Baricitinib


CAS No. : 1187594-09-7

Baricitinib,1187594-09-7
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000674
Synonyms:2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile
Molecular Formula:C₁₆H₁₇N₇O₂S
Molecular Weight:371.42
Target:JAK
IC50:JAK1 (5.9 nM) and JAK2 (5.7 nM) [1].
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Appearance:white solid powder
Purity: > 98%
Cat No:I000674
Cas No:1187594-09-7
Product-Name:Baricitinib
InChI:InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)
InChIKey:XUZMWHLSFXCVMG-UHFFFAOYSA-N
SMILES:CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

Baricitinib(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
IC50 Value: JAK1 (5.9 nM) and JAK2 (5.7 nM) [1].
Target: JAK1/2
in vitro: INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. Significant efficacy, as assessed by improvements in clinical, histologic and radiographic signs of disease, was achieved in the rat adjuvant arthritis model with doses of INCB028050 providing partial and/or periodic inhibition of JAK1/JAK2 and no inhibition of JAK3 [1].
in vivo: The efficacy following daily oral administration of INCB028050 was assessed at doses of 1, 3, or 10 mg/kg based on its pharmacokinetic profile in this species. Disease severity was assessed periodically, scoring clinical signs of disease. These doses were based on the PK/PD relationship established with the IL-6 WBA, with the goal of inhibiting JAK1/2 signaling by no more than 50% for half of the day. Relative to vehicle-treated animals, increasing doses of INCB028050 inhibited disease scores by 24% (p < 0.05), 57% (p < 0.01), and 81% (p < 0.01), respectively [1]. Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies [2].
Clinical trial: Baricitinib (LY3009104, INCB28050) against JAK1/JAK2 starting phase IIb for rheumatoid arthritis


1:[Success for a new generation of disease-modifying antirheumatic drugs : The Janus kinase inhibitor baricitinib in rheumatoid arthritis]. Keyßer G.Z Rheumatol. 2017 Apr 26. doi: 10.1007/s00393-017-0307-3. [Epub ahead of print] Review. German. No abstract available. PMID: 28447156
2:Efficacy and safety of baricitinib in Japanese patients with active rheumatoid arthritis: A 52-week, randomized, single-blind, extension study. Tanaka Y, Ishii T, Cai Z, Schlichting D, Rooney T, Macias W.Mod Rheumatol. 2017 Apr 25:1-10. doi: 10.1080/14397595.2017.1307899. [Epub ahead of print] PMID: 28440680
3:Patient-reported outcomes from a phase III study of baricitinib in patients with conventional synthetic DMARD-refractory rheumatoid arthritis. Emery P, Blanco R, Maldonado Cocco J, Chen YC, Gaich CL, DeLozier AM, de Bono S, Liu J, Rooney T, Chang CH, Dougados M.RMD Open. 2017 Mar 21;3(1):e000410. doi: 10.1136/rmdopen-2016-000410. eCollection 2017. PMID: 28405473 Free PMC Article
4:Questioning the Effectiveness of Baricitinib for Pulmonary Manifestations of Rheumatoid Arthritis. Chertoff J, Ataya A.Am J Respir Crit Care Med. 2017 Mar 30. doi: 10.1164/rccm.201703-0552LE. [Epub ahead of print] No abstract available. PMID: 28358994
5:Baricitinib: First Global Approval. Markham A.Drugs. 2017 Apr;77(6):697-704. doi: 10.1007/s40265-017-0723-3. Review. PMID: 28290136
6:Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential. Kuriya B, Cohen MD, Keystone E.Ther Adv Musculoskelet Dis. 2017 Feb;9(2):37-44. doi: 10.1177/1759720X16687481. Epub 2017 Jan 23. Review. PMID: 28255337 Free PMC Article
7:Rheumatoid Arthritis: Baricitinib more effective than adalimumab. McHugh J.Nat Rev Rheumatol. 2017 Apr;13(4):197. doi: 10.1038/nrrheum.2017.32. Epub 2017 Mar 2. No abstract available. PMID: 28250459
8:Baricitinib versus Placebo or Adalimumab in Rheumatoid Arthritis. Taylor PC, Keystone EC, van der Heijde D, Weinblatt ME, Del Carmen Morales L, Reyes Gonzaga J, Yakushin S, Ishii T, Emoto K, Beattie S, Arora V, Gaich C, Rooney T, Schlichting D, Macias WL, de Bono S, Tanaka Y.N Engl J Med. 2017 Feb 16;376(7):652-662. doi: 10.1056/NEJMoa1608345. PMID: 28199814
9:Comparative efficacy and safety of baricitinib 2 mg and 4 mg in patients with active rheumatoid arthritis : A Bayesian network meta-analysis of randomized controlled trials. Lee YH, Bae SC.Z Rheumatol. 2017 Jan 17. doi: 10.1007/s00393-016-0254-4. [Epub ahead of print] PMID: 28097393
10:Effects of Baricitinib on Lipid, Apolipoprotein, and Lipoprotein Particle Profiles in a Phase IIb Study of Patients With Active Rheumatoid Arthritis. Kremer JM, Genovese MC, Keystone E, Taylor PC, Zuckerman SH, Ruotolo G, Schlichting DE, Crotzer VL, Nantz E, Beattie SD, Macias WL.Arthritis Rheumatol. 2017 May;69(5):943-952. doi: 10.1002/art.40036. PMID: 28029752
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