룩소리티닙

룩소리티닙
룩소리티닙 구조식 이미지
카스 번호:
941678-49-5
한글명:
룩소리티닙
동의어(한글):
룩소리티닙
상품명:
Ruxolitinib
동의어(영문):
Jakafi;Roxolitinib;(R)-3-(4-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile;(R)-Ruxolitinib;CS-163;Pridazole;Russolinib;Benzalolin;Ruxolitinib;Ruxolitinib, >=98%
CBNumber:
CB02499581
분자식:
C17H18N6
포뮬러 무게:
306.37
MOL 파일:
941678-49-5.mol

룩소리티닙 속성

녹는점
84-89°C
밀도
1.40
저장 조건
-20°
용해도
DMSO(최대 28mg/ml) 또는 에탄올(가온 시 최대 15mg/ml)에 용해됩니다.
물리적 상태
백색 분말.
산도 계수 (pKa)
11.63±0.50(Predicted)
색상
하얀색
안정성
제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 또는 에탄올 용액은 -20°에서 최대 3개월 동안 보관할 수 있습니다.
InChI
InChI=1/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/s3
InChIKey
HFNKQEVNSGCOJV-UJHUVDBMNA-N
SMILES
[C@@H](C1CCCC1)(N1N=CC(C2N=CN=C3NC=CC=23)=C1)CC#N |&1:0,r|
CAS 데이터베이스
941678-49-5
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
HS 번호 29335990
유해 물질 데이터 941678-49-5(Hazardous Substances Data)
그림문자(GHS): GHS hazard pictogramsGHS hazard pictograms
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 GHS hazard pictograms P264, P270, P301+P312, P330, P501
예방조치문구:
P202 모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
NFPA 704
0
3 0

룩소리티닙 C화학적 특성, 용도, 생산

개요

In November 2011, the U.S. FDA approved ruxolitinib (INCB018424) for the treatment of patients with intermediate or high-risk myelofibrosis. Ruxolitinib is an ATP-competitive inhibitor of JAK1 and JAK2 (IC50's of 3.3±1.2 nM and 2.8±1.2 nM, respectively) and inhibition occurs regardless of the JAK2V617F mutational status. Ruxolitinib is a moderately potent inhibitor of the related JAK, TYK2 (IC50=19±3.2 nM) but is selective versus JAK3 (IC50=428±243 nM). It was also selective versus a panel of 26 other kinases at concentrations approximately 100-fold the IC50 of JAK1 and JAK2. Inhibition of JAK1 and JAK2 downregulates the JAK-signal transducer and activator of transcription (STAT) pathway, inhibiting myeloproliferation, inducing apoptosis, and reducing numerous cytokine plasma levels.

용도

Ruxolitinib is a selective Janus tyrosine kinase (JAK1 and JAK2) inhibitor used in the treatment of myeloproliferative neoplasms and psoriasis.

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.

정의

ChEBI: A pyrazole substituted at position 1 by a 2-cyano-1-cyclopentylethyl group and at position 3 by a pyrrolo[2,3-d]pyrimidin-4-yl group. Used as the phosphate salt for the treatment of patients with intermediate or high-risk myelofibrosis, includ ng primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis.

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