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-N6794
    10Z-Hymenialdisine
    Inhibitor
    10Z-Hymenialdisine ((Z)-Hymenialdisine) is a natural bioactive pyrrole alkaloid. 10Z-Hymenialdisine is a pan kinase inhibitor, and has anticancer activities.
    10Z-Hymenialdisine
  • HY-10065S1
    Axitinib-d3
    98.03%
    Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
    Axitinib-d<sub>3</sub>
  • HY-50904S1
    Nintedanib-13C,d3
    Inhibitor ≥99.0%
    Nintedanib-13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
    Nintedanib-<sup>13</sup>C,d<sub>3</sub>
  • HY-100315
    XL 999
    Inhibitor 99.01%
    XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC50 values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer.
    XL 999
  • HY-18926
    VEGFR2-IN-7
    Inhibitor 99.79%
    VEGFR2-IN-7 (compound E) is an inhibitor of VEGFR2. VEGFR2-IN-7 can used in study cancers.
    VEGFR2-IN-7
  • HY-13016R
    Cabozantinib (Standard)
    Inhibitor
    Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
    Cabozantinib (Standard)
  • HY-137967
    Genistein 7-β-D-Glucuronide
    98.76%
    Genistein 7-β-D-Glucuronide is a natural product. Genistein 7-β-D-Glucuronide inhibits tubulogenesis and endothelial migration[1].
    Genistein 7-β-D-Glucuronide
  • HY-15769
    WHI-P180
    Inhibitor 99.84%
    WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
    WHI-P180
  • HY-P99905
    Efdamrofusp alfa
    99.89%
    Efdamrofusp alfa is a bispecific fusion protein. Efdamrofusp alfa is capable of neutralizing both VEGF isoforms and C3b/C4b. Efdamrofusp alfa can be used for the research of neovascular age-related macular degeneration (nAMD) and other complement-related ocular conditions.
    Efdamrofusp alfa
  • HY-21289
    SU5205
    Inhibitor 98.02%
    SU5205 is an inhibitor of VEGFR2 (FLK-1), with an IC50 of 9.6 μM.
    SU5205
  • HY-21292
    SU5214
    Inhibitor ≥98.0%
    SU5214 is a potent VEGFR2 inhibitor extracted from patent US5834504A, SU5214, has IC50s of 14.8 µM (FLK-1) and 36.7 µM (EGFR), respectively.
    SU5214
  • HY-W800162
    VEGFR-2-IN-37
    Inhibitor 99.00%
    VEGFR-2-IN-37 (compound 12) is an inhibitor of VEGFR-2. The inhibition rate at 200 μM was approximately 56.9 μM. VEGFR-2-IN-37 is a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation.
    VEGFR-2-IN-37
  • HY-148040
    VEGFR-2-IN-29
    Inhibitor 99.36%
    VEGFR-2-IN-29 (Compound 5) is a VEGFR-2 inhibitor with an IC50 of 16.5 nM.
    VEGFR-2-IN-29
  • HY-160811
    hVEGF-IN-3
    Inhibitor 99.56%
    hVEGF-IN-3 (compound 9) is a potent hVEGF inhibitor. hVEGF-IN-3 inhibits HT-29, MCF-7, and HEK-293 cells proliferation with IC50s of 61, 142, and 114 μM.
    hVEGF-IN-3
  • HY-107417
    Hypothemycin
    Inhibitor ≥98.0%
    Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
    Hypothemycin
  • HY-19897
    4SC-203
    Inhibitor 98.98%
    4SC-203 is a potent multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively FLT3/STK1, FLT3 mutated forms, and VEGFRs.
    4SC-203
  • HY-18317
    JNJ-38158471
    Inhibitor
    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
    JNJ-38158471
  • HY-116116
    Tafetinib
    Inhibitor
    Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.
    Tafetinib
  • HY-10981S
    Lenvatinib-d4
    Inhibitor 99.59%
    Lenvatinib-d4 is the deuterium labeled Lenvatinib. 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-d<sub>4</sub>
  • HY-108444
    (Z)-FeCP-oxindole
    Inhibitor 99.62%
    (Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM.
    (Z)-FeCP-oxindole
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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