同义名 :	BGJ-398 phosphate; NVP-BGJ398 phosphate
	CAS号 :	1310746-10-1
	货号 :	A980301
	分子式 :	C26H34Cl2N7O7P
	纯度 :	98%
	分子量 :	658.47
	MDL号 :	MFCD26960938
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	The FGFR (fibroblast growth factor receptor) family, comprising four members, FGFR1, FGFR2, FGFR3 and FGFR4, belongs to the RTKs which serve as high affinity receptors for FGFs controlling cell proliferation, migration, apoptosis and differentiation. BGJ398 is a selective and potent inhibitor of FGFRs with IC50 values of 1nM for FGFR11-3 and 60nM for FGFR4, as well as 4.9nM for FGFR3-K650E mutant (measured by purified recombinant enzymes). Treatment with BGJ398 in cell lysate from HEK293 cells transfected with FGFRs resulted in inhibition on autophosphorylation on specific tyrosine residues of FGFR 1-3 with IC50 values below 5nM. Consistent with the in vitro study, BGJ398 inhibited the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values ranged from 0.7-52.2nM depended by different FGFR isoforms. Daily oral treatment with BGJ398 at dose of 10 or 30mg/kg for 12 consecutive days induced tumor growth inhibition in the orthotopic xenograft bladder cancer model. Similarly, nearly complete tumor stasis was achieved by oral treatment of BGJ398 at dose of 5, 10 and 15mg/kg in RT112 human bladder cancer xenografted rats.[1]
作用机制	BGJ398 Phosphate binds with ATP-binding pocket of FGFR3.[1]

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.52mL 0.30mL 0.15mL	7.59mL 1.52mL 0.76mL	15.19mL 3.04mL 1.52mL

参考文献
[1]Guagnano V, Furet P, 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.