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-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-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-10207
    Dovitinib lactate
    Inhibitor 99.75%
    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα, respectively.
    Dovitinib lactate
  • HY-13302B
    CP-547632 hydrochloride
    Inhibitor 99.79%
    CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.
    CP-547632 hydrochloride
  • HY-12423
    Pamufetinib
    Inhibitor 98.28%
    Pamufetinib (TAS-115) is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
    Pamufetinib
  • HY-147243
    Ansornitinib
    Inhibitor 98.23%
    Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.
    Ansornitinib
  • HY-13342AS
    Apatinib-d8 free base
    Apatinib-d8 (free base) is the deuterium labeled Apatinib free base. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ.
    Apatinib-d<sub>8</sub> free base
  • HY-13785
    ZM 306416
    Inhibitor 99.80%
    ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.
    ZM 306416
  • HY-147133
    VEGFR2-IN-2
    Inhibitor 99.26%
    VEGFR2-IN-2 (compound 6e) is a potent and selective VEGFR2 inhibitor with an IC50 of 19.32 nM. VEGFR2-IN-2 can be used for researching
    VEGFR2-IN-2
  • HY-10065S1
    Axitinib-d3
    98.07%
    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-16025
    EOC317
    Inhibitor 98.01%
    EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.
    EOC317
  • HY-P5107
    Low molecular weight protamine
    Inhibitor 98.07%
    Low molecular weight protamine (LMWP;TDSP5) is a truncated arginine-rich protamine peptide, as well as a heparin/low-molecular-weight heparin antidote and a cell-penetrating delivery carrier. Low molecular weight protamine neutralizes heparin-induced anticoagulant activities, including aPTT, anti-Xa and anti-IIa activities, and also neutralizes anti-Xa activity of commercially available low-molecular-weight heparin preparations. Low molecular weight protamine translocates across mammalian cell membranes, delivers conjugated impermeable molecules across tumor tissues, enhances skin permeability of conjugated epidermal growth factor, and accelerates wound healing when conjugated with epidermal growth factor. Low molecular weight protamine retains the in vitro cell proliferation activity of conjugated EGF, and also enables site-specific conjugation with peptides or proteins via genetic recombination. Low molecular weight protamine can be used in studies related to colon adenocarcinoma, skin wounds and diabetic skin wounds.
    Low molecular weight protamine
  • HY-107145A
    Ningetinib
    Inhibitor 99.63%
    Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
    Ningetinib
  • HY-16018A
    Ilorasertib hydrochloride
    Inhibitor 98.48%
    Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
    Ilorasertib hydrochloride
  • HY-108798
    Ziv-aflibercept
    Inhibitor
    Ziv-aflibercept is a soluble inhibitor of vascular endothelial growth factor (VEGF). Ziv-aflibercept is an adaptive variant of Aflibercept (HY-108801), Ziv-aflibercept has a low PH value and high osmotic pressure when compared to Aflibercept. Ziv-aflibercept has potential applications in metastatic colorectal carcinoma and retinal diseases.
    Ziv-aflibercept
  • HY-B0446
    Naphazoline hydrochloride
    Inhibitor 99.38%
    Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research.
    Naphazoline hydrochloride
  • HY-19624
    NVP-ACC789
    Inhibitor 99.52%
    NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
    NVP-ACC789
  • HY-50904S2
    Nintedanib-d8
    Inhibitor 99.90%
    Nintedanib-d8 is 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-d<sub>8</sub>
  • HY-18006
    NKP608
    Inhibitor 99.88%
    NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK1) receptor antagonist with IC50 of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK2, NK3 receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer.
    NKP608
  • HY-P991738
    LM-299
    Inhibitor
    LM-299 is a PD-1/VEGF bispecific antibody. LM-299 achieves its dual binding activity through the effective binding of the anti-VEGF-A antibody at the fab end to human VEGF-A, coupled with the blockade of the PD-1/PD-L1 pathway by the anti-PD-1 antibody at the-Fc end. LM-299 can be used for the study of non-small cell lung cancer (NSCLC).
    LM-299
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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