芦可替尼|T1829

Ruxolitinib
941678-49-5

￥233 1mg 起订

￥536 5mg 起订

￥828 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 芦可替尼

英文名称：: Ruxolitinib

CAS号：: 941678-49-5

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.93%

产品类别：: 抑制剂

货号：: T1829

Product Introduction

Bioactivity

名称	Ruxolitinib
描述	Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.
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].
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].
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].
体外活性	方法：Ba/F3-EpoR-JAK2V617F 细胞用 Ruxolitinib (0-10 μM) 处理 48 h，使用 Cell-Titer Glo 检测的细胞活力。结果：Ruxolitinib 剂量依赖性降低细胞活力，IC50 为 126 nM。[1] 方法：霍奇金淋巴瘤细胞 HDLM-2 用 Ruxolitinib (10-100 nM) 处理 24 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Ruxolitinib 显著抑制下游活性 p-STAT3 和 p-STAT5，且呈剂量依赖性，而总 STAT3 和 STAT5 水平保持不变。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Ruxolitinib (3-30 mg/kg，5% dimethyl acetamide, 0.5% methocellulose) 灌胃给药给携带肿瘤 Ba/F3-JAK2V617F 的 BALB/c 小鼠，每天两次，持续三周。结果：Ruxolitinib 显著降低了脾肿大和炎症细胞因子的循环水平，并优先消除了肿瘤细胞，从而显著延长了生存期，而没有骨髓抑制或免疫抑制作用。[1] 方法：为检测体内抗肿瘤活性，将 Ruxolitinib (150 mg/kg) 口服给药给携带人结直肠肿瘤 LS411N 的 BALB/c nude 小鼠，每两天一次，持续两周。结果：口服 Ruxolitinib 可显著抑制人结直肠肿瘤的体内生长，而不会引起肝毒性。[3]
存储条件	store at low temperature,keep away from direct sunlight,keep away from moisture \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 60 mg/mL (195.85 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5.7 mg/mL (18.61 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字	JAK \| INCB 18424 \| inhibit \| Mitochondrial Autophagy \| Mitophagy \| INCB18424 \| Janus kinase \| Autophagy \| INCB 018424 \| Ruxolitinib \| Apoptosis \| INCB-18424 \| INCB-018424 \| Inhibitor
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鲁索替尼|||芦可替尼|||INCB018424|||(R)-Ruxolitinib|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子