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-P10833
    C-VGB3
    		Antagonist
    C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer.
    C-VGB3
  • HY-181097
    EGFR-IN-192
    		Inhibitor
    EGFR-IN-192 is an anticancer agent. EGFR-IN-192 inhibits EGFR (IC50: 0.12 μM), downregulates the HIF-VEGF and PI3K/AKT/mTOR pathways, upregulates the tumor suppressor gene PTEN, and induces cell cycle arrest and apoptosis in tumor cells. EGFR-IN-192 exhibits antitumor activity and can be used in tumor research.
    EGFR-IN-192
  • HY-158233
    Apoptotic agent-4
    		Inhibitor
    Apoptotic agent-4 (Compound 9) is a apoptosis inducer. Apoptotic agent-4 inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 inhibits cancer cell proliferation and arrests the cell at both the G2/M and Pre-G1 phases.
    Apoptotic agent-4
  • HY-P11649
    NYLTHRQ
    		Inhibitor
    NYLTHRQ is a peptide. NYLTHRQ specifically blocks the interaction between sVEGFR1-i13 and β1 integrin, and inhibits the activation of VEGFR1 and VEGFR2. NYLTHRQ inhibits cancer cell proliferation. NYLTHRQ can be used in the research of tumors such as lung squamous cell carcinoma.
    NYLTHRQ
  • HY-164387A
    Sutetinib maleate
    		Inhibitor
    Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo.
    Sutetinib maleate
  • HY-130133
    DHW-221
    		Inhibitor
    DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research.
    DHW-221
  • HY-149407
    Multi-kinase-IN-4
    		Inhibitor
    Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
    Multi-kinase-IN-4
  • HY-144796
    VEGFR-2-IN-15
    		Inhibitor
    VEGFR-2-IN-15 (Compound 14b) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-15 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis.
    VEGFR-2-IN-15
  • HY-177612
    AGN-745
    		Inhibitor
    AGN-745 is a chemically modified siRNA targeted to VEGFR-1. It is used for the study of Macular degeneration.
    AGN-745
  • HY-169409
    VEGFR-2-IN-59
    		Inhibitor
    VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property.
    VEGFR-2-IN-59
  • HY-182005
    EGFR/VEGFR2-IN-12
    		Inhibitor
    EGFR/VEGFR2-IN-12 is a dual EGFR/VEGFR2 inhibitor, with an IC50 value of 64 nM against human EGFR and an IC50 value of 74 nM against human VEGFR2. EGFR/VEGFR2-IN-12 inhibits the phosphorylation of EGFR and VEGFR2, induces cell cycle arrest at the G1/S phase, activates apoptotic pathways, promotes PARP-1 cleavage, exhibits low micromolar antiproliferative activity, and shows much higher selectivity for cancer cells than normal cells. EGFR/VEGFR2-IN-12 is applicable for cancer-related research.
    EGFR/VEGFR2-IN-12
  • HY-P990542
    Anti-VEGFR2/KDR/CD309 Antibody
    		Inhibitor
    Anti-VEGFR2/KDR/CD309 Antibody is a humanized antibody expressed in CHO, targeting VEGFR2/KDR/CD309. The Anti-VEGFR2/KDR/CD309 Antibody is equipped with muIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For isotype control of the Anti-VEGFR2/KDR/CD309 Antibody, refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-VEGFR2/KDR/CD309 Antibody
  • HY-161859
    VEGFR-2/STAT-3-IN-1
    		Inhibitor
    VEGFR-2/STAT-3-IN-1 (Compound 9f) is a dual inhibitor for VEGFR-2 (IC50=26.3 nM) and STAT-3 (IC50=5.63 nM). VEGFR-2/STAT-3-IN-1 inhibits the proliferation of cancer cells PANC1 and PC3 with IC50 of 0.14 and 0.10 µM. VEGFR-2/STAT-3-IN-1 induces apoptosis in PC3.
    VEGFR-2/STAT-3-IN-1
  • HY-175297
    EGFR T790M/VEGFR-2-IN-1
    		Inhibitor
    EGFR T790M/VEGFR-2-IN-1 (Compound 6) is a dual EGFR T790M mutant (IC50=0.26 μM) and VEGFR-2 (IC50=0.95 μM) inhibitor. EGFR T790M/VEGFR-2-IN-1 blocks tumor cell proliferation and angiogenesis signaling pathways. EGFR T790M/VEGFR-2-IN-1 exhibits potent cytotoxicity against multiple cancer cell lines (HCT116, MCF-7, HepG2, A549; IC50=5.35-9.90 μM). EGFR T790M/VEGFR-2-IN-1 is promising for research of non-small cell lung cancer and solid tumors.
    EGFR T790M/VEGFR-2-IN-1
  • HY-10981S2
    Lenvatinib-15N,d4
    		Inhibitor 98.01%
    Lenvatinib-15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). 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-<sup>15</sup>N,d<sub>4</sub>
  • HY-182639
    AM9928
    		Inhibitor
    AM9928 is a monoacylglycerol lipase (MAGL) inhibitor with IC50 and Ki values of 8.9 nM and 7.3 nM, respectively. AM9928 blocks the adhesion and migration of triple-negative breast cancer (TNBC) cells, and inhibits the secretion of IL-6, IL-8 and VEGF-A by TNBC cells. AM9928 suppresses the activation of human brain microvascular endothelial cells (HBMECs) induced by TNBC-derived exosomes, and reduces the secretion of IL-8 and VEGF-A by HBMECs. AM9928 attenuates changes in blood-brain barrier permeability, inhibits tumor growth in the mammary fat pad, and reduces brain colonization of TNBC. AM9928 can be used in studies related to triple-negative breast cancer.
    AM9928
  • HY-P10521
    Apolipoprotein KV domain (67-77)
    		Inhibitor
    Apolipoprotein KV domain (67-77) is an 11-amino acid peptide identified from the KV domain of human apolipoprotein a (ApoA) with antiangiogenic and antitumor activities. Apolipoprotein KV domain (67-77) targets the angiogenic c-Src/ERK pathway by blocking activation signals received from vascular endothelial growth factor (VEGF). Apolipoprotein KV domain (67-77) can be used in cancer research.
    Apolipoprotein KV domain (67-77)
  • HY-142518
    EGFR-IN-26
    		Inhibitor
    EGFR-IN-26 is a EGFR inhibitor extracted from patent WO2019162323A1 compound I-028. EGFR-IN-26 can be used for the research of cancer.
    EGFR-IN-26
  • HY-181793
    VEGFR2/HDAC-IN-1
    		Inhibitor
    VEGFR2/HDAC-IN-1 is a dual selective enzymatic inhibitor of VEGFR2 kinase and HDAC6 with oral activity. VEGFR2/HDAC-IN-1 has an IC50 of 19.19 nM for VEGFR2 and 0.165 μM for HDAC6. VEGFR2/HDAC-IN-1 increases α-tubulin acetylation, exerts antiproliferative effects, inhibits tumor growth, and exhibits antiangiogenic activity. VEGFR2/HDAC-IN-1 can be used for the research of colorectal carcinoma and hepatocellular carcinoma.
    VEGFR2/HDAC-IN-1
  • HY-155694
    hCA/VEGFR-2-IN-1
    		Inhibitor
    hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual Carbonic Anhydrase(CA) IX/XII with Ki values of 4.7 nM and 8.3 nM for hCA XII and hCA IX, respectively. hCA/VEGFR-2-IN-1 (compound 13a) is a potent VEGFR-2 inhibitor with IC50 values 26.3 nM. hCA/VEGFR-2-IN-1 has anticancer activity.
    hCA/VEGFR-2-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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