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Tofacitinib

Tofacitinib 구조식 이미지
카스 번호:
477600-75-2
상품명:
Tofacitinib
동의어(영문):
CP 690550;Tofacitinib;Tasocitinib;477600-75-2;Tofaimpurity;Tofacitinib base;Tropsch iMatinib;Tofacitinib, >=98%;CP-690550 Tofacitinib;Tofacitinib,CP-690550
CBNumber:
CB0970901
분자식:
C16H20N6O
포뮬러 무게:
312.3696
MOL 파일:
477600-75-2.mol

Tofacitinib 속성

밀도
1.3
물리적 상태
Pale powder.
CAS 데이터베이스
477600-75-2

안전

HS 번호 29335990

Tofacitinib C화학적 특성, 용도, 생산

개요

In 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.

화학적 성질

Light Pink to Pale Orange Solid

Originator

Pfizer (United States)

용도

CP-690550 is a pyrrolo[2,3-d]pyrimidine derivative, as Janus kinase inhibitor for treatment of rheumatoid arthritis

정의

ChEBI: 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.

Indications

The 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.

상표명

Xeljanz

Tofacitinib 준비 용품 및 원자재

원자재

준비 용품


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