2. Vías de señalización
  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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-P991628
    SSGJ-707
    		Inhibitor ≥99.0%
    SSGJ-707 (PF-08634404) is a bispecific antibody targeting VEGF and PD-1. SSGJ-707 exerts dual anti-tumor effects by neutralizing VEGF and blocking the PD-1 signaling pathway. SSGJ-707 can be combined with platinum-based chemotherapy to inhibit advanced non-small cell lung cancer (NSCLC), and its inhibitory effect is not limited by PD-L1 expression levels. In the HARMONi-2 trial, the objective response rate of SSGJ-707 correlates with the PD-L1 tumor proportion score, and the incidence of grade ≥3 adverse events is comparable to that of Inetetamab (HY-P99969). SSGJ-707 is being extensively investigated for a variety of malignancies including advanced NSCLC, colorectal cancer and small cell lung cancer.
    SSGJ-707
  • HY-N0819
    Raddeanin A
    		Inhibitor 98.68%
    Raddeanin A is an oleanane-type triterpenoid saponin with oral activity. Raddeanin A inhibits SRC, mTOR, JNK, VEGFR2, NLRP3 inflammasome, Wnt/β-catenin, Wee1, PI3K/AKT signaling pathway, MAPK/ERK signaling pathway, AR-FL, AR-Vs, and downregulates the expression of p-PI3K and p-AKT. Raddeanin A inhibits osteoclast formation, bone resorption, osteolysis, cancer cell invasion, migration, proliferation, angiogenesis and epithelial-mesenchymal transition, while induces apoptosis, cell cycle arrest, ROS production, immunogenic cell death and dendritic cell maturation. Raddeanin A improves blood-retinal barrier function, alleviates inflammation, regulates the tumor microenvironment, and enhances the activity of anti-PD-1 antibody. Raddeanin A is applicable to the research of breast cancer-associated osteolysis, human osteosarcoma, colorectal cancer, glioblastoma, Alzheimer's disease, cholangiocarcinoma, melanoma, non-small cell lung cancer, castration-resistant prostate cancer and multiple myeloma.
    Raddeanin A
  • HY-10406
    Talmapimod
    		Inhibitor 98.68%
    Talmapimod (SCIO-469) is an orally active and selective inhibitor of p38α MAPK with an IC50 of 9 nM. Talmapimod inhibits the secretion of inflammatory factors (such as TNFα, IL-1β, IL-6, and VEGF) by suppressing the p38α MAPK pathway, and it also inhibits angiogenesis and osteoclast activation. Talmapimod inhibits the growth of multiple myeloma cells and induces apoptosis. Talmapimod can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome).
    Talmapimod
  • 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-109561
    Pegaptanib sodium
    		Inhibitor
    Pegaptanib sodium is an RNA aptamer with polyethylene glycol modifications, which is directed against vascular endothelial growth factor (VEGF)-165. Pegaptanib could be used for the study of neovascular age-related macular degeneration (AMD) .
    Pegaptanib sodium
  • 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-N7700A
    Guluronic acid sodium
    		Inhibitor 98.0%
    Guluronic acid (G2013) sodium is an orally active oxidative stress regulator and anti-inflammatory agent that exerts pharmacological effects by down-regulating various pro-inflammatory and oxidative stress-related genes (such as TLR4, NF-κB, iNOS, etc.) and inhibiting the activities of COX-2, MMPs and VEGF. Low-dose Guluronic acid sodium up-regulates the expression of immunoregulatory genes SHIP1 and SOCS1, thereby effectively inhibiting cancer-related inflammation, tumor angiogenesis, cell adhesion and metastasis, while reducing the accumulation of immunosuppressive cells. Guluronic acid sodium significantly prolongs the survival time of tumor-bearing hosts within a concentration range without direct cytotoxicity, demonstrating favorable safety. Guluronic acid sodium has involved in the research of multiple sclerosis, ankylosing spondylitis, breast cancer and other inflammatory diseases.
    Guluronic acid sodium
  • HY-10203
    Vatalanib
    		Inhibitor 99.93%
    Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
    Vatalanib
  • 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
  • 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-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-10330
    Toceranib
    		Inhibitor
    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 Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
    Toceranib
  • 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-18711A
    SCR-1481B1
    		Inhibitor 99.95%
    SCR-1481B1 (Metatinib anhydrous; c-Met inhibitor 2) is an inhibitor of the N-terminal fragment of Gasdermin D (GSDMD), with an IC50 of 1.04 μM and a Ka of 0.42 μM in mice. SCR-1481B1 effectively blocks GSDMD-NT oligomerization and pore formation, inhibits GSDMD-mediated pyroptosis (Pyroptosis), preserves mitochondrial integrity, and reduces proinflammatory cytokine secretion. SCR-1481B1 also inhibits angiogenesis, exerts GSDMD-independent antitumor effects, and enhances the infiltration of antitumor immune cells. SCR-1481B1 is also an inhibitor targeting to c-MET and VEGFR2, can be used in studies related to melanoma and sepsis.
    SCR-1481B1
  • HY-N5074
    Terrestrosin D
    		Activator 99.30%
    Terrestrosin D is an orally active apoptosis inducer. Terrestrosin D induces cell cycle arrest at the G1 and S phases, reduces mitochondrial membrane potential, and inhibits the growth of cancer cells and endothelial cells. Terrestrosin D is studied in castration-resistant prostate cancer and pulmonary fibrosis.
    Terrestrosin D
  • HY-112452
    SU11652
    		Inhibitor 99.18%
    SU11652 is a potent receptor tyrosine kinase (RTK) inhibitor. SU11652 also inhibits several members of the split kinase family of RTKs, including VEGFR, FGFR, PDGFR, and Kit. SU11652 can be uesd for spontaneous cancers expressing Kit mutations research.
    SU11652
  • 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 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-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-N2575
    Hypocrellin A
    		Inhibitor 99.73%
    Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml).
    Hypocrellin A
  • 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
Cat. No. Nombre del producto / Synonyms Species Source
Cat. No. Nombre del producto / Synonyms Application Reactivity
VEGFR Isoform Comparison

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