FGFR
FGFRs are transmembrane receptor tyrosine kinases for fibroblast growth factors, and four FGFRs possess intracellular protein-tyrosine kinase activity[1]. Mechanistically, FGFR signaling activates MAPK, JNK, β-catenin, and related transcriptional programs that regulate proliferation, differentiation, survival, migration, and organogenesis[2][3][4]. In developmental models, FGFR1 supports neurulation and limb development, whereas FGFR2IIIb controls mesenchymal-epithelial signaling during early organogenesis[5][6]. In epithelial and cancer models, isoform context strongly changes biological output: FGFR1-IIIb induces proliferation through p44/42 MAP kinase and JNK pathways, FGFR2IIIb differs from FGFR2IIIc in ligand-binding specificity and tissue distribution, and FGFR4 mediates FGF19 signaling to the prolactin promoter[2][6][7]. Disease relevance also differs by isoform, because FGFR3 mutations account for achondroplasia, hypochondroplasia, and thanatophoric dwarfism, while FGFR4 overexpression associates with poor survival in high-grade serous ovarian carcinoma[8][9]. For experimental applications, FGFR inhibitors such as erdafitinib, infigratinib, futibatinib, and fisogatinib provide tools to interrogate kinase-dependent FGFR signaling and FGFR-driven cancers[1][10].
References:
- [1]. Roskoski R Jr. The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder. Pharmacol Res. 2020 Jan;151:104567. doi: 10.1016/j.phrs.2019.104567. Epub 2019 Nov 23. PMID: 31770593. et al. The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder. Pharmacol Res. 2020 Jan;151:104567. [Content Brief]
- [2]. Fukamachi A, et al. Postoperative extradural hematomas: computed tomographic survey of 1105 intracranial operations. Neurosurgery. 1986 Oct;19(4):589-93. [Content Brief]
- [3]. Brodrick B, et al. Fibroblast growth factor receptor-3 (FGFR-3) regulates expression of paneth cell lineage-specific genes in intestinal epithelial cells through both TCF4/beta-catenin-dependent and -independent signaling pathways. J Biol Chem. 2011 May 27;286(21):18515-25. [Content Brief]
- [4]. Rosenthal R, et al. The fibroblast growth factor receptors, FGFR-1 and FGFR-2, mediate two independent signalling pathways in human retinal pigment epithelial cells. Biochem Biophys Res Commun. 2005 Nov 11;337(1):241-7. [Content Brief]
- [5]. Deng C, et al. Fibroblast growth factor receptor-1 (FGFR-1) is essential for normal neural tube and limb development. Dev Biol. 1997 May 1;185(1):42-54. [Content Brief]
- [6]. Spencer-Dene B, et al. An Important Role for the IIIb Isoform of Fibroblast Growth Factor Receptor 2 in Mesenchymal-Epithelial Signalling during Mouse Organogenesis. Clinical Science. 2000 Aug 1;99(s43):5P-.
- [7]. Yu S, et al. Fibroblast growth factor receptor 4 (FGFR4) mediates signaling to the prolactin but not the FGFR4 promoter. Am J Physiol Endocrinol Metab. 2002 Sep;283(3):E490-5. [Content Brief]
- [8]. Bonaventure J, et al. Common mutations in the fibroblast growth factor receptor 3 (FGFR 3) gene account for achondroplasia, hypochondroplasia, and thanatophoric dwarfism. Am J Med Genet. 1996 May 3;63(1):148-54. [Content Brief]
- [9]. Hao X, et al. Electromagnetic Functional Properties of Flexible Picosecond Laser-Induced Graphene Films Modified with Silver Nanoparticles. ACS Appl Mater Interfaces. 2026 May 27;18(20):28957-28968. [Content Brief]
- [10]. Lu X, et al. Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. J Med Chem. 2019 Mar 28;62(6):2905-2915. [Content Brief]
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FGFR Related Products (187)
Related Products (187)
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Regorafenib monohydrate (Standard)
0 ImagesSynonyms: BAY 73-4506 monohydrate (Standard)Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
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cRY9M
0 ImagesCat. No.: HY-P11853cRY9M is a cyclic peptide that binds to FGFR1, with a KD value of 58 nM. cRY9M binds specifically to FGFR1, exhibits enhanced in vivo stability, and shows extremely low degradation in blood, urine and liver homogenate after injection. cRY9M displays significant specific uptake in FGFR1-positive tumor xenograft models, while its uptake decreases in FGFR1-negative tumor models and blocking models. The NOTA-chelated precursor of cRY9M can be labeled with 68Ga to obtain [68Ga]Ga-NOTA-cRY9M, which is used for research on non-invasive imaging of FGFR1 expression in non-small cell lung cancer.
