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-156790
    FGFR3-IN-6
    		Inhibitor
    FGFR3-IN-6 is a potent and selective FGFR3 inhibitor with IC50 value less than 350 nM. FGFR3-IN-6 can be used in research of cancer.
    FGFR3-IN-6
  • HY-10981S1
    Lenvatinib-d5
    		Inhibitor
    Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
    Lenvatinib-d<sub>5</sub>
  • HY-162577
    FGFR-IN-14
    		Inhibitor
    FGFR-IN-14 (compound 10h) is a pan-FGFR inhibitor. FGFR-IN-14 inhibits FGFR1, FGFR2, FGFR3 and FGFR2 V564F gatekeeper mutant with IC50s of 46, 41, 99, and 62 nM, respectively. FGFR-IN-14 strongly suppresses NCI-H520 lung cancer cells, SNU-16 and KATO III gastric cancer cells proliferation with IC50s of 19, 59, and 73 nM, respectively.
    FGFR-IN-14
  • HY-142921
    FGFR-IN-2
    		Inhibitor
    FGFR-IN-2 (compound 1) is a potent FGFR inhibitor with IC50s of 7.3 nM, 4.3 nM, 7.6 nM, 11 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-2 has the potential for cancer research.
    FGFR-IN-2
  • HY-15472A
    PRX-08066 maleate
    		Inhibitor
    PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
    PRX-08066 maleate
  • HY-158098
    FGFR1 inhibitor-11
    		Inhibitor
    FGFR1 inhibitor-11 (compound 5g) binds to FGFR1, inactivation of its downstream ERK1/2 and IκBα/NF-κB signaling inhibited RANKL-induced osteoclastogenesis. FGFR1 inhibitor-11 has oral bioactivity.
    FGFR1 inhibitor-11
  • HY-122833
    FGFR3-IN-10
    		Inhibitor
    FGFR3-IN-10 is a FGFR3 inhibitor with superior selectivity for FGFR3 over FGFR1.FGFR3-IN-10 can be used for the research of cancer, systemic sclerosis, fibrosis, pulmonary fibrosis, achondroplasia, thanatophoric dysplasia, severe achondroplasia with developmental delay and acanthosis nigricans (SADDAN), Muenke syndrome.
    FGFR3-IN-10
  • HY-RS04915
    FGFR2 Human Pre-designed siRNA Set A
    		Inhibitor

    FGFR2 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    FGFR2 Human Pre-designed siRNA Set A
  • HY-148778
    FGFR3-IN-4
    		Inhibitor
    FGFR3-IN-4 is a selective FGFR3 inhibitor, with an IC50 value of less than 50 nM. FGFR3-IN-4 is at least 10 fold more selective for FGFR3 than for FGFR1.
    FGFR3-IN-4
  • HY-159642G
    Dabogratinib (GMP)
    		Inhibitor
    Dabogratinib (TYRA-300) (GMP) is Dabogratinib (HY-159642) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Dabogratinib is an orally active, selective FGFR3 inhibitor with an IC50 of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia.
    Dabogratinib (GMP)
  • HY-159691B
    IONIS-FGFR4Rx sodium scrambled negative control
    		Inhibitor
    IONIS-FGFR4Rx sodium scrambled negative control is the sequence scrambled negative control of IONIS-FGFR4Rx sodium.
    IONIS-FGFR4Rx sodium scrambled negative control
  • HY-10981S2
    Lenvatinib-15N,d4
    		Inhibitor 98.01%
    Lenvatinib-15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
    Lenvatinib-<sup>15</sup>N,d<sub>4</sub>
  • HY-P10870
    Pep1-DNP conjugate 9
    		Inhibitor
    Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models.
    Pep1-DNP conjugate 9
  • HY-152104
    FGFR-IN-9
    		Inhibitor
    FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively.
    FGFR-IN-9
  • HY-10335
    BMS-645737
    		Inhibitor
    BMS-645737 is an orally active, selective FGF receptor-1 and VEGF receptor-2 inhibitor. BMS-645737 selectively and competitively inhibits both VEGFR-2 and FGFR-1 tyrosine kinases. BMS-645737 has anti-angiogenic activity. BMS-645737 induces lesions in the incisor teeth.
    BMS-645737
  • 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-179381
    FGFR4-IN-24
    		Inhibitor
    FGFR4-IN-24 is a selective irreversible covalent FGFR4 inhibitor (IC50 = 1.2 nM). FGFR4-IN-24 shows much weaker activity against the other three FGFR family kinases (FGFR1-3). FGFR4-IN-24 inhibits the FGF19/FGFR4 signaling pathway, effectively suppressing the proliferation of the HuH-7 HCC cell line (GI50 = 17 nM). FGFR4-IN-24 exhibits significant antitumor activity in a HuH-7 mouse xenograft model. FGFR4-IN-24 can be used for the research of hepatocellular carcinoma.
    FGFR4-IN-24
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity