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.

Literature (1)
Pathways (1)
Gene Data

VEGFR Inhibitors

Cat. No. Product Name / Activity
5318 AEE 788
Potent VEGFR and EGFR inhibitor
4274 AP 24534
Potent multi-kinase and pan-Bcr-Abl inhibitor
4350 Axitinib
Potent VEGFR-1, -2 and -3 inhibitor
7454 Cediranib
Potent inhibitor of VEGFR, PDGFR and FGFR
2542 Ki 8751
Potent, selective VEGFR-2 inhibitor
7743 Linifanib
Potent inhibitor of PDGFRβ, KDR, FLT3 and CSF-1R
7049 Nintedanib
Potent VEGFR, PDGFR and FGFR inhibitor
6814 Sorafenib
VEGFR-2 and VEGFR-3 inhibitor; also inhibits Raf-1, PDGFR-β, Flt-3 and cKIT
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
7497 Vandetanib
Potent VEGFR-2 inhibitor, also inhibits EGFR and RET oncoproteins activity
5680 Vatalanib succinate
Potent VEGFR inhibitor; also aromatase inhibitor
5422 XL 184
Potent VEGFR inhibitor; also inhibits other RTKs
2475 ZM 323881 hydrochloride
Potent, selective inhibitor of VEGFR-2


Cat. No. Product Name / Activity
6986 EG 00229 trifluoroacetate
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.

External sources of pharmacological information for VEGFR :

    Literature for VEGFR

    Tocris offers the following scientific literature for VEGFR to showcase our products. We invite you to request* your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.

    Angiogenesis in Cancer Poster

    Angiogenesis in Cancer Poster

    This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

    Pathways for VEGFR

    VEGF Signaling Pathway

    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