Description
NVP-BGJ398 inhibit FGFR1, FGFR2, FGFR3 with IC50 of 0.9 nM, 1.4 nM and 1 nM.
Storage
2 years at -20centigrade Powder
Targets
FGFR1, FGFR2, FGFR3
Molecular Formula
C26H31Cl2N7O3
Chemical Name
3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-(4-(4-ethylpiperazin-1-yl)phenylamino)pyrimidin-4-yl)-1-methylurea
Solubility
DMSO 2 mg/mL Water
In vitro
NVP-BGJ398 is a novel and selective ?broblast growth factor receptor (FGFR) inhibitor. NVP-BGJ398 inhibit FGFR1, FGFR2, FGFR3 with IC50 of 0.9 nM, 1.4 nM and 1 nM. NVP-BGJ398 inhibited FGFR1, FGFR2, and FGFR3 with single digit nmol/L IC50 in biochemical and cellular autophosphorylation assays and FGFR4 with 38- to 60-fold lower potency. NVP-BGJ398 significantly inhibits proliferation of cancer cell lines bearing FGF/FGFR genetic alterations across various cancer types.Among the 35 cell lines selected from the high-throughput assays, 28 were confirmed as sensitive to NVP-BGJ398 with IC50s ranging from 0.001 to 500 nM. Cancer cell lines harboring FGF19 copy number gain at the 11q13 amplicon are sensitive to NVP-BGJ398 only when concomitant expression of beta-klotho occurs.
In vivo
In tumor tissues from primary tumor model GAM033 treated with 15 mg/kg NVP-BGJ398, NVP-BGJ398 shows inhibition to FGFR and ERK1/2.
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