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  1. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Autophagy Apoptosis
  2. JAK Autophagy Mitophagy Apoptosis
  3. Ruxolitinib

Ruxolitinib  (Synonyms: 蘆可替尼; INCB18424)

目錄號: HY-50856 純度: 99.90%
COA 產品使用指南

Ruxolitinib (INCB18424) 是具有口服活性的,選擇性的 JAK1/2 抑制劑, IC50 值分別為 3.3 nM 和 2.8 nM,選擇性是 JAK3 的 130 多倍。Ruxolitinib 誘導自噬 (autophagy),通過毒性線粒體自噬 (mitophagy) 殺死腫瘤細胞。

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Ruxolitinib Chemical Structure

Ruxolitinib Chemical Structure

CAS No. : 941678-49-5

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10 mM * 1 mL in DMSO ¥825
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5 mg ¥750
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10 mg ¥1100
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50 mg ¥2800
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100 mg ¥4500
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500 mg 現貨 詢價
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5 g   詢價  

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Customer Review

Other Forms of Ruxolitinib:

MCE 顧客使用本產品發(fā)表的 138 篇科研文獻

WB
Proliferation Assay
RT-PCR
IF

    Ruxolitinib purchased from MCE. Usage Cited in: Nature. 2022 Sep;609(7928):785-792.  [Abstract]

    Huh7 cells are pretreated with DMSO, 5?μM Filgotinib, 5?μM Ruxolitinib or 5?μM IFNα-IFNAR-IN-1 hydrochloride for 1?h and infected with MERS-CoV at a MOI of 1. MERS-CoV N gene copy number is quantified by RT-qPCR.

    Ruxolitinib purchased from MCE. Usage Cited in: Nat Cancer. 2022 Sep;3(9):1071-1087.  [Abstract]

    Relative cell number of LNCaP/AR cells treated with annotated treatment: 10?μM Enzalutamide (Enz), 5?μM Filgotinib (Filg), 5?μM Ruxolitinib (Ruxo), 1?μM Fludarabine (Flu), 0.2?μM Niclosamide (Nic) and DMSO for 8 days.

    Ruxolitinib purchased from MCE. Usage Cited in: Cell Mol Immunol. 2022 Oct;19(10):1130-1140.  [Abstract]

    Ruxolitinib (100?mg/kg/day; intraperitoneal injection; 8 weeks) reduces the expression of proinflammatory cytokine genes in the livers of ARE-Del+/? mice. RNA is isolated from the livers of Ruxolitinib-treated mice.

    Ruxolitinib purchased from MCE. Usage Cited in: Cell Mol Immunol. 2022 Oct;19(10):1130-1140.  [Abstract]

    The expression of phosphorylated (p-) and unphosphorylated STAT1 and STAT6 in macrophages is assessed by western blotting.

    Ruxolitinib purchased from MCE. Usage Cited in: Cell Mol Immunol. 2022 Oct;19(10):1130-1140.  [Abstract]

    Levels of IL-6, TNF, and MCP1 production in macrophages isolated from wild-type mice (females/20 weeks) following in vitro treatment with Ruxolitinib are determined utilizing CBA and flow cytometry.

    Ruxolitinib purchased from MCE. Usage Cited in: Theranostics. 2022 Oct 3;12(16):7051-7066.

    A549 cells are treated with 2.5 μM BVD and 10 μM Ruxolitinib (Rux) separately or in combination for 2 days. Immunoblotting is conducted to determine pSTAT3-Y705.

    Ruxolitinib purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Apr 12;119(15):e2122512119.  [Abstract]

    Representative DDX4 immunofluorescence following 48 h incubation of ovaries from PND2 mice cultured ex vivo with 1 μM candidate MISR2 agonists Gandotinib, SP600125, CYC-116, Ruxolitinib.

    Ruxolitinib purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Apr 12;119(15):e2122512119.  [Abstract]

    The induction of MIS target genes Id2, Id3, Smad6, and Igfbp5 was recapitulated as measured by qPCR following a 48 h incubation of ex vivo cultured ovaries from PND2 rat with 1 μM candidate MISR2 agonists Gandotinib, SP600125m, CYC-116, Ruxolitinib.

    Ruxolitinib purchased from MCE. Usage Cited in: Cell Death Dis. 2022 May 25;13(5):496.  [Abstract]

    The xenografts treated with both Trametinib and Ruxolitinib (20?mg/kg; i.p.; every 3 days) show the expression of pSTAT3 and pERK1/2 in xenograft tumors exposed to the indicated treatment. Densitometry analyses of pSTAT3 and pERK1/2 expression normalized to STAT3 and ERK1/2 expression, respectively.

