Fibroblast growth factors (FGFs) are mitogenic signaling molecules that have roles in angiogenesis, wound healing, cell migration, neural outgrowth and embryonic development. FGF receptors (FGFRs) are transmembrane catalytic receptors with intracellular tyrosine kinase activity.

Literature (5)
Gene Data

FGFR Inhibitors

Cat. No. Product Name / Activity
4274 AP 24534
Potent multi-kinase and pan-Bcr-Abl inhibitor
7823 AZD 4547
Potent and selective FGFR inhibitor
7454 Cediranib
Potent inhibitor of VEGFR, PDGFR and FGFR
4002 FIIN 1 hydrochloride
Potent, irreversible FGFR inhibitor
7049 Nintedanib
Potent VEGFR, PDGFR and FGFR inhibitor
3724 PD 161570
Selective FGFR inhibitor
3785 PD 166285 dihydrochloride
FGFR, PDGFRβ and Src inhibitor; also inhibits Wee1
3044 PD 173074
FGFR1 and -3 inhibitor
3300 SU 5402
Potent FGFR and VEGFR inhibitor
3335 SU 6668
FGFR, VEGFR and PDGFR inhibitor

Fibroblast growth factors (FGFs) (FGF1 - 10 and 16 - 23) are mitogenic signaling molecules that have roles in angiogenesis, wound healing, cell migration, neural outgrowth and embryonic development. FGFs bind heparan sulfate glycosaminoglycans (HSGAGs), which facilitates dimerization (activation) of FGF receptors (FGFRs).

FGFRs are transmembrane catalytic receptors that have intracellular tyrosine kinase activity. There are four human genes encoding FGFRs, which produce seven different receptors (FGFR1b, FGFR1c, FGFR2b, FGFR2c, FGFR3b, FGFR3c and FGFR4) due to alternative splicing events occurring both in the extracellular and intracellular regions. The alternative splice isoforms are generally tissue specific: the b isoform is expressed in epithelial tissue, whereas the c isoform is expressed in mesenchymal tissue. HSGAG-FGF-FGFR binding initiates FGFR dimerization, enabling the cytoplasmic kinase domains to transphosphorylate tyrosine residues and become activated. HSGAGs also function to stabilize FGF-FGFR binding and prevent FGF degradation.

FGFs were first isolated as growth factors for fibroblasts. Since the initial discovery of FGF1 and FGF2, a further 20 structurally related FGFs have been identified, all of which are differentially expressed in many tissues. Of these 22 growth factors, 18 are FGFR ligands. FGFRs couple to the PLCγ, MAPK and PI3-K/Akt intracellular signaling cascades and there is evidence of cross talk with the Notch signaling pathway. In addition, some activated FGF-FGFR complexes are endocytosed and function directly in the cytosol and/or nucleus of the cell.

Mutations in FGFR genes are the cause of several human developmental disorders characterized by skeletal abnormalities such as achondroplasia, and upregulation of FGFR expression may lead to cell transformation and cancer.

External sources of pharmacological information for FGFR :

    Literature for FGFR

    Tocris offers the following scientific literature for FGFR 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.

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    FGFR Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    FGFR1 Human FGFR1 NM_023110 Q5BJG2
    Mouse Fgfr1 NM_010206 P16092
    Rat Fgfr1 NM_024146 O35758
    FGFR2 Human FGFR2 NM_022976 Q9UQH7
    Mouse Fgfr2 NM_010207 P21803
    Rat Fgfr2 NM_012712 Q9R2A0
    FGFR3 Human FGFR3 NM_000142 P22607
    Mouse Fgfr3 NM_008010 Q61851
    Rat Fgfr3 NM_053429 Q9JHX9
    FGFR4 Human FGFR4 NM_022963 P22455
    Mouse Fgfr4 NM_008011 Q03142
    Rat Fgfr4 NM_001109904 Q498D6