MedKoo product information:

 BGJ-398

Description of BGJ398: BGJ398 is a pan FGFR kinase inhibitor, and is an orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. pan FGFR kinase inhibitor BGJ398 selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. FGFRs are a family of receptor tyrosine kinases which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:    Novartis Oncology.

BGJ398 is a potent, selective and orally active pan-FGFR inhibitor, with IC50s of 0.9, 1.4, 1.0 and 60 nM for FGFR1, 2, 3 and 4, respectively.

1: Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H, Wartmann M, Berghausen J, Drueckes P, Zimmerlin A, Bussiere D, Murray J, Graus Porta D. Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamin o]-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. Epub 2011 Sep 21. PubMed PMID: 21936542.