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Ruxolitinib

产品编号 T1829 CAS 941678-49-5

别名: 芦可替尼, (R)-Ruxolitinib, INCB018424, 鲁索替尼

Ruxolitinib 是一种选择性的 JAK1/2抑制剂，IC50值分别为 3.3 nM 和 2.8 nM。它通过毒性线粒体自噬杀死肿瘤细胞，可诱导自噬。

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Ruxolitinib, CAS 941678-49-5

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其他形式的 Ruxolitinib:

选择批次

纯度: 100%

纯度: 99.93%

纯度: 99.83%

纯度: 99.42%

纯度: 99.4%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50: 3.3/2.8 nM) and is relatively less selective for JAK3 (IC50: 322 nM).
靶点活性	JAK2:2.8 nM (cell free), JAK1:3.3 nM (cell free), Tyk2:19 nM (cell free)
体外活性	Ruxolitinib (INCB018424) inhibited interleukin-6 signaling (IC50: 281 nM), and proliferation of JAK2V617F(+) Ba/F3 cells (IC50: 127 nM). In primary cultures, INCB018424 preferentially suppressed erythroid progenitor colony formation from JAK2V617F(+) polycythemia vera patients (IC50: 67 nM) versus healthy donors (IC50 > 400nM) [1].
体内活性	In a mouse model of JAK2V617F(+) MPN, oral INCB018424 markedly reduced splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects [1]. A total of 28% of the patients in the ruxolitinib group had at least a 35% reduction in spleen volume at week 48, as compared with 0% in the group receiving the best available therapy; the corresponding percentages at week 24 were 32% and 0%. At 48 weeks, the mean palpable spleen length had decreased by 56% with ruxolitinib but had increased by 4% with the best available therapy [2]. The primary endpoint was reached in 41.9% of patients in the ruxolitinib group as compared with 0.7% in the placebo group. A reduction in spleen volume was maintained in patients who received ruxolitinib; 67.0% of the patients with a response had the response for 48 weeks or more. There was an improvement of 50% or more in the total symptom score at 24 weeks in 45.9% of patients who received ruxolitinib as compared with 5.3% of patients who received placebo [3].
激酶实验	The kinase domains of human JAK1 (837-1142), JAK2 (828-1132), JAK3 (781-1124), and Tyk2 (873-1187) were cloned by PCR with N-terminal epitope tags. Recombinant proteins were expressed using Sf21 cells and baculovirus vectors and purified with affinity chromatography. JAK kinase assays used a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction was carried out with test compound or control, JAK enzyme, 500nM peptide, adenosine triphosphate (ATP; 1mM), and 2.0% dimethyl sulfoxide (DMSO) for 1 hour. The 50% inhibitory concentration (IC50) was calculated as the compound concentration required for inhibition of 50% of the fluorescent signal. Biochemical assays for CHK2 and c-MET enzymes were performed using standard conditions (Michaelis constant [Km] ATP) with recombinantly expressed catalytic domains from each protein and synthetic peptide substrates. An additional panel of kinase assays (Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, c-Met, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JAK2, JAK3, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70) was performed using standard conditions using 200nM INCB018424. Significant inhibition was defined as more than or equal to 30% (average of duplicate assays) compared with control values [1].
细胞实验	Cells were seeded at 2000/well of white bottom 96-well plates, treated with compounds from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO2. Viability was measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values were transformed to percent inhibition relative to vehicle control, and IC50 curves were fitted according to nonlinear regression analysis of the data using PRISM GraphPad [1].
动物实验	All of the procedures were conducted in accordance with the US Public Health Service Policy on Humane Care and Use of Laboratory Animals. Mice were fed standard rodent chow and provided with water ad libitum. Ba/F3-JAK2V617F cells (10^5 per mouse) were inoculated intravenously into 6- to 8-week-old female BALB/c mice. Survival was monitored daily, and moribund mice were humanely killed and considered deceased at time of death. Treatment with vehicle (5% dimethylacetamide, 0.5% methocellulose) or INCB018424 began within 24 hours of cell inoculation, twice daily by oral gavage. Hematologic parameters were measured using a Bayer Advia120 analyzed, and statistical significance was determined using Dunnett testing [1].

