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-10248
    RAF265
    Inhibitor 99.80%
    RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.
    RAF265
  • HY-15511
    Tyrphostin A9
    Inhibitor 99.91%
    Tyrphostin A9, a PDGFR inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. Tyrphostin A9 has anti-influenza virus activities.
    Tyrphostin A9
  • HY-15002
    AST 487
    Inhibitor 98.90%
    AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
    AST 487
  • HY-18303
    AMG-47a
    Inhibitor 99.19%
    AMG-47a is an orally active, ATP-competitive Lck inhibitor (IC50=0.2 nM). AMG-47a inhibits VEGF2, p38α, p38α, Jak3, MLR, and IL-2 with IC50 of 1 nM, 3 nM, 72 nM, 30 nM, and 21 nM, respectively. AMG-47a reduces T cell activation and the production of cytokines such as TGF-β, exerting anti-inflammatory and anti-fibrotic activities. AMG-47a can be used in the research of autoimmune diseases, pulmonary fibrosis, and KRAS mutation-associated cancers[1][2][3].
    AMG-47a
  • HY-B0791
    Altiratinib
    Inhibitor 99.29%
    Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.
    Altiratinib
  • HY-124593
    PTC299
    Inhibitor 99.89%
    PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.
    PTC299
  • HY-14574
    PF-03814735
    Inhibitor 99.45%
    PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
    PF-03814735
  • HY-N0316
    Mollugin
    Inhibitor 99.48%
    Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway.
    Mollugin
  • HY-10517
    Orantinib
    Inhibitor 99.29%
    Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
    Orantinib
  • HY-16135
    CEP-11981
    Inhibitor 99.18%
    CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects.
    CEP-11981
  • HY-10372
    PP121
    Inhibitor 99.51%
    PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.
    PP121
  • HY-P990148
    Anti-Mouse VEGF-A Antibody (2G11-2A05)
    Inhibitor
    Anti-Mouse VEGF-A Antibody (2G11-2A05) is a rat-derived IgG2a κ type antibody inhibitor, tragrting to mouse VEGF-A with high affinity. Anti-Mouse VEGF-A Antibody (2G11-2A05) shows good anti-tumor effect in gastric cancer xenograft models.
    Anti-Mouse VEGF-A Antibody (2G11-2A05)
  • HY-10337
    Brivanib
    Inhibitor 99.92%
    Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
    Brivanib
  • HY-P3325
    P8RI
    Agonist
    P8RI (D-P8RI) is a biomimetic peptide of CD31 and a CD31 agonist. P8RI binds to the juxtamembrane amino acid sequence of the ectodomain of CD31, shows an immunosuppressive effect through restoration of the CD31 inhibitory pathway.
    P8RI
  • HY-B0263
    Thiabendazole
    Inhibitor 99.94%
    Thiabendazole is an orally available benzimidazole fungicide with repellent and anticancer activities. Thiabendazole can result in developmental malformations. Thiabendazole can be used for modeling.
    Thiabendazole
  • HY-12038
    Ki8751
    Inhibitor 99.76%
    Ki8751 is a potent VEGFR2 inhibitor with an IC50 of 0.9 nM.
    Ki8751
  • HY-109019
    Vorolanib
    Inhibitor 99.78%
    Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
    Vorolanib
  • HY-13308
    Regorafenib Hydrochloride
    Inhibitor 99.58%
    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) 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.
    Regorafenib Hydrochloride
  • HY-10228
    Motesanib
    Inhibitor 99.96%
    Motesanib (AMG 706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.
    Motesanib
  • HY-13068
    Golvatinib
    Inhibitor 99.86%
    Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
    Golvatinib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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