2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. FGFR

FGFR

Fibroblast growth factor receptor

FGFR

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FGFR (Fibroblast growth factor receptors) are the receptors that bind to members of the fibroblast growth factor family of proteins. Some of these receptors are involved in pathological conditions. A point mutation in FGFR3 can lead to achondroplasia. Five distinct membrane FGFR have been identified in vertebrates and all of them belong to the tyrosine kinase superfamily (FGFR1, FGFR2, FGFR3, FGFR4, FGFR6). The fibroblast growth factor family constitutes one of the most important groups of paracrine factors that act during development. They are responsible for determining certain cells to become mesoderm, for the production of blood vessels, for limb outgrowth, and for the growth and differentiation of numerous cell types.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-150652
    FGFR-IN-8
    		Inhibitor
    FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities.
    FGFR-IN-8
  • HY-170846
    FGFRs-IN-1
    		Inhibitor
    FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model.
    FGFRs-IN-1
  • HY-122704
    Surfen
    		Inhibitor
    Surfen is a potent heparan sulfate antagonist. Surfen inhibits FGF2 binding and signal transduction. Surfen binds to glycosaminoglycans and reduces tau hyperphosphorylation. Surfen inhibits the activity of recombinant uronyl 2-O-sulfotransferase with an IC50 of approximately 2 μM. Surfen inhibits HSV-1 viral infection. Surfen inhibits neural differentiation, delays remyelination, and alleviates EAE.
    Surfen
  • HY-161610
    FGFR4-IN-21
    		Inhibitor
    FGFR4-IN-21 (Compd 4c) is a FGFR4 inhibitor with an IC50 of 33 nM. FGFR4-IN-21 can be used for hepatocellular carcinoma research.
    FGFR4-IN-21
  • HY-147714
    FGFR3-IN-2
    		Inhibitor
    FGFR3-IN-2 (compound 18b) is a potent and selective FGFR3 inhibitor, with IC50s of 4.1 nM and 570 nM for FGFR3 and VEGFR2, respectively. FGFR3-IN-2 can be used for the research of bladder cancer.
    FGFR3-IN-2
  • HY-10208S1
    Pazopanib-13C,d3
    Pazopanib-13C,d3 is the deuterium and 13C 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-<sup>13</sup>C,d<sub>3</sub>
  • HY-123541
    Tec-IN-6
    		Inhibitor
    Tec-IN-6 (compound 6) is a FGF2 binding to Tec kinase inhibitor, with an IC50 of 8.9 μM (His-FGF2/GST-NΔ173 Tec).
    Tec-IN-6
  • HY-148597
    FGFR-IN-10
    		Inhibitor
    FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively.
    FGFR-IN-10
  • HY-168597
    FGFR1/VEGFR2-IN-3
    		Inhibitor
    FGFR1/VEGFR2-IN-3 (Compound 8m) is a dual inhibitor of FGFR1/VEGFR2. FGFR1/VEGFR2-IN-3 exhibits anti-proliferative and anti-migratory activities against cancer cells, and is capable of inducing cell apoptosis.
    FGFR1/VEGFR2-IN-3
  • HY-174268
    FGFR-IN-21
    		Inhibitor
    FGFR-IN-21 (Compound FP1) is a selective covalent FGFR4 inhibitor with an IC50 value of 70 nM. FGFR-IN-21 is promising for research of FGFR signaling pathways in cancers.
    FGFR-IN-21
  • HY-E70717
    FGFR1 V561M Recombinant Human Active Protein Kinase
    FGFR1 has been implicated in numerous cancer types including non-small cell lung cancer (NSCLC). FGFR1 is activated upon FGF binding to its extracellular domain, resulting in protein dimerization and transautophosphorylation of the intracellular tyrosine kinase domains. FGFR1 V561M gatekeeper mutation drives Fexagratinib (AZD4547) (HY-13330) resistance through STAT3 Activation and EMT. FGFR1 V561M Recombinant Human Active Protein Kinase is a recombinant FGFR1 V561M protein that can be used to study FGFR1 V561M-related functions.
    FGFR1 V561M Recombinant Human Active Protein Kinase
  • HY-146541
    FGFR4-IN-10
    		Inhibitor
    FGFR4-IN-10 (compound 5a) is a potent and selective FGFR4 inhibitor with an IC50 value of 70.7 nM. FGFR4-IN-10 shows no inhibition against other FGFR family members, i.e. FGFR1, FGFR2 and FGFR3.
    FGFR4-IN-10
  • HY-158027
    B-Raf IN 17
    		Inhibitor
    B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer.
    B-Raf IN 17
  • HY-E70722
    FGFR4 V550E Recombinant Human Active Protein Kinase
    FGFR4 is a transcriptional target of the PAX3-FOXO1 fusion gene. FGFR4 expression is significantly higher in rhabdomyosarcoma. FGFR4 V550E is a mutant of FGFR3 that may be present in rhabdomyosarcoma. FGFR4 V550E Recombinant Human Active Protein Kinase is a recombinant FGFR4 V550E protein that can be used to study FGFR4 V550EK-related functions.
    FGFR4 V550E Recombinant Human Active Protein Kinase
  • HY-E70720
    FGFR3 K650M Recombinant Human Active Protein Kinase
    FGFR3 activating mutations are drivers of malignancy in several human tissues, including bladder, lung, cervix, and blood. FGFR3 K650M is a mutant of FGFR3. FGFR3 K650M Recombinant Human Active Protein Kinase is a recombinant FGFR3 K650M protein that can be used to study FGFR3 K650M-related functions.
    FGFR3 K650M Recombinant Human Active Protein Kinase
  • HY-E70815
    FGFR2 K526E Recombinant Human Active Protein Kinase
    FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 K526E is a mutant of FGFR3. FGFR2 K526E Recombinant Human Active Protein Kinase is a recombinant FGFR2 K526E protein that can be used to study FGFR2 K526E-related functions.
    FGFR2 K526E Recombinant Human Active Protein Kinase
  • HY-170869
    PROTAC FGFR1 degrader-1
    		Degrader
    PROTAC FGFR1 degrader-1 (compound S2H) is a PROTAC degrader targeting FGFR1, with IC50=26.81 nM and DC50=39.78 nM in KG1a cells. PROTAC FGFR1 degrader-1 is composed of CRBN-type E3 ligase ligand (blue part) Pomalidomide (HY-10984), target protein ligand (red part) FGFR1 ligand-1 (HY-170871), and PROTAC linker (black part) 9-Bromononanoic acid (HY-W007587), in which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 164 (HY-170870).
    PROTAC FGFR1 degrader-1
  • HY-158010
    FGFR3-IN-8
    		Inhibitor
    FGFR3-IN-8 (example91) is a selective FGFR3 inhibitor.
    FGFR3-IN-8
  • HY-E70827
    FGFR2 V564L Recombinant Human Active Protein Kinase
    FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 V564L is a mutant of FGFR3. FGFR2 V564L Recombinant Human Active Protein Kinase is a recombinant FGFR2 V564L protein that can be used to study FGFR2 V564L-related functions.
    FGFR2 V564L Recombinant Human Active Protein Kinase
  • HY-149488
    FGFR1 inhibitor-9
    		Inhibitor
    FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor (IC50s: 0.85 nM). FGFR1 inhibitor-9 binds to the ATP-binding pocket of FGFR1. FGFR1 inhibitor-9 has anticancer activity.
    FGFR1 inhibitor-9
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity