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鲁索替尼

规格或纯度: 98%
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货号 (SKU) 包装规格 是否现货 价格 数量
S129613-1mg
 1mg 现货 Stock Image
S129613-5mg
 5mg 现货 Stock Image
S129613-10mg
 10mg 现货 Stock Image
S129613-25mg
 25mg 现货 Stock Image
S129613-50mg
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S129613-100mg
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Janus kinase 1 Inhibitor Janus kinase 2 Inhibitor Janus kinase 3 Inhibitor tyrosine kinase 2 Inhibitor
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基本描述

规格或纯度 98%
英文名称 S-Ruxolitinib (INCB018424)
别名 1H-Pyrazole-1-propanenitrile, β-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (βS)-
英文别名 1H-Pyrazole-1-propanenitrile;β-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-;(βS)-;(3S)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

产品介绍：
S-Ruxolitinib (INCB018424)是第一个应用到临床的，有效的，选择性JAK1/2抑制剂，IC50为3.3 nM/2.8 nM，作用于JAK1/2比作用于JAK3选择性高130倍以上。 Phase 3。

名称和标识符

IUPAC Name (3S)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile
INCHI InChI=1S/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-/m0/s1
InChi Key HFNKQEVNSGCOJV-HNNXBMFYSA-N
Canonical SMILES C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
PubChem CID 50878566
分子量 306.37

化学和物理性质

溶解性 DMSO 61 mg/mL Water 5 mg/mL Ethanol 61 mg/mL
熔点 138-143oC

关联配体

Ligand ID 5688
名称 ruxolitinib
别名 INCB 18424
类别 Synthetic organic
学名 (3R)-3-cyclopentyl-3-(4-{7H-pyrrolo[2,3-d]pyrimidin-4-yl}-1H-pyrazol-1-yl)propanenitrile
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Ruxolitinib is a Type-1 kinase inhibitor and was first approved by the US FDA in 2011. Ruxolitinib has high potency against Janus kinases 1 and 2 (JAK1, JAK2), as well as against the related family member, tyrosine kinase 2 (TYK2) . Inhibitory activity against JAK3 is only slightly reduced compared to the other three family kinases.
Marketed formulations may contain ruxolitinib phosphate (PubChem CID 25127112).
临床描述 The purpose of this study will be to examine the efficacy, safety, and tolerability of ruxolitinib cream in subjects with vitiligo.
The purpose of this study is to evaluate the efficacy and safety of ruxolitinib cream in adolescent and adult participants with non-segmental vitiligo for whom total body involved vitiligo area (facial and nonfacial) does not exceed 10% body surface area (BSA).
The purpose of this study is to evaluate the efficacy and safety of ruxolitinib cream in adolescent and adult participants with non-segmental vitiligo for whom total body involved vitiligo area (facial and nonfacial) does not exceed 10% body surface area (BSA).
来源公司 Incyte Corporation
Incyte Corporation
Incyte Corporation

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参考文献

1. Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA et al..  (2012)  Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors..  J Med Chem,  55  (22):  (10090-107).  [PMID:23061660]
2. Mackay-Wiggan J, Jabbari A, Nguyen N, Cerise JE, Clark C, Ulerio G, Furniss M, Vaughan R, Christiano AM, Clynes R.  (2016)  Oral ruxolitinib induces hair regrowth in patients with moderate-to-severe alopecia areata..  JCI Insight,  1  (15):  (e89790).  [PMID:27699253]
3. Xing L, Dai Z, Jabbari A, Cerise JE, Higgins CA, Gong W, de Jong A, Harel S, DeStefano GM, Rothman L et al..  (2014)  Alopecia areata is driven by cytotoxic T lymphocytes and is reversed by JAK inhibition..  Nat Med,  20  (9):  (1043-9).  [PMID:25129481]
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