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 (188)
Related Products (188)
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SUN11602
0 ImagesSUN11602 is a novel aniline compound with basic fibroblast growth factor-like activity.
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U3-1784
0 ImagesCat. No.: HY-P990672
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Resigratinib
0 ImagesSynonyms: KIN-3248Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer).
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MAX-40279
0 ImagesCat. No.: HY-145723CAS No.: 2070931-57-4MAX-40279 is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 is also effective against the FLT3 mutants such as FLT3D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 can be used for the research of acute myelogenous leukemia (AML).
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S6K2-IN-1
0 ImagesS6K2-IN-1 (Compound 2) is a S6K2 inhibitor (IC50: 22 nM). S6K2-IN-1 also inhibits FGFR4 (IC50: 216 nM). S6K2-IN-1 has acceptable stability in mouse liver microsomes.
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Formononetin (Standard)
0 ImagesSynonyms: Biochanin B (Standard); Flavosil (Standard); Formononetol (Standard)Formononetin (Standard) is the analytical standard of Formononetin. This product is intended for research and analytical applications. Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth.
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1-Phenylindole
0 Images1-Phenylindole (Compound 8) is a 1-Phenylbenzimidazole analogue. 1-Phenylindole shows IC50 values of >50 μM and >50 μM for PDGFR and FGFR, respectively. 1-Phenylbenzimidazole is a selective PDGFR inhibitor.
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Nintedanib-d8
0 ImagesSynonyms: BIBF 1120-d8Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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Lenvatinib (Standard)
0 ImagesSynonyms: E7080 (Standard)
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Futibatinib (Standard)
0 ImagesSynonyms: TAS-120 (Standard)Futibatinib (Standard) is the analytical standard of Futibatinib. This product is intended for research and analytical applications. Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM).
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FGL peptide
0 ImagesFGL peptide is a fibroblast growth factor receptor (FGFR) modulator and blood-brain barrier-penetrant. FGL peptide activates NCAM-FGFR and FGFR1 signaling pathways. FGL peptide alters expression of apoptosis, signal transduction and metabolism regulator genes in traumatic brain injury contexts. FGL peptide can be used for the research of traumatic brain injury.
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Lenvatinib-d4
0 ImagesSynonyms: E7080-d4
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FGFR1 Human Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS04911FGFR1 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Infigratinib-Boc
0 ImagesInfigratinib-Boc is a derivative of Infigratinib containing a Boc (t-Butyloxy carbonyl) group. Infigratinib is an ATP-competitive pan-FGFR inhibitor.
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FGFR3 Human Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS04918FGFR3 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Formononetin-d3-1
0 ImagesCat. No.: HY-N0183S4Purity: 99.67%
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Nintedanib-13C,d3
0 ImagesCat. No.: HY-50904S1Synonyms: BIBF 1120-13C,d3Nintedanib-13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
