Tofacitinib
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Tofacitinib 속성
- 밀도
- 1.3
- 저장 조건
- -20°C
- 용해도
- DMSO(최대 100mg/ml) 또는 에탄올(최대 100mg/ml)에 용해됩니다.
- 물리적 상태
- 창백한 가루.
- 산도 계수 (pKa)
- 6.04±0.60(Predicted)
- 색상
- 회백색
- 안정성
- 제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 또는 에탄올 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
- InChI
- InChI=1/C16H20N6O/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20)/t11-,13+/s3
- InChIKey
- UJLAWZDWDVHWOW-BCFRMRSDNA-N
- SMILES
- N([C@@H]1[C@@H](CCN(C(=O)CC#N)C1)C)(C1N=CN=C2NC=CC=12)C |&1:1,2,r|
- CAS 데이터베이스
- 477600-75-2
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
HS 번호 | 29335990 | ||
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유해 물질 데이터 | 477600-75-2(Hazardous Substances Data) |
그림문자(GHS): | |||||||||||||||
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신호 어: | Warning | ||||||||||||||
유해·위험 문구: |
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예방조치문구: |
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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 SolidCharacteristics
Class: non-receptor tyrosine kinaseTreatment: RA, PA, JIA, UC
Oral bioavailability = 74%
Elimination half-life = 3.2 h
Protein binding = 40%
용도
CP-690550 is a pyrrolo[2,3-d]pyrimidine derivative, as Janus kinase inhibitor for treatment of rheumatoid arthritisIndications
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.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.Clinical Use
Tofacitinib was approved for treating rheumatoid arthritis in 2012, joint pain and swelling, psoriatic arthritis in 2017, and ulcerative colitis in 2018. However, severe side effects observed during clinical studies prevented the FDA from approving more efficacious doses for the treatment of rheumatoid arthritis (RA). Tofacitinib also carries a black box warning for an increased risk of pulmonary embolism and death associated with the 10 mg BID dose.Tofacitinib 준비 용품 및 원자재
원자재
준비 용품
Tofacitinib 공급 업체
글로벌( 465)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Changsha Junyu Chemexpress.co., Ltd | +86-13723890100 |
info@csjyyy.cn | China | 134 | 58 |
Changzhou Rokechem Technology Co., Ltd. | 18758118018 |
sales001@rokechem.com | China | 255 | 58 |
Senova Technology Co. Ltd. | +86-0755-86703119 +8618503098836 |
info@senovatech.com | China | 351 | 58 |
HangZhou RunYan Pharma Technology Co.,LTD. | +8618882027439 |
sales2@runyanpharma.com | China | 304 | 58 |
Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 |
sales@hbmojin.com | China | 12446 | 58 |
Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 |
info@fdachem.com | China | 20293 | 58 |
Hebei Mojin Biotechnology Co.,Ltd | +86-15028179902 |
angelia@hbmojin.com | China | 1069 | 58 |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29798 | 60 |
Shanghai Daken Advanced Materials Co.,Ltd | +86-371-66670886 |
info@dakenam.com | China | 18629 | 58 |
Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
Tofacitinib 관련 검색:
N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Tofacitinib citrate
N-((3R,4R)-1-benzyl-4-Methylpiperidin-3-yl)-2-chloro-N-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-aMine
N-((3R,4R)-1-benzyl-4-Methylpiperidin-3-yl)-N-Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-aMine
2-Pentenoic acid, 3-amino-2-cyano-5-[(3R,4R)-4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-5-oxo-, butyl ester
7H-Pyrrolo[2,3-d]pyrimidine-7-propanenitrile, 4-[[(3R,4R)-1-(2-cyanoacetyl)-4-methyl-3-piperidinyl]methylamino]-β-oxo-
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