别名	芦可替尼, (R)-Ruxolitinib, INCB018424, 鲁索替尼
化合物与蛋白结合的复合物	C-Src in complex with Ruxolitinib
分子量	306.37
分子式	C17H18N6
CAS No.	941678-49-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

H2O: <1 mg/mL

DMSO: 57 mg/mL (186 mM)

Ethanol: <1 mg/mL

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117. 2. Harrison C, et al. JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis. N Engl J Med. 2012 Mar 1;366(9):787-98. 3. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807. 4. Datta J, Lamichhane P, Dai X, et al. Combined MEK and STAT3 inhibition reprograms the tumor microenvironment to overcome immunotherapy resistance in pancreatic cancer[J]. bioRxiv. 2021 5. Ryan M M, Patel M, Hogan K, et al. Ruxolitinib inhibits IFNγ licensing of human bone marrow derived Mesenchymal Stromal Cells[J]. Transplantation and Cellular Therapy. 2021, 27(5): 389. e1-389. e10. 6. Chen X, Gao C, Cheng Z, et al. Ruxolitinib exerts neuroprotection via repressing ferroptosis in a mouse model of traumatic brain injury[J]. Experimental Neurology. 2021: 113762. 7. Zhang C, Yan Y, He H, et al. IFN-stimulated P2Y13 protects mice from viral infection by suppressing the cAMP/EPAC1 signaling pathway[J]. Journal of molecular cell biology. 2018 Aug 22. 8. Espinet E, Gu Z, Imbusch C D, et al. Cancer Discovery. 2021, 11(3): 638-659.

文献引用

1. Datta J, Dai X, Bianchi A, et al. Combined MEK and STAT3 inhibition uncovers stromal plasticity by enriching for cancer-associated fibroblasts with mesenchymal stem cell-like features to overcome immunotherapy resistance in pancreatic cancer. Gastroenterology. 2022 2. Datta J, Lamichhane P, Dai X, et al. Combined MEK and STAT3 inhibition reprograms the tumor microenvironment to overcome immunotherapy resistance in pancreatic cancer. Cancer Research. 2022, 82(12_Supplement): 4187-4187. 3. Si H, Wang J, He R, et al. Identification of U937JAK3-M511I Acute Myeloid Leukemia Cells as a Sensitive Model to JAK3 Inhibitor. Frontiers in oncology. 2021, 11: 807200-807200. 4. Alfi O, Hamdan M, Wald O, et al. SARS-CoV-2 Omicron Induces Enhanced Mucosal Interferon Response Compared to other Variants of Concern, Associated with Restricted Replication in Human Lung Tissues. Viruses. 2022, 14(7): 1583. 5. Zhang C, Yan Y, He H, et al. IFN-stimulated P2Y13 protects mice from viral infection by suppressing the cAMP/EPAC1 signaling pathway. Journal of Molecular Cell Biology. 2018 Aug 22 6. Chen X, Gao C, Cheng Z, et al. Ruxolitinib exerts neuroprotection via repressing ferroptosis in a mouse model of traumatic brain injury. Experimental Neurology. 2021: 113762. 7. Wang H, Jia X, Zhang M, et al.Isoliquiritigenin inhibits virus replication and virus-mediated inflammation via NRF2 signaling.Phytomedicine.2023: 154786.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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溶液体积

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配液浓度

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ruxolitinib 941678-49-5 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Mitophagy Tyrosine Kinases JAK INCB 18424 芦可替尼 (R)-Ruxolitinib inhibit Mitochondrial Autophagy INCB18424 Janus kinase INCB018424 INCB-18424 Inhibitor 鲁索替尼 inhibitor

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Ruxolitinib

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溶解度

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剂量换算

体内实验配液计算器

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