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Baricitinib (LY3009104, INCB028050)
JAK1/JAK2 inhibitor,selective orally bioavailable

Baricitinib (LY3009104, INCB028050)

Catalog No. A4141
Size Price Stock Qty
5mg $70.00 In stock
10mg $90.00 In stock
50mg $250.00 In stock
200mg $750.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Baricitinib (LY3009104, INCB028050)

Biological Activity

Description Baricitinib (LY3009104, INCB028050) is a selective inhibitor of JAK1 and JAK2 with IC50 values of 5.9 nM and 5.7 nM,
Targets JAK2 JAK1 TYK2 JAK3 Chk2 c-Met
IC50 5.7 nM 5.9 nM 53 nM >400 nM >1 μM >10 μM

Baricitinib (LY3009104, INCB028050) Dilution Calculator

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Baricitinib (LY3009104, INCB028050) Molarity Calculator

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Chemical Properties

Cas No. 1187594-09-7 SDF Download SDF
Synonyms INCB 028050,INCB-028050,LY 3009104,LY-3009104
Chemical Name 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile
Canonical SMILES CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
Formula C16H17N7O2S M.Wt 371.42
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Baricitinib, formerly named LY3009104 or INCB028050, is a new selective orally bioavailable inhibitor of tyrosine-protein kinase JAK1 or JAK2. Also, it is an ATP competitive kinase inhibitor. In vitro, it is able to inhibit JAK1 and JAK2 in a low nanomolar range with IC50 values of 5.9 and 5.7 nM, respectively, while it demonstrates low inhibitory activity for JAK3 and moderate activity for TYK2. Baricitinib inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. It should also be recognized that JAK signaling is central to a number of fundamental processes, including the generation of RBCs

Reference

Gras, J. Baricitinib. Tyrosine-protein kinase JAK1/JAK2 inhibitor, treatment of rheumatoid arthritis. Drugs of the future. 2013, 38(9): 611.

Jordan S. Fridman, Peggy A. Scherle, Robert Collins, Timothy C. Burn, Yanlong Li, Jun Li, Maryanne B. Covington, Beth Thomas, Paul Collier, Margaret F. Favata, Xiaoming Wen, Jack Shi, Ryan McGee, Patrick J. Haley, Stacey Shepard, James D. Rodgers, Swamy Yeleswaram, Greg Hollis, Robert C. Newton, Brian Metcalf, Steven M. Friedman and Kris Vaddi. Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050. The Journal of Immunology May 1, 2010 vol. 184 no. 9 5298-5307.