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-10204
    OSI-930
    		Inhibitor 98.57%
    OSI-930 is an orally selective inhibitor of Kit, VEGFR2/KDR/Flk-1 and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.
    OSI-930
  • HY-119367
    ODM-203
    		Inhibitor 99.91%
    ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/Flt-4/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment.
    ODM-203
  • HY-10977A
    Tivozanib hydrochloride hydrate
    		Inhibitor 99.77%
    Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy.
    Tivozanib hydrochloride hydrate
  • HY-10408
    Ki20227
    		Inhibitor 99.17%
    Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2/KDR/Flk-1 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.
    Ki20227
  • HY-100349
    SU4312
    		Inhibitor 99.76%
    SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and VEGFR2/KDR/Flk-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, VEGFR2/KDR/Flk-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively.
    SU4312
  • HY-15992
    BIBF 1202
    		Inhibitor 99.86%
    BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2/KDR/Flk-1 kinase with an IC50 of 62 nM.
    BIBF 1202
  • HY-107145A
    Ningetinib
    		Inhibitor 99.82%
    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/KDR/Flk-1 and Axl, respectively.
    Ningetinib
  • HY-108713
    Famitinib
    		Inhibitor 98.43%
    Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis.
    Famitinib
  • HY-10336
    Brivanib (alaninate)
    		Inhibitor 99.45%
    Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2/KDR/Flk-1 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.
    Brivanib (alaninate)
  • HY-P99330
    Vanucizumab
    		Inhibitor
    Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects.
    Vanucizumab
  • HY-13302
    CP-547632
    		Inhibitor 99.16%
    CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2/KDR/Flk-1 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.
    CP-547632
  • HY-124526
    Chiauranib
    		Inhibitor 99.28%
    Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects.
    Chiauranib
  • 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-103647
    K00546
    		Inhibitor 98.08%
    K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively.
    K00546
  • HY-111138
    CZC-8004
    		Inhibitor 99.81%
    CZC-8004 (CZC-00008004), an aminopyrimidine, is a pan-kinase inhibitor. CZC-8004 can bind a range of tyrosine kinases, including EGFR and VEGFR2/KDR/Flk-1 with IC50 values of 650 and 437 nM, respectively.CZC-8004 has antitumor activity.
    CZC-8004
  • HY-10330A
    Toceranib phosphate
    		Inhibitor 98.54%
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and VEGFR2/KDR/Flk-1/VEGFR2/KDR/Flk-1, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
    Toceranib phosphate
  • HY-Y0121
    Ethyl cinnamate
    		Inhibitor 99.80%
    Ethyl cinnamate, an orally active chemical constituent of the rhizome of Kaempferia galanga, exhibits anti-cancer, nematocidal, sedative and vasorelaxant activities. Ethyl cinnamate is a fragrance ingredient used as a food flavor and additive for cosmetic products. Ethyl cinnamate is also an excellent clearing reagent for mammalian tissues. Ethyl cinnamate suppresses tumor growth through anti-angiogenesis by attenuating VEGFR2/KDR/Flk-1 signal pathway in colorectal cancer. Ethyl cinnamate inhibits the tonic contractions induced by high K+ and phenylephrine (PE) with respective IC50 values of 0.30 mM and 0.38 mM in rat aorta.
    Ethyl cinnamate
  • HY-10991
    MGCD-265 analog
    		Inhibitor 98.47%
    MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2/KDR/Flk-1 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity.
    MGCD-265 analog
  • HY-10501A
    SU14813 maleate
    		Inhibitor 99.04%
    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2/KDR/Flk-1, VEGFR1/Flt-1, PDGFRβ and KIT.
    SU14813 maleate
  • HY-103002
    SU5408
    		Inhibitor ≥98.0%
    SU5408 (VEGFR2/KDR/Flk-1 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2/KDR/Flk-1 kinase with an IC50 of 70 nM.
    SU5408
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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