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Baricitinib

Chemical Structure : Baricitinib

CAS No.: 1187594-09-7

Baricitinib (LY3009104, INCB028050)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 371.42
Formula C16H17N7O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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