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-10201
    Sorafenib
    		Inhibitor 99.92%
    Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib
  • HY-10981
    Lenvatinib
    		Inhibitor 99.61%
    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
  • HY-P9906
    Bevacizumab
    		Inhibitor ≥99.0%
    Bevacizumab, a humanized IgG1 monoclonal antibody, specifically binds to all VEGF-A isoforms with high affinity.
    Bevacizumab
  • HY-10331
    Regorafenib
    		Inhibitor 99.93%
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
    Regorafenib
  • HY-10374
    Semaxinib
    		Inhibitor 99.96%
    Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (VEGFR2/KDR/Flk-1/VEGFR2/KDR/Flk-1) with an IC50 of 1.23 μM.
    Semaxinib
  • HY-15458A
    (S)-SAR131675
    		Inhibitor 99.72%
    (S)-SAR131675 is the S-enantiomer of SAR131675 (HY-15458), a potent and selective VEGFR3/Flt-4 inhibitor and a click chemistry reagent.
    (S)-SAR131675
  • HY-169100
    Antiproliferative agent-57
    		Inhibitor
    Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC50=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues.
    Antiproliferative agent-57
  • HY-P10426
    cyclo(CLLFVY)
    		Inhibitor
    cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC50 of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers.
    cyclo(CLLFVY)
  • HY-10255A
    Sunitinib
    		Inhibitor 98.96%
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2/KDR/Flk-1 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib
  • HY-50904
    Nintedanib
    		Inhibitor 99.94%
    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/Flt-1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib
  • HY-13016
    Cabozantinib
    		Inhibitor 99.96%
    Cabozantinib is a potent and orally active inhibitor of VEGFR2/KDR/Flk-1 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
    Cabozantinib
  • HY-12047
    Ponatinib
    		Inhibitor 99.43%
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2/KDR/Flk-1, FGFR1, and Src, respectively.
    Ponatinib
  • HY-10065
    Axitinib
    		Inhibitor 99.94%
    Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, VEGFR3/Flt-4 and PDGFRβ, respectively.
    Axitinib
  • HY-B0239
    Chloramphenicol
    		Inhibitor 99.82%
    Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research.
    Chloramphenicol
  • HY-10230
    Midostaurin
    		Inhibitor 99.95%
    Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, VEGFR2/KDR/Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/Flt-1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
    Midostaurin
  • HY-10208
    Pazopanib
    		Inhibitor 99.91%
    Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib
  • HY-Y0966
    Glycine
    		Inhibitor 99.26%
    Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis.
    Glycine
  • HY-10321
    PD173074
    		Inhibitor 99.70%
    PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2/KDR/Flk-1 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.
    PD173074
  • HY-10201A
    Sorafenib Tosylate
    		Inhibitor 99.91%
    Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.
    Sorafenib Tosylate
  • HY-N0135
    Tanshinone IIA
    		Inhibitor 99.78%
    Tanshinone IIA (Tan IIA) is one of the main compositions in the root of Salvia miltiorrhiza Bunge. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2/KDR/Flk-1.
    Tanshinone IIA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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