Infigratinib

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Chemical Structure| 872511-34-7 同义名 : NVP-BGJ398;BGJ398;​NVP-BGJ398
CAS号 : 872511-34-7
货号 : A107926
分子式 : C26H31Cl2N7O3
纯度 : 99%+
分子量 : 560.475
MDL号 : MFCD22123241
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(21.41 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

1%CMC-Na+water 30 mg/mL suspension

生物活性
靶点

  • FGFR2

    FGFR2, IC50:1.4 nM

  • FGFR3

    FGFR3, IC50:1.0 nM

    FGFR3 (K650E), IC50:4.9 nM

  • FGFR4

    FGFR4, IC50:60 nM

  • FGFR1

    FGFR1, IC50:0.9 nM
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 1 nM for FGFR11-3 and 60 nM for FGFR4, as well as 4.9 nM 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 5 nM. 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 - 52.2 nM depended by different FGFR isoforms. Daily oral treatment with BGJ398 at dose of 10 or 30 mg/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 15 mg/kg in RT112 human bladder cancer xenografted rats[1].
作用机制 BGJ398 binds with ATP-binding pocket of FGFR3[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
AN3CA Growth Inhibition Assay IC50=1.00 ± 0.20 μM 23443805
ECC1 Growth Inhibition Assay IC50=6.74 ± 0.59 μM 23443805
EFE184 Growth Inhibition Assay IC50=8.04 ± 0.69 μM 23443805
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.92mL

1.78mL

0.89mL

17.84mL

3.57mL

1.78mL
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.

[2]Xiao L, Du E, et al. Inhibition of FGFR Signaling Partially Rescues Hypophosphatemic Rickets in HMWFGF2 Tg Male Mice. Endocrinology. 2017 Oct 1;158(10):3629-3646.