ChemicalBook > Product Catalog > Biochemical Engineering > Inhibitors > Protein tyrosine kinase /JAK / STAT > JAK inhibitors > Tofacitinib
Tofacitinib Chemical Properties
- Density 1.3
- form Pale powder.
- CAS DataBase Reference477600-75-2
- HS Code 29335990
Tofacitinib Usage And Synthesis
- DescriptionIn November 2012, the US FDA approved tofacitinib (also referred to as CP-690550) for the treatment of adult patients with moderate to severely active rheumatoid arthritis (RA) who have had an inadequate response or intolerance to methotrexate. Tofacitinib is the first small molecule kinase inhibitor approved for the treatment of RA. Tofacitinib is an inhibitor of the four subtypes of Janus kinase (JAK): JAK1, JAK2, JAK3, and Tyk2. The JAKs are intracellular, nonreceptor tyrosine kinases that play important roles in the signal transduction pathway of many cytokines (e.g., interleukins 2, 4, 7, 9, 15, and 21) and are involved in the propagation of inflammation in RA. Tofacitinib acts by inhibiting the phosphorylation and activation of signal transducers and activators of transcription (STATs), thereby suppressing the production of inflammatory mediators in joint tissue. At the enzyme level, tofacitinib inhibits JAKs 1, 2, 3, and Tyk2 with IC50s of 3.2, 4.1, 1.6, and 34 nM, respectively. At the cellular level, tofacitinib inhibits the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC50s of 406, 56, and 1377 nM, respectively.
- Chemical PropertiesLight Pink to Pale Orange Solid
- OriginatorPfizer (United States)
- UsesCP-690550 is a pyrrolo[2,3-d]pyrimidine derivative, as Janus kinase inhibitor for treatment of rheumatoid arthritis
- DefinitionChEBI: A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely ctive rheumatoid arthritis.
- IndicationsThe JAK family includes four isoforms, JAK1, JAK2, JAK3, and tyrosine kinase (TYK2). Ruxolitinib (Jakafi(R), Incyte Corp.) was the first approved JAK inhibitor, which inhibits both JAK1 and JAK2, used for the treatment of different types of myelofibrosis. Tofacitinib (Xeljanz(R), Pfizer) was approved by FDA as a JAK3-selective inhibitor for the treatment of rheumatoid arthritis and is one of the only two FDA-approved kinase inhibitors for non-oncological indications.
- brand nameXeljanz
- Nilotinib hydrochloride anhydrous GZD 824 Axitinib Cabozantinib Palbociclib Trametinib Dacomitinib (PF299804) Lenvatinib Tofacitinib citrate AZD1480 Pictilisib Sunitinib Malate Ibrutinib N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide Ruxolitinib Tofacitinib DEAZAPURINE N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
- Company Name:Shanghai Boc Chemical Co.,Ltd Gold
- Tel:18721111801 021-34975603-808
- Company Name:Shanghai Coupling Pharmaceutical R&D Co.,Ltd.（Former company is Brother Chemistry） Gold
- Company Name:Zhuhai Yourun Co., Ltd. Gold
- Company Name:Shanghai BLT Biological Pharmaceutical Co., Ltd. Gold
- Tel:021-20786057 18918495077
- Company Name:Suzhou Shang Enda Biotechnology Ltd. Gold
- Tel:13382105697 0512-66242155-
- Oct 11，2019
- Oct 11，2019