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-19357
    E3330
    Inhibitor 99.34%
    E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities.
    E3330
  • HY-15458
    SAR131675
    Inhibitor 99.76%
    SAR131675 is a potent and selective VEGFR3/Flt-4 inhibitor with an IC50 of 23 nM. SAR131675 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SAR131675
  • HY-B0223
    Albendazole
    Inhibitor 99.00%
    Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells.
    Albendazole
  • HY-10201S
    Sorafenib-d3
    Inhibitor 99.57%
    Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
    Sorafenib-d<sub>3</sub>
  • HY-12297
    Sulfatinib
    Inhibitor 98.65%
    Sulfatinib (Surufatinib) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/Flt-1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.
    Sulfatinib
  • HY-D0803
    Thymoquinone
    Inhibitor 99.59%
    Thymoquinone is an orally active natural product isolated from N. sativa Thymoquinone down-regulates the VEGFR2-PI3K-Akt pathway. Thymoquinone has antioxidant, anti-inflammatory, anticancer, antiviral, anticonvulsant, antifungal, antiviral, antiangiogenic activity and hepatoprotective effects. Thymoquinone can be used to study Alzheimer's disease, cancer, cardiovascular disease, infectious disease and inflammation .
    Thymoquinone
  • HY-P9906A
    Bevacizumab (PBS)
    Inhibitor 98.94%
    Bevacizumab, a humanized IgG1 monoclonal antibody, specifically binds to all VEGF-A isoforms with high affinity.
    Bevacizumab (PBS)
  • HY-14574
    PF-03814735
    Inhibitor 99.58%
    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-138696
    Zanzalintinib
    Inhibitor 99.73%
    Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2/KDR/Flk-1, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research.
    Zanzalintinib
  • HY-108766
    Ponatinib hydrochloride
    Inhibitor 99.55%
    Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib 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 hydrochloride
  • HY-10331A
    Regorafenib monohydrate
    Inhibitor 99.96%
    Regorafenib (BAY 73-4506) monohydrate 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 monohydrate shows very robust antitumor and antiangiogenic activity.
    Regorafenib monohydrate
  • HY-12044
    Cabozantinib S-malate
    Inhibitor 99.90%
    Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2/KDR/Flk-1, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
    Cabozantinib S-malate
  • HY-13308
    Regorafenib Hydrochloride
    Inhibitor 99.58%
    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/Flt-1/2/3, 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-15002
    AST 487
    Inhibitor 99.42%
    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-15511
    Tyrphostin A9
    Inhibitor 99.87%
    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-13034
    Gandotinib
    Inhibitor 99.82%
    Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
    Gandotinib
  • HY-108801
    Aflibercept
    Inhibitor
    Aflibercept (VEGF Trap) is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease.
    Aflibercept
  • HY-122704A
    Surfen dihydrochloride
    Inhibitor ≥99.0%
    Surfen dihydrochloride is a potent HS (heparan sulfate) antagonist. Surfen binds to glycosaminoglycans. Surfen neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins. Surfen affects sulfation of heparin and inhibits degradation by heparin lyases. Surfen inhibits FGF2 binding and signaling. Surfen inhibits cell attachment, and virus infection.
    Surfen dihydrochloride
  • HY-10032
    PF 477736
    Inhibitor 99.21%
    PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2/KDR/Flk-1, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
    PF 477736
  • HY-B0791
    Altiratinib
    Inhibitor 98.05%
    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/KDR/Flk-1, FLT3, Trk1, Trk2, and Trk3 respectively.
    Altiratinib
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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