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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MAX-40279 hydrochloride
0 ImagesCat. No.: HY-145723ACAS No.: 2388506-51-0MAX-40279 hydrochloride is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hydrochloride 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 hydrochloride inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hydrochloride can be used for the research of acute myelogenous leukemia (AML).
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MAX-40279 hemifumarate
0 ImagesCat. No.: HY-145723BCAS No.: 2388506-43-0MAX-40279 hemifumarate is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemifumarate 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 hemifumarate inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemifumarate can be used for the research of acute myelogenous leukemia (AML).
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Antitumor agent-177
0 ImagesCat. No.: HY-161841Antitumor agent-177 (compound 57), a non-steroidal NSC12 derivative, shows potent FGF2 binding affinity with a Kd of 24 μM by SPR. Antitumor agent-177 significantly inhibits the formation of HSPG/FGF2/FGFR1 ternary complexes. Antitumor agent-177 inhibits FGFR activation and exerts a potent anti-tumor activity on multiple myeloma (MM) cell lines in vitro and in vivo.
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FGFR1/VEGFR2-IN-2
0 ImagesCat. No.: HY-161995FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells.
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FIIN-4
0 ImagesCat. No.: HY-123134CAS No.: 2093088-81-2FIIN-4 is a first-in-class, orally active and covalent FGFR inhibitor with IC50s of 2.6 nM, 2.6 nM, 5.6 nM, 9.2 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. FIIN-4 can inhibit metastatic tumor growth.
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FGFR4-IN-14
0 ImagesCat. No.: HY-155046CAS No.: 3027827-02-4FGFR4-IN-14 (Compound 27i) is a FGFR4 inhibitor (IC50: 2.4 nM. FGFR4-IN-14 inhibits the proliferation of V550L and N535K mutant strains, with IC50s of 21 nM, 2.5 nM, 171 nM against huh7, BaF3/ETV6-FGFR4-V550L and BaF3/ETV6-FGFR4-N535K cells respectively. FGFR4-IN-14 has potent antitumor efficacy in the Huh7 xenograft model. FGFR4-IN-14 can be used for research of hepatocellular carcinoma (HCC).
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FGFR2 K659M Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70818FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 K659M is a mutant of FGFR3. FGFR2 K659M Recombinant Human Active Protein Kinase is a recombinant FGFR2 K659M protein that can be used to study FGFR2 K659M-related functions.
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FGFR-IN-4
0 ImagesCat. No.: HY-147619CAS No.: 2761211-49-6FGFR-IN-4 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-4 has the potential for the research of cancer diseases (extracted from patent WO2022033532A1, compound 20). FGFR-IN-4 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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FGFR1 inhibitor 7
0 ImagesCat. No.: HY-149486FGFR1 inhibitor 7 (compound 5) is an inhibitor of FGFR1 Tyrosine Kinase with IC50 value of 0.33 nM. FGFR1 inhibitor 7 shows broad-spectrum cytotoxicity agasinst human cancer cell lines, and inhibits MOLT3 cells with IC50 of 2.1 μM.
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FGFR2 N549K Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70823FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 N549K is a mutant of FGFR3. FGFR2 N549K Recombinant Human Active Protein Kinase is a recombinant FGFR4 N535K protein that can be used to study FGFR4 N535K-related functions.
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Lenvatinib-d5
0 ImagesCat. No.: HY-10981S1Synonyms: E7080-d5; MK-7902-d5
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FGFR-IN-14
0 ImagesCat. No.: HY-162577CAS No.: 3047446-75-0FGFR-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.
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FGFR1 inhibitor-11
0 ImagesCat. No.: HY-158098CAS No.: 2157482-40-9FGFR1 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.
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FGFR2 Human Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS04915FGFR2 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.
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IONIS-FGFR4Rx sodium scrambled negative control
0 ImagesCat. No.: HY-159691BIONIS-FGFR4Rx sodium scrambled negative control is the sequence scrambled negative control of IONIS-FGFR4Rx sodium.
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Pep1-DNP conjugate 9
0 ImagesCat. No.: HY-P10870Pep1-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.
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FGFR-IN-3
0 ImagesCat. No.: HY-147683CAS No.: 2488762-63-4FGFR-IN-3 (compound 6) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-3 shows neuroprotective activity. FGFR-IN-3 can be used for neurodegenerative diseases research.
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PROTAC FGFR3 Degrader-1
0 ImagesCat. No.: HY-181153PROTAC FGFR3 Degrader-1 is a fibroblast growth factor receptor 3 (FGFR3) PROTAC degrader, promotes FGFR3 degradation via the ubiquitin-proteasome pathway, and inhibits the downstream FGFR3/PI3K/AKT signaling pathway. PROTAC FGFR3 Degrader-1 can be used for the research of hepatocellular carcinoma.
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Pazopanib-13C,d3
0 ImagesCat. No.: HY-10208S1CAS No.: 1261734-88-6Synonyms: GW786034-13C,d3
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Tec-IN-6
0 ImagesCat. No.: HY-123541CAS No.: 923762-87-2