    Ruxolitinib purchased from MCE. Usage Cited in: J Hematol Oncol. 2021 Jun 24;14(1):97.  [Abstract]

    Growth curves for DND-41, RPMI-8402 and LOUCY T-ALL cell lines. Growth medium is supplemented with DMSO, MRK-560 100 nM, Ruxolitinib 1 μM or both compounds.

    Ruxolitinib purchased from MCE. Usage Cited in: Cancer Commun (Lond). 2021 Dec;41(12):1354-1372.  [Abstract]

    The MAGE‐C3 overexpressing KYSE30 cells are treated with Ruxolitinib (2 μM, for 20 h.) and probed for STAT1 expression pSTAT1Tyr701. The pSTAT1Tyr701 expression levels are almost unchanged when exposure to Ruxolitinib in presence with IFN‐γ.

    Ruxolitinib purchased from MCE. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917.  [Abstract]

    The A3A mRNA level is monitored in MCF10A cells 16?h after treatment with 3p-hpRNA and JAK inhibitors (JAKi #1: 2?μM Pacritinib, JAKi #2: 2?μM Ruxolitinib).

    Ruxolitinib purchased from MCE. Usage Cited in: Cell Rep. 2020 Sep 15;32(11):108158.  [Abstract]

    Cxcl10 and Ccl5 mRNA levels are analyzed in TNF-α (100 ng/mL)-stimulated BMDMs for 6 h, which are pretreated with notopterol (10 mM) in the presence or absence of ruxolitinib (10 μM) or SD1029 (10 μM) for 3 h.

    Ruxolitinib purchased from MCE. Usage Cited in: Nat Med. 2018 Aug;24(8):1143-1150.  [Abstract]

    Immunoblot of pSTAT1, STAT1 and β-actin levels in H69AR cells±200 ng/mL IFNg 10 min pulse followed by 24 h chase in media with DMSO, Ruxolitinib (100 nM) or MRT67307 (1 μM).

    Ruxolitinib purchased from MCE. Usage Cited in: Cancer Discov. 2018 May;8(5):616-631.  [Abstract]

    Analysis of PIM1 RNA and protein expression in HOXA9 positive patient derived xenograft (PDX) samples ex vivo after 1 μM Ruxolitinib over 6 hours.

    Ruxolitinib purchased from MCE. Usage Cited in: Clin Cancer Res. 2018 Apr 15;24(8):1917-1931.  [Abstract]

    Jak2 is inhibited by lentiviral expression of Jak2 shRNA or control shRNA in CWR22Pc and CWR22Rv1 cells. Alternatively, cells are treated with Jak2 inhibitors AZD1480 (0.8 μM) and Ruxolitinib (0.4 μM) (72 h), followed by Western blot analysis of Jak2 and active Stat5a/b.

    Ruxolitinib purchased from MCE. Usage Cited in: JCI Insight. 2018 Sep 6;3(17). pii: 120750.  [Abstract]

    A431 cells are then treated in full growth media with vehicle, CSA (50 ng/mL), Ruxolitinib (20 μM), or both Ruxolitinib and CSA for 36 hours.

    Ruxolitinib purchased from MCE. Usage Cited in: J Biol Chem. 2015 Nov 27;290(48):29022-34.  [Abstract]

    106 autonomous Ba/F3 cells stably transduced with ALL-associated JAK3 mutant V674A or double mutant L857P/Y100A are treated with increasing concentration of Ruxolitinib (0–2 μM). Two hours after treatment, the cells are lysed and subjected to Western blot analysis. Phosphorylation of STAT5, JAK3, and JAK1 is detected using specific anti-pY694 STAT5, anti-pY980/81 JAK3, and anti-pY1034/35 JAK1 antibodies. Membranes are reprobed with anti-STAT5, anti-JAK3, anti-JAK1, and anti-β-actin an

    Ruxolitinib purchased from MCE. Usage Cited in: Blood. 2013 Nov 21;122(22):3628-31.  [Abstract]

    Ruxolitinib decreases spleen weight. Mice are sacrificed on day 21 or 24 to evaluate spleen size.

    查看 JAK 亞型特異性產品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產品資料

    • 參考文獻

    生物活性

    Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3[1]. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy[3].

