Roblitinib

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Chemical Structure| 1708971-55-4 同义名 : FGF-401
CAS号 : 1708971-55-4
货号 : A303280
分子式 : C25H30N8O4
纯度 : 99%+
分子量 : 506.557
MDL号 : MFCD31381923
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

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

DMSO: 4 mg/mL(7.9 mM)，配合低频超声，并水浴加热至45℃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：
生物活性
靶点

  • FGFR4

    FGFR4, IC50:1.9 nM
描述 Roblitinib, also known as FGF-401, is an orally active, highly selective inhibitor of FGFR4, with an IC50 of 1.9 nM. Roblitinib shows no activity against FGFR1, FGFR2, FGFR3, rat FGFR4, and C552A FGFR4 (all IC50s >10 µM). It inhibits HUH7 (IC50=12 nM), Hep3B (IC50=9 nM), JHH7 (IC50=9 nM), while showing no inhibitory activity in HEPG2 and JHH (both IC50s >10 µM)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL
参考文献

[1]Nicole Buschmann, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. WO2015059668A1.