMT). AC-P19M shows anti-angiogenic activity through the inhibition of VEGF-VEGFR2/ERK/Akt signaling. AC-P19M can be used for lung cancer research.
    AC-P19M
  • HY-146491
    VEGFR-2/BRAF-IN-1
    Inhibitor
    VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAFV600E and BRAFWT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase.
    VEGFR-2/BRAF-IN-1
  • HY-179392
    Sunitinib-platinum(IV) prodrug-1
    Inhibitor
    Sunitinib-platinum(IV) prodrug-1 (Complex A) is a Pt(IV) prodrug based on Cisplatin (HY-17394), and this design aims to enable Pt(IV) to be reduced to active Pt(II) under intracellular reducing conditions, while simultaneously releasing a derivative of Sunitinib (HY-10255A) with tyrosine kinase inhibitor (TKI) activity. Sunitinib-platinum(IV) prodrug-1 exhibits excellent cytotoxicity against renal cell carcinoma (RCC), causing DNA crosslinking and apoptosis. Sunitinib-platinum(IV) prodrug-1 inhibits the VEGFR/PDGFR signaling pathway, suppressing tumor growth and angiogenesis. Sunitinib-platinum(IV) prodrug-1 can be used for research on renal cell carcinoma.
    Sunitinib-platinum(IV) prodrug-1
  • HY-177614A
    ALN-3133 sodium scrambled negative control
    Inhibitor
    ALN-3133 sodium scrambled negative control is the sequence scrambled negative control of ALN-3133 sodium.
    ALN-3133 sodium scrambled negative control
  • HY-158027
    B-Raf IN 17
    Inhibitor
    B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer.
    B-Raf IN 17
  • HY-12044R
    Cabozantinib S-malate (Standard)
    Inhibitor
    Cabozantinib (S-malate) (Standard) is the analytical standard of Cabozantinib (S-malate). This product is intended for research and analytical applications. Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
    Cabozantinib S-malate (Standard)
  • HY-155610
    VEGFR-2-IN-32
    Inhibitor
    VEGFR-2-IN-32 (Comp 3a) is an inhibitor of VEGFR-2 with an IC50 of 8.93 nM. VEGFR-2-IN-32 has cytotoxic activity against PC-3 cells with an IC50 of 1.22 μM. VEGFR-2-IN-32 can be used for anti-prostate cancer research.
    VEGFR-2-IN-32
  • HY-149024
    VEGFR-2-IN-23
    Inhibitor
    VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cell cycle arrest at G1 phase.
    VEGFR-2-IN-23
  • HY-10406B
    rel-Talmapimod hydrochloride
    Inhibitor
    rel-Talmapimod (rel-SCIO-469) hydrochloride is an orally active and selective inhibitor of p38α MAPK with an IC50 of 9 nM. rel-Talmapimod hydrochloride inhibits the secretion of inflammatory factors (such as TNFα, IL-1β, IL-6, and VEGF) by suppressing the p38α MAPK pathway, and it also inhibits angiogenesis and osteoclast activation. rel-Talmapimod hydrochloride inhibits the growth of multiple myeloma cells and induces apoptosis. rel-Talmapimod hydrochloride can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome).
    rel-Talmapimod hydrochloride
  • HY-160687
    GW549390X
    Inhibitor
    GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.26 μM and 1.2 μM, respectively. GW549390X can bind to the ATP pocket of FLuc through the aniline side chain and is an ATP-competitive inhibitor of Fluc. GW549390X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, with potential implications for Fluc reporter assays.
    GW549390X
  • HY-10260S
    Vandetanib-d6
    Inhibitor
    Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) 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).
    Vandetanib-d<sub>6</sub>
  • HY-157960
    VEGFR-2-IN-42
    Inhibitor
    VEGFR-2-IN-42 (compound 8c) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-42 shows anti-proliferative effect against MCF7 cells with the IC50 of 25 µM.
    VEGFR-2-IN-42
  • HY-10338A
    Foretinib phosphate
    Inhibitor
    Foretinib phosphate is an orally bioavailable small molecule with potential anti-tumor activity. Foretinib phosphate can selectively inhibit hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), thereby potentially inhibiting tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib phosphate shows different anti-cancer activity from cabozantinib in lung cancer cells and has stronger inhibitory effects on targets such as MEK1/2, FER and AURKB.
    Foretinib phosphate
  • HY-169216
    Multi-target kinase inhibitor 3
    Inhibitor
    Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM.
    Multi-target kinase inhibitor 3
  • HY-174324
    VEGFR-2/P-gp-IN-1
    Inhibitor
    VEGFR-2/P-gp-IN-1, a Licochalcone A (HY-N0372) derivative, is an orally active VEGFR-2 (IC50 = 0.885 μM) and P-gp inhibitor. VEGFR-2/P-gp-IN-1 achieves anti-tumor proliferation and overcomes chemotherapy resistance by synchronously inhibiting VEGFR-2 kinase activity and P-gp drug efflux pump function. VEGFR-2/P-gp-IN-1 inhibits phosphorylation of VEGFR-2 and downstream PI3K/AKT signaling pathway proteins, induces apoptosis, blocks cells in the S phase, and inhibits invasive migration. VEGFR-2/P-gp-IN-1 exerts potent in vivo anti-tumor effects in the HeLa/DDP cell xenograft tumor model. VEGFR-2/P-gp-IN-1 is used in cervical cancer research.
    VEGFR-2/P-gp-IN-1
  • HY-172272B
    DSPE-PEG5000-A7R
    DSPE-PEG5000-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-PEG5000-A7R
  • HY-125142
    AP-24567
    Inhibitor
    AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342).
    AP-24567
  • HY-146539
    HDAC-IN-35
    Inhibitor
    HDAC-IN-35 (Compound 14) is a potent, selective HDAC and VEGFR-2 inhibitor, with IC50 values of 0.166 and 13.2 µM for HDAC6 and VEGFR-2, respectively.
    HDAC-IN-35
  • HY-123795
    NY0123
    Inhibitor
    NY0123 is a EPAC1 inhibitor. NY0123 significantly inhibits the expression of EPAC1, phosphorylated AKT, phosphorylated ERK1/2 and phosphorylated VEGFR2. NY0123 inhibits angiogenesis and tumor growth of triple-negative breast cancer. NY0123 is applicable to relevant research on triple-negative breast cancer.
    NY0123
  • HY-163710
    hCA/VEGFR-2-IN-5
    Inhibitor
    hCA/VEGFR-2 IN-5 (compound 9) is an indolone-phenylsulfonamide and a potential dual inhibitor of cancer-related hCA IX/XII and VEGFR-2. The IC50 values of hCA/VEGFR-2-IN-5 for VEGFR-2, hCA IX and hCA XII are 0.38 μM, 40 and 3.2 nM, respectively. hCA/VEGFR-2-IN-5 has antitumor activity.
    hCA/VEGFR-2-IN-5
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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