B-1600 Baricitinib, Free Base, >99%

Solubility: DMSO.

BRC-101

View the SDS for this product

• Baricitinib, also known as INCB028050, is a janus kinase (JAK) inhibitor.  It potently and selectively inhibited JAK1 and JAK2 kinases with IC50 values of 5.9 nM and 5.7 nM, respectively.  It inhibited intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23, with IC50 values of <50 nM.  Baricitinib at doses providing partial and/or periodic inhibition of JAK1/JAK2 significantly improved rheumatoid arthritis as assessed by clinical, histologic and radiographic signs of disease in the rat adjuvant arthritis model.  It was also effective in multiple murine models of arthritis.  Fridman J.S., et al. "Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050." J. Immunol. 184: 5298-5307 (2010).
• Baricitinib was well tolerated and demonstrated clinically meaningful responses in patients with active rheumatois arthritis.  Greenwald M.W., et al. "A Randomized Dose-Ranging, Placebo-Controlled Study of INCB028050, a Selective JAK1 and JAK2 Inhibitor in Subjects with Active Rheumatoid Arthritis." http://www.blackwellpublishing.com/acrmeeting/abstract.asp?MeetingID=774&id=90814.
• Baricitinib reversed alopecia areata in in vivo preclinical studies and in patients.  Jabbari A., et al. "Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib." EBioMedicine. 2: 351-355 (2015).
• Related  CAS numbers: 1187595-84-1 for the phosphate salt; 1187594-10-0 for the trifluoroacetate salt.
• Other CAS numbers previously assigned to Baricitinib, Free Base, 1231199-29-3 and 1374987-77-5, have been deleted by CAS and are no longer in use.
• Baricitinib is the active ingredient in the drug product sold under the trade name Olumiant®.  This drug is currently approved in a least one country for treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response to one or more TNF antagonist therapies. NOTE: THE BARICITINIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT OLUMIANT®, AND IS NOT FOR HUMAN USE.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This  product is offered for R&D use in accordance with (i) 35 USC  271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in  Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in  Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977  in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law  exemptions of Canadian patent law; (vi) Section 68B of the Patents Act  of 1953 in New Zealand together with the amendment of same by the  Statutes Amendment Bill of 2002; (vii) such related legislation and/or  case law as may be or become applicable in the aforementioned countries;  and (viii) such similar laws and rules as may apply in various other  countries.
• Not available in some countries; not available to some institutions; not available for some uses.