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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cRY9M acetate
0 ImagesCat. No.: HY-P11853AcRY9M acetate is a cyclic peptide that binds to FGFR1, with a KD value of 58 nM. cRY9M acetate binds specifically to FGFR1, exhibits enhanced in vivo stability, and shows extremely low degradation in blood, urine and liver homogenate after injection. cRY9M acetate 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 acetate 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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3-Ethyltoluene
0 ImagesSynonyms: 3-Methylethylbenzene3-Ethyltoluene (3-Methylethylbenzene) is an isomer of Ethyltoluenes. 3-Ethyltoluene inhibits cell survival and proliferation and increases ROS production. 3-Ethyltoluene upregulates cellular inflammatory gene expression. 3-Ethyltoluene induces cell fibrosis with increased level of AST, FGF-23, Cyt-7 p21, TGFβ, TIMP2, and MMP2. 3-Ethyltoluene can be used for liver diseases such as NAFLD research.
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FGFR1 V561M Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70717FGFR1 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.
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B-Raf IN 17
0 ImagesCat. No.: HY-158027B-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.
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FGFR4 V550E Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70722FGFR4 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.
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FGFR3 K650M Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70720FGFR3 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.
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FGFR2 K526E Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70815FGFR2 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.
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FGFR2 V564L Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70827FGFR2 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.
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FGFR1 inhibitor-9
0 ImagesCat. No.: HY-149488FGFR1 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.
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FGFR-IN-6
0 ImagesCat. No.: HY-147621CAS No.: 2762955-18-8
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Dovitinib-d8
0 ImagesCat. No.: HY-50905SCAS No.: 1246819-84-0
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IONIS-FGFR4Rx
0 ImagesCat. No.: HY-159691CAS No.: 1416376-17-4Synonyms: ISIS 463588IONIS-FGFR4Rx (ISIS 463588) is an antisense inhibitor of fibroblast growth factor receptor 4 (FGFR4), which is promising for research of renal diseases.
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INCB126503
0 ImagesCat. No.: HY-174154CAS No.: 2640089-88-7INCB126503 is an orally activeM, selective FGFR2/3 Inhibitor with IC50 values of 70 nM (FGFR1), 2.1 nM (FGFR2), 1.2 nM (FGFR3), 0.92 nM (FGFR3-V555L), 0.85 nM (FGFR3-V555M) and 64 nM (FGFR4). INCB126503 suppresses FGFR signaling in vivo without causing hyperphosphatemia and shows antitumor efficacy in xenograft models harboring FGFR3 genetic alterations.
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FGFR3 V555M Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70829FGFR3 kinase mutations are associated with a variety of malignancies. FGFR3 V555M mutation leads to resistance to FGFR inhibitors. FGFR3 V555M Recombinant Human Active Protein Kinase is a recombinant FGFR3 V555M protein that can be used to study FGFR3 V555M-related functions.
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FGFR4-IN-17
0 ImagesCat. No.: HY-163273CAS No.: 3011805-61-8FGFR4-IN-17 (Compound (S)-23) is a piperazinyl diflurindan derivative containing pyridinyl. FGFR4-IN-17 is a FGFR inhibitor with IC50 values of 24.2, 16.1, 78.0, and 68.0 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. FGFR4-IN-17 has antitumor activity.
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FGFR3 V555L Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70828FGFR3 kinase mutations are associated with a variety of malignancies. FGFR3 V555L mutation leads to resistance to FGFR inhibitors. FGFR3 V555L Recombinant Human Active Protein Kinase is a recombinant FGFR3 V555L protein that can be used to study FGFR3 V555L-related functions.
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HuGAL-F2
0 ImagesCat. No.: HY-P990597Purity: 98.30%
