1. Protein Tyrosine Kinase/RTK
  2. VEGFR

VEGFR

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:

  • VEGFR1/Flt-1

  • VEGFR2/KDR/Flk-1

  • VEGFR3/Flt-4

VEGFR Related Products (105):

Cat. No. Product Name Effect Purity
  • HY-10201
    Sorafenib Inhibitor 99.83%
    Sorafenib is a potent multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  • HY-10331
    Regorafenib Inhibitor 99.95%
    Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  • HY-13016
    Cabozantinib Inhibitor 99.92%
    Cabozantinib is a potent multiple RTKs inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50 of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
  • HY-10374
    SU5416 Inhibitor 99.93%
    SU5416 is a potent and selective inhibitor of the VEGFR (Flk-1/KDR) that inhibits tyrosine kinase catalysis, and inhibits autophosphorylation of the Flk-1 receptor with an IC50 of 1.23±0.2 μM (n=4) using an ELISA-based biochemical kinase assay.
  • HY-10201A
    Sorafenib Tosylate Inhibitor 99.73%
    Sorafenib tosylate is a potent multikinase inhibitor, with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  • HY-107145A
    Ningetinib Inhibitor 98.75%
    Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
  • HY-19716A
    Anlotinib Dihydrochloride Inhibitor 99.70%
    Anlotinib Dihydrochloride is a novel multi-target tyrosine kinase inhibitor that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret.
  • HY-12686
    5Z-7-Oxozeaenol Inhibitor >99.0%
    5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
  • HY-12047
    Ponatinib Inhibitor 98.96%
    Ponatinib is a potent, orally available multi-targeted kinase inhibitor with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-50904
    BIBF 1120 Inhibitor 99.75%
    BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
  • HY-10255A
    Sunitinib Inhibitor 99.66%
    Sunitinib is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC50 of 80 nM and 2 nM, respectively.
  • HY-10981
    Lenvatinib Inhibitor 99.69%
    Lenvatinib is an orally active, multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, and less potent against VEGFR1/Flt-1, and approximately 10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β.
  • HY-10260
    Vandetanib Inhibitor 99.89%
    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
  • HY-10255
    Sunitinib Malate Inhibitor 99.47%
    Sunitinib Malate is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC50 of 80 nM and 2 nM, respectively.
  • HY-10321
    PD173074 Inhibitor 99.55%
    PD173074 is a potent FGFR1 inhibitor with IC50 of 25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, 1000-fold selective for FGFR1 than PDGFR and c-Src.
  • HY-13342
    Apatinib Inhibitor 99.89%
    Apatinib is a selective VEGFR2 inhibitor with IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. Apatinib has no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM.
  • HY-10208
    Pazopanib Inhibitor 99.44%
    Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
  • HY-10338
    Foretinib Inhibitor 99.81%
    Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, with IC50 of 0.4 nM and 0.9 nM for Met and KDR, less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and has little activity to FGFR1 and EGFR.
  • HY-10407
    SU 5402 Inhibitor 99.23%
    SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
  • HY-10065
    Axitinib Inhibitor 99.77%
    Axitinib is a receptor kinase inhibitor of VEGFRs and, at higher doses, PDGFRs (IC50=0.1 nM for VEGFR1, 0.2 nM for VEGFR2, 0.1-0.3 nM for VEGFR3, and 1.6 nM for PDGFRβ).
Isoform Specific Products

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