룩소리티닙

한글명:룩소리티닙

카스 번호941678-49-5

상품명:Ruxolitinib

CBNumberCB02499581

분자식C17H18N6

포뮬러 무게306.37

MOL 파일941678-49-5.mol

동의어(한글)

룩소리티닙

룩소리티니브

화학적 성질

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

위험 및 안전 성명

HS 번호

29335990

유해 물질 데이터

941678-49-5(Hazardous Substances Data)

NFPA 704:

	0
3		0

그림문자(GHS)

룩소리티닙 화학적 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 (IC_50'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.
Characteristics
Class: non-receptor tyrosine kinase
Treatment: MF, PV, cGVHD
Oral bioavailability >95%
Elimination half-life = 3 h
Protein binding = 97%
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.

룩소리티닙 공급 업체

룩소리티닙 관련 검색

Send Inquriy