产品说明书

Filgotinib

Print
Chemical Structure| 1206161-97-8 同义名 : -
CAS号 : 1206161-97-8
货号 : A302163
分子式 : C21H23N5O3S
纯度 : 99%
分子量 : 425.504
MDL号 : MFCD20527867
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(58.75 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：

IP 2% DMSO+2% Tween80+40% PEG300+water 4.4 mg/mL clear

PO 0.5% CMC-Na 46 mg/mL suspension

生物活性
靶点

  • JAK1

    JAK1, IC50:10 nM

  • JAK3

    JAK3, IC50:810 nM

  • Tyk2

    TYK2, IC50:116 nM

  • JAK2

    JAK2, IC50:28 nM
描述 Filgotinib, identified as GLPG0634, selectively inhibits the differentiation of Th2 cells by interfering with IL-4 signaling, which is mediated through JAK1 and JAK3, showcasing dose-dependent efficacy at concentrations of 1 μM or lower. This action also extends to Th1 cell differentiation, indicating its broad immunomodulatory potential[1]. Remarkably, Filgotinib does not impact JAK2 homodimer-mediated pathways triggered by erythropoietin (EPO) or prolactin (PRL), with its IC50 exceeding 10 μM. This specificity underscores its targeted approach in modulating immune responses without affecting certain critical hematopoietic signals[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human CD34+ cells Function assay 45 mins Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis 24417533
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.75mL

2.35mL

1.18mL

23.50mL

4.70mL

2.35mL
参考文献

[1]Van Rompaey L, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013, 191(7), 3568-3577.

[2]Menet CJ, et al. Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634. J Med Chem. 2014 Nov 17.