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-172272A
    DSPE-PEG2000-Mal-Cys-ATWLPPR
    DSPE-PEG2000-A7R is a PEG compound which composed of DSPE and a tumor vascular targeting peptide (A7R). A7R exhibits high affinity and specificity for VEGFR-2, which is overexpressed in various tumors.
    DSPE-PEG2000-Mal-Cys-ATWLPPR
  • HY-147926
    VEGFR-2-IN-28
    		Inhibitor
    VEGFR-2-IN-28 (compound 12c) is a potent VEGFR-2 inhibitor with IC50 value of 0.83 µM. VEGFR-2-IN-28 induces apoptosis and has anticancer activity.
    VEGFR-2-IN-28
  • HY-14979A
    ML786 dihydrochloride
    		Inhibitor
    ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.
    ML786 dihydrochloride
  • HY-151459
    VEGFR-2/DHFR-IN-2
    		Inhibitor
    VEGFR-2/DHFR-IN-2 (compound 5b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.623 and 9.085 μM, respectively. VEGFR-2/DHFR-IN-2 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 3.59-8.38 μM. VEGFR-2/DHFR-IN-2 can be used for the research of cancer.
    VEGFR-2/DHFR-IN-2
  • HY-10260S2
    Vandetanib-13C6
    		Inhibitor
    Vandetanib-13C6 is a 13C labeled Vandetanib (HY-10260). Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
    Vandetanib-<sup>13</sup>C<sub>6</sub>
  • HY-172112
    VEGFR-2-IN-64
    		Inhibitor
    VEGFR-2-IN-64 (Compound 28) is the inhibitor for VEGFR2 with IC50 of 27.8 nM. VEGFR-2-IN-64 inhibits the proliferation of cancer cell A549, T-47D and Caco-2, exhibits anti-migration and anti-cloning activities in cell T-47D, induces apoptosis in T-47D.
    VEGFR-2-IN-64
  • HY-153158
    VEGFR2-IN-3
    		Inhibitor
    VEGFR2-IN-3 (compound 385) is a potent VEGFR2 inhibitor.
    VEGFR2-IN-3
  • HY-162887
    VEGFR-2-IN-53
    		Inhibitor
    VEGFR-2-IN-53 (Compound 15w) is a VEGFR-2 inhibitor with an IC50 of 4.34 μM. VEGFR-2-IN-53 induces apoptosis by inhibiting VEGFR-2 activity and preventing cell migration, thereby exhibiting anti-angiogenic effects. The IC50 value of VEGFR-2-IN-53 for inhibiting MCF-7 cell growth is 3.87 μM. VEGFR-2-IN-53 can be used in cancer research.
    VEGFR-2-IN-53
  • HY-P3995
    Scospondistatin
    Scospondistatin is an anti-angiogenic peptide that can inhibit proliferation and migration of human umbilical vein endothelial cells in vitro.
    Scospondistatin
  • HY-162557
    VEGFR-2-IN-45
    		Inhibitor
    VEGFR-2-IN-45 (compound 3j) is a potent inhibitor of VEGFR-2, with the IC50 of 0.2 μM. VEGFR-2-IN-45 plays an important role in cancer research.
    VEGFR-2-IN-45
  • HY-15268
    PP487
    		Inhibitor
    PP487 is a selective dual inhibitor of Tyrosine kinase/PI3-K, with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used in cancer research.
    PP487
  • HY-178942
    EGFR/VEGFR2-IN-9
    		Inhibitor
    EGFR/VEGFR2-IN-9 (Compound 9b) is an inhibitor of VEGFR-2 (IC50 = 1.325 μM) and EGFR (IC50 = 1.891 μM). EGFR/VEGFR2-IN-9 significantly inhibits the proliferation of multiple cancer cell lines, particularly leukemia cells. EGFR/VEGFR2-IN-9 upregulates the expression levels of Bax, caspase-3, and p53, while downregulating the expression of Bcl-2. EGFR/VEGFR2-IN-9 induces apoptosis and arrests the cell cycle in the G1 phase. EGFR/VEGFR2-IN-9 can be used to investigate anti-tumor angiogenesis and multi-drug resistant cancers.
    EGFR/VEGFR2-IN-9
  • HY-W751179
    Midostaurin-13C6
    Midostaurin-13C6 (PKC412-13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
    Midostaurin-<sup>13</sup>C<sub>6</sub>
  • HY-155242
    VEGFR-2-IN-36
    		Inhibitor
    VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM).
    VEGFR-2-IN-36
  • HY-18318
    Takeda-6D
    		Inhibitor 99.41%
    Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity.
    Takeda-6D
  • HY-122010
    NVP-AAD777
    		Inhibitor
    NVP-AAD777 is a specific inhibitor of VEGFR-2, demonstrated in vivo by its effective suppression of phospho-VEGFR-2 (Tyr1175) signaling in rat lung tissues. Unlike the nonspecific VEGFR inhibitor SUG-5416, NVP-AAD777 did not induce emphysematous changes in the lungs after three weeks of treatment, even when combined with exposure to cigarette smoke. Additionally, there were no alterations observed in vascular density compared to control animals. This indicates NVP-AAD777's targeted action in inhibiting VEGFR-2 without adverse pulmonary effects, highlighting its potential therapeutic utility in managing conditions associated with aberrant VEGFR-2 signaling.
    NVP-AAD777
  • HY-162064
    T-1-MBHEPA
    		Inhibitor
    T-1-MBHEPA is a potent inhibitor of VEGFR-2, with the IC50 value of 0.121±0.051 μM. T-1-MBHEPA has anti-tumor and anti-angiogenic effect.
    T-1-MBHEPA
  • HY-117991
    DW10075
    		Inhibitor
    DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
    DW10075
  • HY-133806
    Fumarranol
    Fumarranol, a Fumagillin (HY-B0751) analogue, is a selective type 2 methionine aminopeptidase (MetAP2) inhibitor with a human IC50 of 3.2 μM. Fumarranol inhibits proliferation of bovine aortic endothelial cells and inhibits angiogenesis in a mouse matrigel plug model. Fumarranol can be used for the researches of cancer, diabetic retinopathy, age-related macular degeneration.
    Fumarranol
  • HY-N0545S
    Taurocholic acid-13C2,15N sodium
    		Agonist
    Taurocholic acid-13C2,15N (sodium) is the 13C- and 15N- labeled Taurocholic acid (sodium).
    Taurocholic acid-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N sodium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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