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Fibroblast growth factor receptor (FGFR) inhibitors act on FGFR1 to FGFR4, four receptor tyrosine kinases. FGFR signaling controls cell proliferation, migration and differentiation in development and angiogenesis. Amplifications, activating mutations and gene fusions of FGFR genes have been found in many tumor types. PD173074 was crystallized with the FGFR1 kinase domain in 1998, which showed how it occupies the adenosine triphosphate (ATP) pocket. Infigratinib and fexagratinib are FGFR-focused inhibitors used to study cells that depend on FGFR signaling. Nintedanib and pazopanib HCl inhibit FGFR together with vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs). Kinases outside the FGFR family are covered by sibling categories such as VEGFR and PDGFR.
LC-MB12 is an orally active PROTAC compound that targets FGFR2 degradation, with a DC₅₀ of 11.8 nM. It consists of the FGFR2 inhibitor BGJ398, a PROTAC linker, and a cereblon (CRBN) ligand. LC-MB12 effectively inhibits FGFR2 signaling in gastric cancer cells and exhibits antitumor activity.
PROTAC FGFR2 degrader 1 is a specialized degrader designed to selectively target and degrade FGFR2, exhibiting a DC50 of 6.46 nM and an FGFR2 IC50 of 0.08 nM. This compound demonstrates significant anti-proliferative activity, inducing G0/G1 cell cycle arrest in KATOIII and SNU16 cell lines while inhibiting apoptosis through modulation of downstream signaling proteins, p-ERK and p-PLCγ. In in vivo studies, PROTAC FGFR2 degrader 1 effectively suppresses the growth of SNU16 xenograft tumors, showcasing its potential for research in gastric cancer therapeutic applications.
SNIPER(TACC3)-11 is a potent degrader of the FGFR3-TACC3 fusion protein, utilizing targeted protein degradation to reduce its levels within cells. This compound effectively suppresses the proliferation of cancer cells that express the FGFR3-TACC3 fusion, making it a valuable tool for research related to targeting oncogenic protein fusions in cancer therapy. Its potential applications include studies in cancer biology and the development of novel therapeutic strategies against FGFR3-TACC3-positive tumors.
DGY-09-192 is a PROTAC degrader targeting FGFR1 and FGFR2, demonstrating DC50 values of 4.35 nM and 70 nM, respectively. This compound selectively degrades both wild-type FGFR1/2 and various FGFR2 fusion proteins, such as FGFR2-PHGDH and FGFR2-OPTN. By suppressing downstream FGFR signaling, DGY-09-192 effectively reduces the phosphorylation of key targets including FRS2 Y196 and ERK1/2 T202/Y204, making it a valuable tool for investigating FGFR-driven malignancies in both in vitro and in vivo studies.
