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-P5107A
    Low molecular weight protamine acetate
    		98.64%
    Low molecular weight protamine acetate (LMWP acetate;TDSP5 acetate) is a truncated arginine-rich protamine peptide, which also acts as an antidote for heparin/low molecular weight heparin and a cell-penetrating delivery vector. Low molecular weight protamine acetate neutralizes heparin-induced anticoagulant activities, including aPTT, anti-Xa and anti-IIa activities. Low molecular weight protamine acetate translocates across mammalian cell membranes, delivers conjugated impermeable molecules through tumor tissues, enhances the skin permeability of conjugated epidermal growth factor, and accelerates wound healing when conjugated with epidermal growth factor. Low molecular weight protamine acetate 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 acetate can be used in studies related to colon cancer, skin wounds and diabetic skin wounds.
    Low molecular weight protamine acetate
  • HY-P10971
    Nef-M1
    		Inhibitor
    Nef-M1 (Nef-Motif-1) is an antagonist peptide targeting CXCR4 and an apoptosis inducer derived from a myristoylated protein encoded by the nef gene in HIV. Nef-M1 inhibits tumor angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 activates the apoptosis pathway by increasing the level of caspase-3 in cancer cells. Nef-M1 simultaneously inhibits VEGF-A, p-GSK-3β and vimentin, and enhances E-cadherin, thereby inhibiting angiogenesis and EMT processes. Nef-M1 can be used in the study of colorectal cancer and breast cancer.
    Nef-M1
  • HY-N1983R
    Caudatin (Standard)
    Caudatin (Standard) is the analytical standard of Caudatin (HY-N1983). This product is intended for research and analytical applications. Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease.
    Caudatin (Standard)
  • HY-P991689
    Girancitug
    		Inhibitor 98.80%
    Girancitug is a humanized IgG1κ monoclonal antibody inhibitor targeting VEGFR2/KDR/CD309. Girancitug effectively inhibits angiogenesis. Girancitug can be used for anti-angiogenic therapy in cancers like colorectal and ovarian cancer research.
    Girancitug
  • 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-182700
    NRPa-308
    		Inhibitor 98.96%
    NRPa-308 is a potent and orally active Neuropilin-1 (NRP-1) antagonist with an IC50 of 42 μM for inhibiting VEGF-A165 binding to NRP-1. NRPa-308 blocks the specific interaction between VEGF-A165 and NRP-1. NRPa-308 effectively suppresses angiogenesis in vitro and in vivo and reduces the viability of a broad spectrum of human solid and haematological cancer cells. NRPa-308 inhibits tumor growth and prolongs median survival in a human breast cancer xenograft mouse model. NRPa-308 can be used for the research of multiple human malignancies including solid tumors and hematological cancers.
    NRPa-308
  • HY-U00002
    ZD-4190
    		Inhibitor 98.08%
    ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
    ZD-4190
  • HY-112294
    TIE-2/VEGFR-2 kinase-IN-1
    		Inhibitor 99.91%
    TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors, extracted from patent WO2003022852, example 14. TIE-2/VEGFR-2 kinase-IN-1 is used for the study of diseases associated with inappropriate angiogenesis.
    TIE-2/VEGFR-2 kinase-IN-1
  • HY-P992139
    Valancitug
    		Inhibitor
    Valancitug is a human monoclonal antibody targeting VEGFA. Its corresponding isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Valancitug
  • HY-120640
    BMS-605541
    		Inhibitor 99.57%
    BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research.
    BMS-605541
  • HY-N7700
    Guluronic acid
    		Inhibitor 98.90%
    Guluronic acid (G2013) is an orally active oxidative stress regulator and anti-inflammatory agent that exerts pharmacological effects by down-regulating various pro-inflammatory and oxidative stress-related genes (such as TLR4, NF-κB, iNOS, etc.) and inhibiting the activities of COX-2, MMPs and VEGF. Low-dose Guluronic acid up-regulates the expression of immunoregulatory genes SHIP1 and SOCS1, thereby effectively inhibiting cancer-related inflammation, tumor angiogenesis, cell adhesion and metastasis, while reducing the accumulation of immunosuppressive cells. Guluronic acid significantly prolongs the survival time of tumor-bearing hosts within a concentration range without direct cytotoxicity, demonstrating favorable safety. Guluronic acid has involved in the research of multiple sclerosis, ankylosing spondylitis, breast cancer and other inflammatory diseases.
    Guluronic acid
  • HY-10208S
    Pazopanib-d6
    		Inhibitor 98.0%
    Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib-d<sub>6</sub>
  • HY-153556
    GW297361
    		Inhibitor 98.13%
    GW297361 is an oxindole CDK inhibitor that elicits a Pho85-selective response in cells. GW297361 inhibits yeast Cdk1 and Pho85 with IC50s of 20 nM and 400 nM in vitro, respectively.
    GW297361
  • HY-P991141
    Inlecitug
    		Ligand 98.62%
    Inlecitug is a chimeric monoclonal antibody targeting human KDR (kinase insert domain receptor). Inlecitug specifically binds to KDR, blocking the binding of vascular endothelial growth factor (VEGF) to KDR and inhibiting angiogenesis, thus exerting antitumor activity. Inlecitug is promising for research of cancers.
    Inlecitug
  • HY-10255AS
    Sunitinib-d10
    		Inhibitor 99.89%
    Sunitinib-d10 (SU 11248-d10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib-d<sub>10</sub>
  • HY-12047S
    Ponatinib-d8
    		Inhibitor 99.16%
    Ponatinib-d8 (AP24534-d8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
    Ponatinib-d<sub>8</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
  • HY-108226
    Regorafenib N-oxide and N-desmethyl (M5)
    		Inhibitor
    Regorafenib N-oxide and N-desmethyl (M5) (N-Desmethyl regorafenib N-oxide) is an active metabolite of Sorafenib (HY-10201) and can be metabolized by CYP3A4.
    Regorafenib N-oxide and N-desmethyl (M5)
  • 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-118105
    RK-20448
    		Inhibitor 99.38%
    RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC50 values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259 (HY-15764).
    RK-20448
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
VEGFR Isoform Comparison

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