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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Infigratinib phosphate (Standard)
0 ImagesSynonyms: BGJ-398 phosphate (Standard); NVP-BGJ398 phosphate (Standard)Infigratinib phosphate (Standard) is the analytical standard of Infigratinib phosphate. This product is intended for research and analytical applications. Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
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Pazopanib-d3
0 ImagesCat. No.: HY-10208S2CAS No.: 1219591-97-5Synonyms: GW786034-d3
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XL 999 (Standard)
0 ImagesCat. No.: HY-100315RCAS No.: 705946-27-6Synonyms: Tyrosine kinase-IN-1 (Standard)XL 999 (Standard) is the analytical standard of XL 999 (HY-100315). This product is intended for research and analytical applications. XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC50 values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer.
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Lucitanib (Standard)
0 ImagesCat. No.: HY-15391RCAS No.: 1058137-23-7Synonyms: E-3810 (Standard)Lucitanib (Standard) is the analytical standard of Lucitanib. This product is intended for research and analytical applications. Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
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E7090 (Standard)
0 ImagesCat. No.: HY-101466RCAS No.: 1622204-21-0E7090 (Standard) is the analytical standard of E7090 (HY-101466). This product is intended for research and analytical applications. E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively.
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TG 100572 hydrochloride (Standard)
0 ImagesCat. No.: HY-10185RCAS No.: 867331-64-4TG 100572 hydrochloride (Standard) is the analytical standard of TG 100572 hydrochloride (HY-10185). This product is intended for research and analytical applications. TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
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KW-2449 (Standard)
0 ImagesCat. No.: HY-10339RCAS No.: 1000669-72-6
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Dovitinib lactate (Standard)
0 ImagesSynonyms: CHIR-258 lactate (Standard); TKI-258 lactate (Standard)Dovitinib (lactate) (Standard) is the analytical standard of Dovitinib (lactate). This product is intended for research and analytical applications. Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
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Lenvatinib mesylate (Standard)
0 ImagesSynonyms: E7080 mesylate (Standard); MK-7902 mesylate (Standard)Lenvatinib (mesylate) (Standard) is the analytical standard of Lenvatinib (mesylate). This product is intended for research and analytical applications. Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
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H3B-6527 (Standard)
0 ImagesCat. No.: HY-100491RCAS No.: 1702259-66-2H3B-6527 (Standard) is the analytical standard of H3B-6527 (HY-100491). This product is intended for research and analytical applications. H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity.
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Pazopanib-d3 hydrochloride
0 ImagesCat. No.: HY-W705479CAS No.: 2469755-67-5Synonyms: GW786034-d3 hydrochloridePazopanib-d3 (hydrochloride) (GW786034-d3 (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
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ENMD-2076 (Standard)
0 ImagesCat. No.: HY-10987ARCAS No.: 934353-76-1ENMD-2076 (Standard) is the analytical standard of ENMD-2076 (HY-10987A). This product is intended for research and analytical applications. ENMD-2076 is a multi-targeted Kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KdR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
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SU 5402 (Standard)
0 ImagesCat. No.: HY-10407RCAS No.: 215543-92-3
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Roblitinib (Standard)
0 ImagesSynonyms: FGF-401 (Standard)Roblitinib (Standard) is the analytical standard of Roblitinib (HY-101568). This product is intended for research and analytical applications. Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
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AFG210
0 ImagesCat. No.: HY-18817CAS No.: 228400-22-4AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC50=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase.
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Pemigatinib-d6
0 ImagesCat. No.: HY-W754878CAS No.: 2649492-49-7Synonyms: INCB054828-d6Pemigatinib-d6 (INCB054828-d6) is deuterium labeled Pemigatinib. Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.
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Ponatinib (Standard)
0 ImagesSynonyms: AP24534 (Standard)Ponatinib (Standard) is the analytical standard of Ponatinib. This product is intended for research and analytical applications. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
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Ponatinib hydrochloride (Standard)
0 ImagesSynonyms: AP24534 hydrochloride (Standard)Ponatinib (hydrochloride) (Standard) is the analytical standard of Ponatinib (hydrochloride). This product is intended for research and analytical applications. Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
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JK-P3 (Standard)
0 ImagesCat. No.: HY-108933RCAS No.: 942655-44-9JK-P3 (Standard) is the analytical standard of JK-P3 (HY-108933). This product is intended for research and analytical applications. JK-P3 is a potent and pan VEGFR2 inhibitor, with IC50s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well as fibroblast growth factor receptor Kinase activity in vitro. JK-P3 has anti-angiogenic activity.
