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BGJ398

(CAS No:872511-34-7)
BGJ398 (NVP-BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
CAS No:872511-34-7
Molecular Weight(MW):560.48
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 872511-34-7
Molecular formula(MF) C26H31Cl2N7O3
Molecular Weight(MW): 560.48
Alias 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea
Solubility
In vitro DMSO 1 mg/mL warmed (1.78 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
Biological Activity
Description BGJ398 (NVP-BGJ398) is a potent and selective FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. Phase 2.
Targets
FGFR1 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
FGFR2 [1]
(Cell-free assay)
FGFR3 (K650E) [1]
(Cell-free assay)
FGFR4 [1]
(Cell-free assay)
0.9 nM 1.0 nM 1.4 nM 4.9 nM 60 nM
In vitro

BGJ398 also prevents VEGFR2 with low potency. The IC50 of BGJ398 for inhibiting VEGFR2 is 0.18 μM. BGJ398 suppresses other kinases including ABL, FYN, KIT, LCK, LYN and YES with IC50 of 2.3 μM, 1.9 μM, 0.75 μM, 2.5 μM, 0.3 μM and 1.1 μM, respectively. At the cellular level, BGJ398 inhibits the proliferation of the FGFR1-, FGFR2-Q, and FGFR3-dependent BaF3 cells with IC50 of 2.9 μM, 2.0 μM and 2 μM, respectively. BGJ398 interferes with autophosphorylation on specific tyrosine residues including FGFR-WT, FGFR2-WT, FGFR3-K650E, FGFR3-S249C and FGFR4-WT with IC50 of 4.6 nM, 4.9 nM, 5 nM, 5 nM and 168 nM, respectively. BGJ398 suppresses proliferation of the cancer cells with wild-type (WT) FGFR3 overexpression such as RT112, RT4, SW780 and JMSU1 with IC50 of 5 nM, 30 nM, 32 nM and 15 nM, respectively. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC Growth Inhibition Assay 1-2500 nM 48 h  IC50= 2359 nm 25688743
HCC Growth Inhibition Assay 1-2500 nM 48 h IC50=1124 nm 25688743
HCT116 Growth Inhibition Assay 48 h IC50=3 μM 24503538
HKH2 Growth Inhibition Assay 48 h IC50=4 μM 24503538
RKO Growth Inhibition Assay 48 h IC50=1.2 μM 24503538
LS174T Growth Inhibition Assay 48 h IC50=4 μM 24503538
HCD9 Growth Inhibition Assay 0.5-5 μM 48/72 h DMSO decreases cell viability 24135816
HCT116 Growth Inhibition Assay 0.5-5 μM 48/72 h DMSO decreases cell viability 24135816
SNU-C1 Growth Inhibition Assay 0.5-5 μM 48/72 h DMSO no effect 24135816
MFE280 Growth Inhibition Assay IC50=2.63 ± 0.82 μM 23443805
AN3CA Growth Inhibition Assay IC50=1.00 ± 0.20 μM 23443805
HEC155 Growth Inhibition Assay IC50=4.74 ± 1.09 μM 23443805
MFE296 Growth Inhibition Assay IC50=2.86 ± 0.20 μM 23443805
SPAC1S Growth Inhibition Assay IC50=3.19 ± 0.93 μM 23443805
RL952 Growth Inhibition Assay IC50=3.41 ± 0.23 μM 23443805
EN1 Growth Inhibition Assay IC50=4.75 ± 0.62 μM 23443805
SNGII Growth Inhibition Assay IC50=4.29 ± 0.58 μM 23443805
ISHIKAWA Growth Inhibition Assay IC50=5.48 ± 0.03 μM 23443805
HEC1A Growth Inhibition Assay IC50=10.00 ± 1.00 μM 23443805
KLE Growth Inhibition Assay IC50=3.03 ± 0.11 μM 23443805
SNGM Growth Inhibition Assay IC50=5.00 ± 0.41 μM 23443805
USPC2 Growth Inhibition Assay IC50=7.00 ± 0.21 μM 23443805
EN Growth Inhibition Assay IC50=6.03 ± 0.31 μM 23443805
MFE319 Growth Inhibition Assay IC50=5.37 ± 0.03 μM 23443805
EFE184 Growth Inhibition Assay IC50=8.04 ± 0.69 μM 23443805
ECC1 Growth Inhibition Assay IC50=6.74 ± 0.59 μM 23443805
HEC1B Growth Inhibition Assay IC50=6.45 ± 0.67 μM 23443805
USPC1 Growth Inhibition Assay IC50=5.75 ± 0.50 μM 23443805
SPAC1L Growth Inhibition Assay IC50=4.92 ± 0.50 μM 23443805

... Click to View More Cell Line Experimental Data

In vivo In this orthotopic xenograft bladder cancer model, BGJ398 induces tumor growth inhibition and stasis after oral administration for 12 consecutive days at the doses of 10 and 30 mg/kg, respectively. Interestingly, the animals that received BGJ398 exhibits either no body weight loss (10 mg/kg) or 10% body weight gain (30 mg/kg), a further indication of efficacy. RT112 tumor-bearing and female Rowett rats receive a single oral administration of the monophosphate salt of BGJ398 at the doses of 4.25 and 8.51 mg/kg. BGJ398 significantly decreases the levels of pFRS2 and pMAPK in a dose-dependent manner. BGJ398 inhibits significantly bFGF-stimulated angiogenesis in a dose-dependent manner. However, BGJ398 does not impair VEGF-induced blood vessel formation. [1]