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AXL/Angiokinase-IN-1
0 ImagesCat. No.: HY-170776AXL/Angiokinase-IN-1 (compound 11b) is an AXL/triple angiokinase inhibitor, IC50=3.75 nM (AXL expression). AXL/Angiokinase-IN-1 inhibits epithelial-mesenchymal transition (EMT) in Bxpc-3, blocking lung cancer cell metastasis. AXL/Angiokinase-IN-1 also inhibits vascular and fibroblast functions, promoting apoptosis (apoptosis) in cancer cells and fibroblasts. AXL/Angiokinase-IN-1 features low toxicity and good metabolic stability.
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FGFR2 V564F Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70825FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 V564F is a mutant of FGFR3. FGFR2 V564F Recombinant Human Active Protein Kinase is a recombinant FGFR2 V564F protein that can be used to study FGFR2 V564F-related functions.
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FGFR3-IN-9
0 ImagesCat. No.: HY-158011CAS No.: 2446523-17-5FGFR3-IN-9 (example27) is a selective FGFR3 inhibitor.
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FGFR2 V564I Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70826FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 V564I is a mutant of FGFR3. FGFR2 V564I Recombinant Human Active Protein Kinase is a recombinant FGFR2 V564I protein that can be used to study FGFR2 V564I-related functions.
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ZINC13407541
0 ImagesCat. No.: HY-183371CAS No.: 864868-22-4ZINC13407541 is a fibroblast growth factor 23 (FGF23) antagonist with an IC50 of 0.45 μM. ZINC13407541 preferentially binds to the FGF23:FGFR interface to disrupt their protein-protein interactions. ZINC13407541 can be used for the research of hypophosphatemia.
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Fgfr4 Rat Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS04923Fgfr4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Fgfr4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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FGFR4-IN-16
0 ImagesCat. No.: HY-156704CAS No.: 1970120-44-5
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FGFR2 C491S Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70814FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 C491S is a mutant of FGFR3. FGFR2 C491S Recombinant Human Active Protein Kinase is a recombinant FGFR2 C491S protein that can be used to study FGFR2 C491S-related functions.
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FGFR2 K641R Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70817FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 K641R is a mutant of FGFR3. FGFR2 K641R Recombinant Human Active Protein Kinase is a recombinant FGFR2 K641R protein that can be used to study FGFR2 K641R-related functions.
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FGFR-IN-5
0 ImagesCat. No.: HY-147620CAS No.: 2762750-70-7FGFR-IN-5 is a potent inhibitor of FGFR. Fibroblast growth factor receptor (FGFR) is a tyrosine kinase receptor that binds to fibroblast growth factor ligands. FGFR-IN-5 has the potential for the research of cancer diseases (extracted from patent WO2022042612A1, compound 3). FGFR-IN-5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Tec-IN-14
0 ImagesCat. No.: HY-111289CAS No.: 852838-07-4
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FGFR4-IN-12
0 ImagesCat. No.: HY-147793CAS No.: 2423992-63-4FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases. FGFR4-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Antitumor agent-176
0 ImagesCat. No.: HY-161840Antitumor agent-176 (Compound 22), an antitumor agent, can effectively bind to FGF2 and inhibit the activation of fibroblast growth factor receptor (FGFR) in multiple myeloma (MM) cells, exhibiting significant antitumor activity both in vivo and in vitro against MM.
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FGFR-IN-13
0 ImagesCat. No.: HY-163527CAS No.: 2962941-25-7FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity.
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FGFR4 Human Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS04921FGFR4 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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FGFR3 K650E Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70719FGFR3 activating mutations are drivers of malignancy in several human tissues, including bladder, lung, cervix, and blood. FGFR3 K650E is a mutant of FGFR3 that may be present in multiple myeloma cell lines. FGFR3 K650E Recombinant Human Active Protein Kinase is a recombinant FGFR3 K650E protein that can be used to study FGFR3 K650E-related functions.
