Description
NVP-BGJ398 is an inhibitor of FGFR that exhibits anticancer chemotherapeutic and antirachitic activities. NVP-BGJ398 inhibits cell viability in colon cancer cells and prevents progression and tumor formation in animal models of malignant rhabdoid tumors. In endometrial cancer cells, NVP-BGJ398 induces cell cycle arrest and inhibits growth; in vivo, it also inhibits tumor growth. NVP-BGJ398 inhibits aberrant FGFR signaling in animal models of rickets disease, normalizing bone growth and mineralization.
References
Turkington RC, Longley DB, Allen WL, et al. Fibroblast growth factor receptor 4 (FGFR4): a targetable regulator of drug resistance in colorectal cancer. Cell Death Dis. 2014 Feb 6;5:e1046. PMID: 24503538.
Wöhrle S, Weiss A, Ito M, et al. Fibroblast growth factor receptors as novel therapeutic targets in SNF5-deleted malignant rhabdoid tumors. PLoS One. 2013 Oct 30;8(10):e77652. PMID: 24204904.
Konecny GE, Kolarova T, O'Brien NA, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42. PMID: 23443805.
Wöhrle S, Henninger C, Bonny O, et al. Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911. PMID: 23129509.
Guagnano V, Furet P, Spanka C, et al. Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem. 2011 Oct 27;54(20):7066-83. PMID: 21936542.
