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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-Baricitinib
Baricitinib

Chemical Structure : Baricitinib

CAS No.: 1187594-09-7

Baricitinib (LY3009104, INCB028050)

货号: PC-73190Not For Human Use, Lab Use Only.

Baricitinib (LY3009104, INCB028050) is a potent, selective and orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9/5.7 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Baricitinib (LY3009104, INCB028050) is a potent, selective and orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9/5.7 nM, respectively.
Baricitinib (LY3009104, INCB028050) shows moderate selectivity against Tyk2 (IC50=53 nM) and 100-fold selectivity over JAK3.
INCB028050 inhibited IL-6–stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively, in PBMCs.
Baricitinib (LY3009104, INCB028050) suppressed phosphorylated STAT3 in the peripheral blood of rAIA animals.
Baricitinib (LY3009104, INCB028050) (10 mg/kg) reduces elevated cytokine mRNA levels in draining lymph nodes from rats with AIA.

物理化学性质&存储条件

分子量 371.42
分子式 C16H17N7O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(3-(4-(3H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile

参考文献

1. Fridman JS, et al. J Immunol. 2010 May 1;184(9):5298-307.

2. Migita K, et al. Clin Exp Immunol. 2013 Dec;174(3):356-63.

3. Genovese MC, et al. N Engl J Med. 2016 Mar 31;374(13):1243-52.

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