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-152120
    (±)-Aiphanol
    		Inhibitor
    (±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak.(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 μM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active.
    (±)-Aiphanol
  • HY-173124
    CDK2/FLT4/PDGFRA-IN-1
    		Inhibitor
    CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3) and PDGFRA, with IC50s of 1.672, 0.554, and 0.629 μM, respectively. CDK2/FLT4/PDGFRA-IN-1 exhibits potent antiproliferative effects against cancer cells (lung EBC-1, pancreatic ductal adenocarcinoma AsPC-1, colorectal HT-29 cells). CDK2/FLT4/PDGFRA-IN-1 can also induce apoptosis in cancer cells.
    CDK2/FLT4/PDGFRA-IN-1
  • HY-168104
    VEGFR-2-IN-55
    		Inhibitor
    VEGFR-2-IN-55 (Compound 30) is a potent VEGFR-2 kinase inhibitor with an IC50 value of 1.24 nM . VEGFR-2-IN-55 has antitumor activity.
    VEGFR-2-IN-55
  • HY-157546
    VEGFR-2-IN-40
    		Inhibitor
    VEGFR-2-IN-40 is a VEGFR-2 inhibitor. VEGFR-2-IN-40 boosts early and late apoptosis. VEGFR-2-IN-40 decreases the levels immunomodulatory proteins TNF-α and IL-6 while showing a four-fold rise in an apoptotic marker caspase-3.
    VEGFR-2-IN-40
  • HY-146884
    MET kinase-IN-3
    		Inhibitor
    MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines.
    MET kinase-IN-3
  • HY-171992
    COX-2-IN-55
    		Inhibitor 99.20%
    COX-2-IN-55 (compound 1) is an orally active, Celecoxib (HY-14398)-based analog with broad-spectrum anticancer activity and weak COX-2 inhibition. COX-2-IN-55 specifically inhibits SERCA2, increases caspase-3 cleavage and DR5 levels, thereby activating GRP78 and inhibiting the development of triple-negative breast cancer (TNBC). COX-2-IN-55 can also downregulate the levels of angiogenic markers VEGF-α and IL-8, inhibiting the formation of microvessels.
    COX-2-IN-55
  • HY-160685
    GW809897X
    		Inhibitor
    GW809897X is a dual inhibitor of Fluc and VEGFR with IC50 of 0.58 μM and 65 nM, respectively. GW809897X is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential impact on Fluc reporter assays.
    GW809897X
  • HY-158328A
    CA IX/VEGFR-2-IN-2
    		Inhibitor
    CA IX/VEGFR-2-IN-2 (compound 5e) is a dual-targeted inhibitor. CA IX/VEGFR-2-IN-2 shows strong inhibitory effects on both CA IX (Ki=3.1 μM) and VEGFR-2 (IC50=32.1 nM). CA IX/VEGFR-2-IN-2 can be used for the study of pancreatic (PANC1), breast cancer (MCF7) and prostate cancer (PC3) .
    CA IX/VEGFR-2-IN-2
  • HY-177612B
    AGN-745 sodium scrambled negative control
    		Inhibitor
    AGN-745 sodium scrambled negative control is the sequence scrambled negative control of AGN-745 sodium.
    AGN-745 sodium scrambled negative control
  • HY-P991132
    Efclarofusp alfa
    		Inhibitor
    Efclarofusp alfa is a CHO-expressed humanized antibody consisting of VEGFR-1 and VEGFR-2 regions fused to human IgG1 Fc. Efclarofusp alfa is an angiogenesis inhibitor.
    Efclarofusp alfa
  • HY-183090
    EGFR/VEGFR2-IN-13
    		Inhibitor
    EGFR/VEGFR2-IN-13 is a multi-target inhibitor, with an IC50 of 0.98 µM against VEGFR-2, 1.01 µM against EGFR, and 1.94 µM against topoisomerase II. EGFR/VEGFR2-IN-13 induces cell cycle arrest and apoptosis in tumor cells. As an anticancer agent, EGFR/VEGFR2-IN-13 exhibits cytotoxicity against cancer cells. EGFR/VEGFR2-IN-13 can be used in research related to breast cancer, colon cancer, and liver cancer.
    EGFR/VEGFR2-IN-13
  • HY-139822
    VEGFR-2-IN-10
    		Inhibitor
    VEGFR-2-IN-10 exhibits increased antiangiogenic potency (IC50 = 0.7 μM) against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects.
    VEGFR-2-IN-10
  • HY-179098
    Multi-target kinase-IN-8
    		Inhibitor
    Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf V600E (IC50 = 0.078 µg/mL), c-Met (IC50 = 0.405 µg/mL), Pim-1 (IC50 = 1.053 µg/mL), EGFR WT (IC50 = 0.177 µg/mL), VEGFR-2 (IC50 = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly used in cancer research.
    Multi-target kinase-IN-8
  • HY-149675
    VEGFR-2/c-Met-IN-2
    		Inhibitor
    VEGFR-2/c-Met-IN-2 (compound 3e) is a VEGFR-2/c-Met inhibitor, with IC50 values of 83 and 48 nM, respectively. VEGFR-2/c-Met-IN-2 exhibits cytotoxic activity against HCT-116 cell line (IC50: 3.403 µM).
    VEGFR-2/c-Met-IN-2
  • HY-168655
    EGFR/VEGFR2-IN-3
    		Inhibitor
    EGFR/VEGFR2-IN-3 (compound 9) is a potent EGFR and VEGFR-2 inhibitor with IC50 values of 0.129, 0.142, 3.428 µM for EGFR, VEGFR-2, COX-2, respectively. EGFR/VEGFR2-IN-3 shows cytotoxicity. EGFR/VEGFR2-IN-3 induces apoptosis and cell cycle arrest at G2/M phase.
    EGFR/VEGFR2-IN-3
  • HY-183684
    RET-IN-33
    		Inhibitor
    RET-IN-33 is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer.
    RET-IN-33
  • HY-116452
    YLT192
    		Inhibitor
    YLT192 is an orally active and highly bioavailable VEGFR2 inhibitor with potent anti-angiogenic activity and anti-tumor efficacy. YLT192 significantly inhibited the kinase activity of VEGFR2 and inhibited the proliferation, migration, invasion and tube formation of human umbilical cord vascular endothelial cells. YLT192 also inhibited VEGF-induced VEGFR2 phosphorylation and its downstream signaling regulators. YLT192 also showed the ability to inhibit angiogenesis in vivo in zebrafish embryo models and alginate-coated tumor cell experiments. YLT192 can directly inhibit the proliferation of cancer cells and induce their apoptosis.
    YLT192
  • HY-107144
    LY2457546
    		Inhibitor
    LY2457546 is a potent and orally active multi-targeted anti-angiogenic tyrosine kinases inhibitor. LY2457546 demonstrates potent activity against targets that include VEGFR2, PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. LY2457546 can be used for the research of cancer, such as leukemia.
    LY2457546
  • HY-144803
    VEGFR-2-IN-16
    		Inhibitor
    VEGFR-2-IN-16 (Compound 15b) is a potent VEGFR-2 inhibitor with an IC50 of 86.36 nM. VEGFR-2-IN-16 shows antitumor activities.
    VEGFR-2-IN-16
  • HY-18333
    EG00229
    		Inhibitor
    EG00229 is an inhibitor for VEGF-A and NRP1 interaction with an IC50 of 8 μM. EG00229 inhibits the migration of HUVECS and the phosphorylation of VEGFR2 in endothelial cells. EG00229 exhibits cytotoxicity in cancer cell A549.
    EG00229
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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