    IC50 & Target[1]

    JAK2

    2.8 nM (IC50)

    JAK1

    3.3 nM (IC50)

    Tyk2

    19 nM (IC50)

    JAK3

    428 nM (IC50)

    體外研究
    (In Vitro)

    Ruxolitinib 有效且選擇性地抑制 JAK2V617F 介導的信號傳導和增殖,以劑量依賴性方式顯著增加細胞凋亡,并且在 64 nM 時導致 Ba/F3 細胞中具有去極化線粒體的細胞加倍。
    Ruxolitinib 顯示出顯著的抗紅細胞作用集落形成,IC50 為 67 nM,并抑制正常供體和真性紅細胞增多癥患者紅細胞祖細胞的增殖,IC50 值分別為 407 nM 和 223 nM[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    體內研究
    (In Vivo)

    Ruxolitinib (180 mg/kg,口服,每天兩次) 導致第 22 天時的存活率超過 90%,并顯著降低脾腫大和炎癥細胞因子的循環(huán)水平,并優(yōu)先消除腫瘤細胞,從而顯著延長存活時間,而無骨髓抑制或JAK2V617F 驅動的小鼠模型中的免疫抑制作用[1]
    在 Ruxolitinib 組中,41.9% 的患者達到主要終點,而安慰劑組為 0.7% 在骨髓纖維化的雙盲試驗中。Ruxolitinib 可維持脾臟體積減少,總癥狀評分改善 50% 或更多[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    306.37

    Formula

    C17H18N6

    CAS 號
    性狀

    固體

    顏色

    White to light yellow

    中文名稱

    魯索利替尼;盧索替尼;魯索替尼;蘆可替尼

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數據
    細胞實驗: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (326.40 mM; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質量 1 mg 5 mg 10 mg
    1 mM 3.2640 mL 16.3201 mL 32.6403 mL
    5 mM 0.6528 mL 3.2640 mL 6.5281 mL
    查看完整儲備液配制表

    * 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

    • 摩爾計算器

    • 稀釋計算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗:

    請根據您的 實驗動物和給藥方式 選擇適當的溶解方案。

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結果的可靠性,澄清的儲備液可以根據儲存條件,適當保存;體內實驗的工作液,建議您現用現配,當天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現沉淀、析出現象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.79 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.79 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      20% SBE-β-CD in Saline 的配制(4°C,儲存一周):2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。

    以下溶解方案,請直接配制工作液。建議現用現配,在短期內盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現沉淀、析出現象,可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑: 0.5% Methylcellulose/saline water

      Solubility: 5 mg/mL (16.32 mM); 澄清溶液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑: 5% DMAc in 0.5% Methyl cellulose/Saline water

      Solubility: 5 mg/mL (16.32 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數量

    由于實驗過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO ,均可在 MCE 網站選購。 ,Tween 80,均可在 MCE 網站選購。
    計算結果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術支持聯系。
    動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
    連續(xù)給藥周期超過半月以上,請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產品資料

    純度: 99.99%

    參考文獻
    Kinase Assay
    [1]

    Recombinant proteins are expressed using Sf21 cells and baculovirus vectors and purified with affinity chromatography. JAK kinase assays use a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction is carried out with Ruxolitinib or control, JAK enzyme, 500 nM peptide, adenosine triphosphate (ATP; 1mM), and 2% dimethyl sulfoxide (DMSO) for 1 hour. The 50% inhibitory concentration (IC50) is calculated as INCB018424 concentration required for inhibition of 50% of the fluorescent signal.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Cells are seeded at 2×103/well of white bottom 96-well plates, treated with Ruxolitinib (INCB018424) from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO2. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC50 curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice are fed standard rodent chow and provided with water ad libitum. Ba/F3-JAK2V617F cells (105?per mouse) are inoculated intravenously into 6- to 8-week-old female BALB/c mice. Survival is monitored daily, and moribund mice are humanely killed and considered deceased at time of death. Treatment with vehicle (5% dimethyl acetamide, 0.5% methocellulose) or Ruxolitinib (INCB018424) begin within 24 hours of cell inoculation, twice daily by oral gavage. Hematologic parameters are measured using a Bayer Advia120 analyzed, and statistical significance is determined using Dunnett testing.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    參考文獻

    完整儲備液配制表

    * 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.2640 mL 16.3201 mL 32.6403 mL 81.6007 mL
    5 mM 0.6528 mL 3.2640 mL 6.5281 mL 16.3201 mL
    10 mM 0.3264 mL 1.6320 mL 3.2640 mL 8.1601 mL
    15 mM 0.2176 mL 1.0880 mL 2.1760 mL 5.4400 mL
    20 mM 0.1632 mL 0.8160 mL 1.6320 mL 4.0800 mL
    25 mM 0.1306 mL 0.6528 mL 1.3056 mL 3.2640 mL
    30 mM 0.1088 mL 0.5440 mL 1.0880 mL 2.7200 mL
    40 mM 0.0816 mL 0.4080 mL 0.8160 mL 2.0400 mL
    50 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6320 mL
    60 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3600 mL
    80 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0200 mL
    100 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8160 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    產品名稱:
    Ruxolitinib
    目錄號:
    HY-50856
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