WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205893
CAS#: 1187594-09-7 (free base)
Description: Baricitinib, also known as INCB028050 or LY3009104, is a selective orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (5.9 nM) and JAK2 (5.7 nM). INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. INCB028050 was also effective in multiple murine models of arthritis, with no evidence of suppression of humoral immunity or adverse hematologic effects. Baricitinib was approved for the treatment of rheumatoid arthritis (RA) in the United States.
MedKoo Cat#: 205893
Name: Baricitinib
CAS#: 1187594-09-7 (free base)
Chemical Formula: C16H17N7O2S
Exact Mass: 371.11644
Molecular Weight: 371.41688
Elemental Analysis: C, 51.74; H, 4.61; N, 26.40; O, 8.62; S, 8.63
Related CAS #: 1187594-09-7 (free base) 1187595-84-1 (phosphate)
Synonym: INCB028050; INCB-028050; INCB 028050; LY3009104; LY-3009104; LY 3009104; Baricitinib; Olumiant
IUPAC/Chemical Name: 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile
InChi Key: XUZMWHLSFXCVMG-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(S(=O)(CC)=O)C1
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 371.41688 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Pharmacoeconomic Review Report: Baricitinib (Olumiant): (Eli Lilly Canada Inc.): Indication: For use in combination with methotrexate (MTX) for the treatment of adult patients with moderate to severe rheumatoid arthritis who have responded inadequately to one or more disease-modifying antirheumatic drugs (DMARDs). Baricitinib may also be used as monotherapy in cases of intolerance to MTX [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Sep. Available from http://www.ncbi.nlm.nih.gov/books/NBK549720/ PubMed PMID: 31742965.
2: Clinical Review Report: Baricitinib (Olumiant): (Eli Lilly Canada Inc.): Indication: For use in combination with methotrexate (MTX) for the treatment of adult patients with moderate to severe rheumatoid arthritis who have responded inadequately to one or more disease-modifying antirheumatic drugs (DMARDs). Baricitinib may also be used as monotherapy in cases of intolerance to MTX [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Sep. Available from http://www.ncbi.nlm.nih.gov/books/NBK549711/ PubMed PMID: 31742964.
3: CADTH Canadian Drug Expert Committee Recommendation: Baricitinib (Olumiant — Eli Lilly Canada Inc.): Indication: For use in combination with methotrexate (MTX) for the treatment of adult patients with moderate to severe rheumatoid arthritis (RA) who have responded inadequately to one or more disease-modifying anti-rheumatic drugs (DMARDs). Baricitinib may also be used as monotherapy in cases of intolerance to MTX [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2019 Aug. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK549614/ PubMed PMID: 31738494.
4: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548012/ PubMed PMID: 31643344.
5: Krutzke S, Rietschel C, Horneff G. Baricitinib in therapy of COPA syndrome in a 15-year-old girl. Eur J Rheumatol. 2019 Aug 20:1-4. doi: 10.5152/eurjrheum.2019.18177. [Epub ahead of print] Review. PubMed PMID: 31449490.
6: Kawalec P, Śladowska K, Malinowska-Lipień I, Brzostek T, Kózka M. New alternative in the treatment of rheumatoid arthritis: clinical utility of baricitinib. Ther Clin Risk Manag. 2019 Feb 13;15:275-284. doi: 10.2147/TCRM.S192440. eCollection 2019. Review. PubMed PMID: 30858707; PubMed Central PMCID: PMC6385775.
7: Choy EHS, Miceli-Richard C, González-Gay MA, Sinigaglia L, Schlichting DE, Meszaros G, de la Torre I, Schulze-Koops H. The effect of JAK1/JAK2 inhibition in rheumatoid arthritis: efficacy and safety of baricitinib. Clin Exp Rheumatol. 2019 Jul-Aug;37(4):694-704. Epub 2019 Feb 11. Review. PubMed PMID: 30767864.
8: Baricitinib for rheumatoid arthritis. Aust Prescr. 2019 Feb;42(1):34-35. doi: 10.18773/austprescr.2018.070. Epub 2018 Dec 13. Review. PubMed PMID: 30765909; PubMed Central PMCID: PMC6370601.
9: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK525499/ PubMed PMID: 30222291.
10: Al-Salama ZT, Scott LJ. Baricitinib: A Review in Rheumatoid Arthritis. Drugs. 2018 May;78(7):761-772. doi: 10.1007/s40265-018-0908-4. Review. PubMed PMID: 29687421.
11: Ren S, Bermejo I, Simpson E, Wong R, Scott DL, Young A, Stevenson M. Baricitinib for Previously Treated Moderate or Severe Rheumatoid Arthritis: An Evidence Review Group Perspective of a NICE Single Technology Appraisal. Pharmacoeconomics. 2018 Jul;36(7):769-778. doi: 10.1007/s40273-018-0616-7. Review. PubMed PMID: 29502174; PubMed Central PMCID: PMC5999127.
12: Taylor PC, Kremer JM, Emery P, Zuckerman SH, Ruotolo G, Zhong J, Chen L, Witt S, Saifan C, Kurzawa M, Otvos JD, Connelly MA, Macias WL, Schlichting DE, Rooney TP, de Bono S, McInnes IB. Lipid profile and effect of statin treatment in pooled phase II and phase III baricitinib studies. Ann Rheum Dis. 2018 Jul;77(7):988-995. doi: 10.1136/annrheumdis-2017-212461. Epub 2018 Feb 20. Review. PubMed PMID: 29463520; PubMed Central PMCID: PMC6029633.
13: Richez C, Truchetet ME, Kostine M, Schaeverbeke T, Bannwarth B. Efficacy of baricitinib in the treatment of rheumatoid arthritis. Expert Opin Pharmacother. 2017 Sep;18(13):1399-1407. doi: 10.1080/14656566.2017.1359256. Epub 2017 Jul 27. Review. PubMed PMID: 28737053.
14: Keyßer G. [Success for a new generation of disease-modifying antirheumatic drugs : The Janus kinase inhibitor baricitinib in rheumatoid arthritis]. Z Rheumatol. 2017 Jun;76(5):461-462. doi: 10.1007/s00393-017-0307-3. Review. German. PubMed PMID: 28447156.
15: Markham A. Baricitinib: First Global Approval. Drugs. 2017 Apr;77(6):697-704. doi: 10.1007/s40265-017-0723-3. Review. PubMed PMID: 28290136.
16: Kuriya B, Cohen MD, Keystone E. Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential. Ther Adv Musculoskelet Dis. 2017 Feb;9(2):37-44. doi: 10.1177/1759720X16687481. Epub 2017 Jan 23. Review. PubMed PMID: 28255337; PubMed Central PMCID: PMC5315227.
17: Gras J. Baricitinib: JAK inhibition for rheumatoid arthritis. Drugs Today (Barc). 2016 Oct;52(10):543-550. Review. PubMed PMID: 27910962.
18: Kubo S, Nakayamada S, Tanaka Y. Baricitinib for the treatment of rheumatoid arthritis. Expert Rev Clin Immunol. 2016 Sep;12(9):911-9. doi: 10.1080/1744666X.2016.1214576. Epub 2016 Aug 5. Review. PubMed PMID: 27427830.
Related CAS#
1187594-09-7 (Baricitinib free base)
1187595-84-1 (Baricitinib phosphate)
