NVP-BGJ398 phosphate
Catalog No.
A3673
FGFR抑制剂
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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
Storage | Store at -20°C |
M.Wt | 658.47 |
Cas No. | 1310746-10-1 |
Formula | C26H34Cl2N7O7P |
Synonyms | BGJ-398 phosphate; BGJ 398 phosphate; NVP BGJ398 phosphate |
Solubility | insoluble in EtOH; ≥28.07 mg/mL in H2O with gentle warming and ultrasonic; ≥95.7 mg/mL in DMSO |
Chemical Name | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea phosphate |
SDF | Download SDF |
Canonical SMILES | COC1=C(Cl)C(NC(N(C)C2=CC(NC3=CC=C(N4CCN(CC)CC4)C=C3)=NC=N2)=O)=C(Cl)C(OC)=C1.OP(O)(O)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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