VEGFR

Vascular endothelial growth factor is a signaling protein involved in the regulation of angiogenesis and vasculogenesis. VEGF binds to and activates a receptor tyrosine kinase, VEGFR, through transphosphorylation. Three VEGFR isoforms have been identified in humans.

Products
Background
Literature
Pathways
Gene Data

Inhibitors

Cat No Product Name / Activity
5318 AEE 788
Potent VEGFR and EGFR inhibitor
2617 AG 879
VEGFR-2 inhibitor
4274 AP 24534
Potent multi-kinase and pan-Bcr-Abl inhibitor
4350 Axitinib
Potent VEGFR-1, -2 and -3 inhibitor
4471 DMH4
Selective VEGFR-2 inhibitor
3882 (E)-FeCP-oxindole
Selective VEGFR-2 inhibitor
3883 (Z)-FeCP-oxindole
Selective VEGFR-2 inhibitor
6056 GSK 1363089
Potent inhibitor of MET, VEGFR2, Ron and AXL
2542 Ki 8751
Potent, selective VEGFR-2 inhibitor
6015 RAF 265
VEGFR-2 and Raf kinase inhibitor
1459 SU 4312
Potent inhibitor of VEGFR tyrosine kinase
3300 SU 5402
Potent VEGFR and FGFR inhibitor
3037 SU 5416
VEGFR inhibitor. Also inhibits KIT, RET, MET and FLT3
3335 SU 6668
VEGFR, PDGFR and FGFR inhibitor
3768 Sunitinib malate
Potent VEGFR, PDGFRβ and KIT inhibitor
3909 Toceranib
Potent PDGFR and VEGFR inhibitor
5680 Vatalanib succinate
Potent VEGFR inhibitor; also aromatase inhibitor
5422 XL 184
Potent VEGFR inhibitor; also inhibits other RTKs
2499 ZM 306416 hydrochloride
Inhibitor of VEGF receptor tyrosine kinase
2475 ZM 323881 hydrochloride
Potent, selective inhibitor of VEGFR-2

Other

Cat No Product Name / Activity
4931 EG 00229
Neuropilin 1 (NRP1) receptor antagonist; inhibits VEGFA binding to NRP1

Vascular endothelial growth factor is a signaling protein involved in the regulation of angiogenesis and vasculogenesis.

Whilst multiple receptors and ligands are involved in angiogenesis, VEGF signaling is one of the most important, rate-limiting steps of the process. VEGF is diffusible and selective for vascular endothelial cells, and possesses the ability to promote the growth and survival of these cells in vitro. Hypoxic conditions activate hypoxia-inducible factor 1 (HIF-1), resulting in increased VEGF mRNA expression. Other growth factors such as EGF, TGF-β and PDGF may also upregulate VEGF expression. The increased expression levels of VEGF in solid tumors, hematological malignancies, age-related macular degeneration (AMD), diabetes mellitus and various inflammatory disorders has placed great emphasis on developing VEGF inhibitors.

VEGF binds to and activates the receptor tyrosine kinase, VEGFR. Three VEGFR isoforms have been identified in humans: VEGFR-1 (Flt-1), VEGFR-2 (KDR/Flk-1) and VEGFR-3 (Flt-4) VEGFR-2 mediates the majority of cellular responses to VEGF, in particular its mitogenic and angiogenic effects. VEGFR-1 is thought to modulate VEGFR-2 signaling or to act as a dummy/decoy receptor to sequester VEGF away from VEGFR-2. The expression of VEGFR-1 is also up-regulated by hypoxia, in a similar mechanism to VEGF, via HIF-1; its functions may vary depending on cell type and developmental stage.

Literature for VEGFR

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for VEGFR

VEGF

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.

VEGF Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
VEGFR-1 Human FLT1 NM_002019 P17948
Mouse Flt1 NM_010228 P35969
Rat Flt1 NM_019306 P53767
VEGFR-2 Human KDR NM_002253 P35968
Mouse Kdr NM_010612 P35918
Rat Kdr NM_013062 O08775
VEGFR-3 Human FLT4 NM_182925 P35916
Mouse Flt4 NM_008029 P35917
Rat Flt4 NM_053652 Q91ZT1