Description
NVP-BGJ398 (872511-34-7) is a potent and selective pan-FGFR inhibitor (IC50?= 0.9nM, 1.4 nM, 1.0 nM, and 60 nM for FGFR1,2,3,4 respectively).1? It has also been used in a mouse model of Achondroplasia (most common form of dwarfism) to correct pathological hallmarks of this condition.
Definition
ChEBI: BGJ-398 is a member of the class of phenylureas that is urea in which a hydrogen attached to one of the nitrogens is replaced by a 2,6-dichloro-3,5-dimethoxyphenyl group, while the hydrogens attached to the other nitrogen are replaced by a methyl group and a 6-{[4-(4-ethylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl group. It is a potent and selective fibroblast growth factor receptor inhibitor. It has a role as a fibroblast growth factor receptor antagonist and an antineoplastic agent. It is an aminopyrimidine, a N-arylpiperazine, a N-alkylpiperazine, a dichlorobenzene and a member of phenylureas.
General Description
Class: receptor tyrosine kinase;
Treatment: cholangiocarcinoma;
Other name: NVP-BGJ398;
Elimination half-life = 34 h;
Protein binding = 96.8%
IC 50
FGFR1~4 IC50 = 0.9, 1.4, 1.0, and 60
nM; VEGFR2 IC50 = 180 nM
References
1) Guagnano?et al.?(2011),?Discovery of 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-{[4-(4-ethyl-1-piperazinyl)phenyl]amino}-4-pyrimidinyl)-1-methylurea (NVP-BGJ398),?a Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase?; J. Med. Chem.?54?7066
2) Komla-Ebri?et al.?(2016),?Tyrosine kinase inhibitor NVP-BGJ398 functionally improves FGFR3-related dwarfism in mouse model; J. Clin. Invest.?126?1871
