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

Ruxolitinib phosphate  (Synonyms: INCB018424 phosphate)

目錄號: HY-50858 純度: 99.97%
COA 產(chǎn)品使用指南 技術(shù)支持

Ruxolitinib phosphate (INCB018424 phosphate) 是一種有效的 JAK1/2 抑制劑， IC50 分別為3.3 nM/2.8 nM，比JAK3選擇性高130倍。

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Ruxolitinib phosphate Chemical Structure

Ruxolitinib phosphate Chemical Structure

CAS No. : 1092939-17-7

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥325
In-stock
1 mg ￥180
In-stock
5 mg ￥365
In-stock
10 mg ￥550
In-stock
25 mg ￥1100
In-stock
50 mg ￥1700
In-stock
100 mg ￥2460
In-stock
200 mg ￥3680
In-stock
500 mg ￥5900
In-stock
1 g 現(xiàn)貨 詢價
5 g   詢價  
10 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Ruxolitinib phosphate:

MCE 顧客使用本產(chǎn)品發(fā)表的 144 篇科研文獻

WB
Proliferation Assay
RT-PCR
IF

    Ruxolitinib phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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 phosphate 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(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.

    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 phosphate (INCB018424) 有效且選擇性地抑制 JAK2V617F 介導(dǎo)的信號傳導(dǎo)和增殖。Ruxolitinib phosphate 抑制 HEL 細胞的生長，EC50 值為 186 nM。Ruxolitinib phosphate 顯著增加 Ba/F3-EpoR-JAK2V617F 細胞凋亡，并抑制原代 MPN 患者樣本中的造血祖細胞增殖[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Ruxolitinib phosphate (180 mg/kg，口服) 可減輕接種 JAK2V617F 表達細胞的小鼠的腫瘤負荷，而不會引起貧血或淋巴細胞減少[1]。

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

    404.36

    Formula

    C17H21N6O4P
    CAS 號
    性狀

    固體

    顏色

    White to gray

    中文名稱

    魯索利替尼磷酸鹽
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 220 mg/mL (544.07 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    H2O 中的溶解度 : 10 mg/mL (24.73 mM; 超聲助溶)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.4730 mL 12.3652 mL 24.7304 mL
    5 mM 0.4946 mL 2.4730 mL 4.9461 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)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(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)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(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    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(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.75 mg/mL (6.80 mM); 澄清溶液

    • 方案 二

      請依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.75 mg/mL (6.80 mM); 澄清溶液

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)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(xiàn)沉淀、析出現(xiàn)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% Methyl cellulose/0.5% Tween-80 in Saline water

      Solubility: 10 mg/mL (24.73 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(shù)量

    只
    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(nèi)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(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)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）。

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    您所需的儲備液濃度超過該產(chǎn)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(shù)支持聯(lián)系。
    動物實驗體內(nèi)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(jǐn)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(chǎn)品資料

    純度: 99.97%

    參考文獻
    Cell Assay
    [1]

    Cells are 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 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) begins 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(jù)產(chǎn)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(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.4730 mL 12.3652 mL 24.7304 mL 61.8261 mL
    5 mM 0.4946 mL 2.4730 mL 4.9461 mL 12.3652 mL
    10 mM 0.2473 mL 1.2365 mL 2.4730 mL 6.1826 mL
    15 mM 0.1649 mL 0.8243 mL 1.6487 mL 4.1217 mL
    20 mM 0.1237 mL 0.6183 mL 1.2365 mL 3.0913 mL
    DMSO 25 mM 0.0989 mL 0.4946 mL 0.9892 mL 2.4730 mL
    30 mM 0.0824 mL 0.4122 mL 0.8243 mL 2.0609 mL
    40 mM 0.0618 mL 0.3091 mL 0.6183 mL 1.5457 mL
    50 mM 0.0495 mL 0.2473 mL 0.4946 mL 1.2365 mL
    60 mM 0.0412 mL 0.2061 mL 0.4122 mL 1.0304 mL
    80 mM 0.0309 mL 0.1546 mL 0.3091 mL 0.7728 mL
    100 mM 0.0247 mL 0.1237 mL 0.2473 mL 0.6183 mL

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    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(chǎn)品名稱：
    Ruxolitinib phosphate
    目錄號：
    HY-50858
    需求量：