NVP-BGJ398 phosphate

- Overview
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    Background
    
    Description: IC50 Value: 0.9 nM (FGFR1); 1.4 nM (FGFR2); 1 nM (FGFR2) [1] NVP-BGJ398 is a novel selective, pan-specific FGFR inhibitor currently in Phase I clinical trials for cancer therapy. in vitro: NVP-BGJ398 is a novel and selective fibroblast 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 [1]. Cell lines with activating FGFR2 mutations (S252W, N550K) were more sensitive to dovitinib or NVP-BGJ398 when compared with their FGFR2 wild-type counterparts (P = 0.073 and P = 0.021, respectively). Both agents inhibited FGFR2 signaling, induced cell-cycle arrest, and significantly increased apoptosis in FGFR2-mutant lines. In vitro, dovitinib and NVP-BGJ398 were both potent at inhibiting cell growth of FGFR2-mutant endometrial cancer cells, but the activity of dovitinib was less restricted to FGFR2-mutant lines when compared with NVP-BGJ398 [2]. 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 [1].NVP-BGJ398 significantly inhibited the growth of FGFR2-mutated endometrial cancer xenograft models [2]. Toxicity: N/A Clinical trial: Phase 1
- Properties
  - Alternative Name
    
    BGJ-398 phosphate; BGJ 398 phosphate; NVP BGJ398 phosphate; 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea phosphate
    
    CAS Number
    
    1310746-10-1
    
    Molecular Formula
    
    C26H34Cl2N7O7P
    
    Molecular Weight
    
    658.47
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; ≥28.07 mg/mL in H2O with gentle warming and ultrasonic; ≥95.7 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

NVP-BGJ398 phosphate

Background

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