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Ruxolitinib

Cat. No. 7064 3 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
Pricing Availability   Qty
说明： Potent and selective JAK1/JAK2 inhibitor; orally bioavailable
别名： INCB018424
化学名： (3R)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile
纯度： ≥98% (HPLC)
说明书
引用文献 (3)
评论
通路 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Ruxolitinib

Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50 values are 3.3 and 2.8 nM, respectively). Exhibits selectivity for JAK1/2 over Tyk2 and JAK3 (~6-fold and >130-fold, respectively). Exhibits no significant inhibition against a commercial panel of 26 additional kinases. Inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. Increases survival rates in a JAK2V617F-driven myeloproliferative neoplasm mouse model. Ruxolitinib has been identified as targeting human host proteins that interact with SARS-CoV-2. The compound can also be used in protocols for the chemical reprogramming of somatic cells to iPSCs. Orally bioavailable.

Phosphate salt (Cat. No. 7048) also available.

化合物库 for Ruxolitinib

Ruxolitinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library, Tocriscreen Epigenetics Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。

技术数据 for Ruxolitinib

分子量 306.37
公式 C17H18N6
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 941678-49-5
PubChem ID 25126798
InChI Key HFNKQEVNSGCOJV-OAHLLOKOSA-N
Smiles N#CC[C@@H](N1C=C(C2=C3C=CNC3=NC=N2)C=N1)C4CCCC4

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Ruxolitinib

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 30.64 100

制备储备液 for Ruxolitinib

以下数据基于产品分子量 306.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 3.26 mL 16.32 mL 32.64 mL
5 mM 0.65 mL 3.26 mL 6.53 mL
10 mM 0.33 mL 1.63 mL 3.26 mL
50 mM 0.07 mL 0.33 mL 0.65 mL

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产品说明书 for Ruxolitinib

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for Ruxolitinib

参考文献是支持产品生物活性的出版物。

Lin et al (2009) Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction. Org.Lett. 11 1999 PMID: 19385672

Quintás-Cardama et al (2010) Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 115 3109 PMID: 20130243

Gordon et al (2020) A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 583 PMID: 32353859

Guan et al (2022) Chemical reprogramming of human somatic cells to pluripotent stem cells Nature 605 325 PMID: 35418683

If you know of a relevant reference for Ruxolitinib, please let us know.

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关键词: Ruxolitinib, Ruxolitinib supplier, Potent, selective, JAK1/JAK2, inhibitors, inhibits, JAK1, JAK2, orally, bioavailable, active, in, vivo, COVID-19, SARS-CoV-2, severe, acute, respiratory, syndrome, induced, pluripotent, stem, cells, reprogramming, iPSC, INCB018424, JAK, Kinase, Coronavirus, Stem, Cell, Reprogramming, 7064, Tocris Bioscience

3 篇 Ruxolitinib 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Ruxolitinib 的部分引用包括：

Chin Wai et al (2022) Interleukins 4 and 21 Protect Anti-IgM Induced Cell Death in Ramos B Cells: Implication for Autoimmune Diseases. Front Immunol 13 919854 PMID: 35911775

Anastasia et al (2022) RNAi-based modulation of IFN-γ signaling in skin. Mol Ther 30 2709-2721 PMID: 35477658

Jung Mo et al (2023) Endothelial cell-derived stem cell factor promotes lipid accumulation through c-Kit-mediated increase of lipogenic enzymes in brown adipocytes. Nat Commun 14 2754 PMID: 37179330

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Pathways for Ruxolitinib

JAK-STAT Signaling Pathway

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.