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-10527C
    Telatinib mesylate
    Inhibitor 99.74%
    Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.
    Telatinib mesylate
  • HY-101990
    IMS2186
    Inhibitor 99.96%
    IMS2186 is an anti-choroidal neovascularization (CNV) agent that inhibits angiogenesis upstream of VEGF. IMS2186 can arrest cancer cell cycle in G2/M phase, thus exerting anti-proliferation and anti-angiogenesis effects. IMS2186 has no intraocular toxicity and reduces the amount of eye leakage and diseased cells.
    IMS2186
  • HY-21289
    SU5205
    Inhibitor 98.02%
    SU5205 is an inhibitor of VEGFR2 (FLK-1), with an IC50 of 9.6 μM.
    SU5205
  • HY-126319
    SU5204
    Inhibitor 99.46%
    SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
    SU5204
  • HY-12009S
    Pazopanib-13C,d3 hydrochloride
    Pazopanib-13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib-<sup>13</sup>C,d<sub>3</sub> hydrochloride
  • HY-P4253A
    Arginyl-Glutamine TFA
    Inhibitor 99.22%
    Arginyl-Glutamine TFA is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy.
    Arginyl-Glutamine TFA
  • 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-149636
    Multi-target kinase inhibitor 2
    Inhibitor 99.82%
    Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
    Multi-target kinase inhibitor 2
  • HY-N0135R
    Tanshinone IIA (Standard)
    Inhibitor
    Tanshinone IIA (Standard) is the analytical standard of Tanshinone IIA. This product is intended for research and analytical applications. Tanshinone IIA (Tan IIA) is one of the main compositions in the root of Salvia miltiorrhiza Bunge. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.
    Tanshinone IIA (Standard)
  • HY-W800162
    VEGFR-2-IN-37
    Inhibitor 99.11%
    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-10331S
    Regorafenib-d3
    Inhibitor 98.0%
    Regorafenib-d3 (BAY 73-4506-d3) is a deuterium labeled Regorafenib (HY-10331). Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor.
    Regorafenib-d<sub>3</sub>
  • HY-P991664
    AG01
    Inhibitor
    AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers.
    AG01
  • 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-50904S
    Nintedanib-d3
    Inhibitor
    Nintedanib-d3 is the 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>3</sub>
  • HY-131658
    VEGFR-2-IN-6
    Inhibitor 99.89%
    VEGFR-2-IN-6 (example 64) is a VEGFR2 inhibitor (angiogenesis modulator), which is extracted from patent WO 02/059110.
    VEGFR-2-IN-6
  • HY-10255C
    Sunitinib glucuronate
    Inhibitor
    Sunitinib (SU 11248) glucuronate is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib glucuronate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib glucuronate
  • HY-164387
    Sutetinib
    Inhibitor 99.27%
    Sutetinib 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 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
  • HY-18625
    VEGFR-2-IN-5
    Inhibitor
    VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 69.
    VEGFR-2-IN-5
  • HY-N5014
    Liensinine perchlorate
    Inhibitor 99.67%
    Liensinine perchlorate is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine perchlorate suppresses autophagy and apoptosis, clears , and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine perchlorate activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine perchlorate exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine perchlorate can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.
    Liensinine perchlorate
  • HY-13302C
    CP-547632 TFA
    Inhibitor 99.42%
    CP-547632 TFA 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 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy.
    CP-547632 TFA
Cat. No. Product Name / Synonyms Species Source
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