产品说明书

Baricitinib

Print
Chemical Structure| 1187594-09-7 同义名 : 巴瑞克替尼 ;LY3009104;INCB028050
CAS号 : 1187594-09-7
货号 : A102707
分子式 : C16H17N7O2S
纯度 : 99%
分子量 : 371.417
MDL号 : MFCD27920779
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(67.31 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：

2% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
靶点

  • JAK1

    JAK1, IC50:5.9 nM

  • Tyk2

    TYK2, IC50:53 nM

  • JAK2

    JAK2, IC50:5.7 nM
描述 Baricitinib (INCB028050) is demonstrated as a potent inhibitor of Janus kinase (JAK) signaling and functionality in cell-based assays. In peripheral blood mononuclear cells (PBMCs), Baricitinib curtails IL-6-induced phosphorylation of STAT3 (pSTAT3) and the subsequent secretion of the chemokine MCP-1, with IC50 values being 44 nM and 40 nM, respectively. Furthermore, in isolated naive T-cells, it suppresses pSTAT3 activation by IL-23 with an IC50 value of 20 nM, significantly inhibiting the production of IL-17 and IL-22, two cytokines produced by Th17 cells, known for their inflammatory and pathogenic roles, with an IC50 of 50 nM. This is in sharp contrast to structurally similar but less effective JAK1/2 inhibitors INCB027753 and INCB029843, which show no notable effect in these assay systems up to 10 μM[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
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, IC50=0.0878μM 24417533
human TF1 cells Function assay Inhibition of JAK1 in human TF1 cells assessed as suppression of IL6-stimulated STAT3 phosphorylation by AlphaScreen assay 26372653
human UT7 cells Function assay Inhibition of JAK2 in human UT7 cells assessed as suppression of EPO-stimulated STAT5 phosphorylation by AlphaScreen assay 26372653
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03440892 - Recruiting January 2020 Sweden ... 展开 >> Dept of Rheumatology and Inflammation research Recruiting Gothenburg, Sweden Contact: Sofia T Silfverswärd       sofia.silfversward@rheuma.gu.se 收起 <<
NCT01185353 Arthritis, Rheumatoid Phase 2 Completed - -
NCT01398475 Chronic Inflammatory Disorder ... 展开 >> Arthritis, Rheumatoid 收起 << Phase 1 Completed - Singapore ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Singapore, Singapore, 117597 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL
参考文献

[1]Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307.

[2]Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5.