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

Ruxolitinib sulfate  (Synonyms: INCB018424 sulfate)

目录号: HY-50859
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摩尔计算器

Ruxolitinib sulfate (INCB018424 sulfate) 是一种有效的 JAK1/2 抑制剂，IC50 值为 3.3 nM/2.8 nM，选择性是对 JAK3 的 130 倍。

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Ruxolitinib sulfate Chemical Structure

Ruxolitinib sulfate Chemical Structure

CAS No. : 1092939-16-6

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Ruxolitinib sulfate 的其他形式现货产品:

Other Forms of Ruxolitinib sulfate:

Ruxolitinib sulfate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 140 篇科研文献

WB
Proliferation Assay
RT-PCR
IF

    Ruxolitinib sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 sulfate 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 亚型特异性产品:

    查看所有亚型
    JAK1 JAK2 JAK3 Tyk2 JAK

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.

    IC50 & Target[1]

    JAK2

    2.8 nM (IC50)

    JAK1

    3.3 nM (IC50)

    Tyk2

    19 nM (IC50)

    JAK3

    428 nM (IC50)

    体外研究
    (In Vitro)

    Ruxolitinib sulfate (INCB018424 sulfate) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation, markedly increases apoptosis in a dose dependent manner, and at 64 nM results in a doubling of cells with depolarized mitochondria in Ba/F3 cells. Ruxolitinib demonstrates remarkable potency against erythroid colony formation with IC50 of 67 nM, and inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC50 values of 407 nM and 223 nM, respectively[1].

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

    Ruxolitinib sulfate 相关抗体:
    体内研究
    (In Vivo)

    Ruxolitinib (INCB018424 sulfate; 180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 and markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects in a JAK2V617F-driven mouse model[1].
    In the Ruxolitinib group, the primary end point is reached in 41.9% of patients, as compared with 0.7% in the placebo group in the double-blind trial of myelofibrosis. Ruxolitinib results in maintaining of reduction in spleen volume and improvement of 50% or more in the total symptom score[2].
    Ruxolitinib (15 mg twice daily) treatment leads a total of 28% of the patients to have at least a 35% reduction in spleen volume at week 48 in patients with myelofibrosis, as compared with 0% in the group receiving the best available therapy. The mean palpable spleen length has decreased by 56% with Ruxolitinib but has increased by 4% with the best available therapy at week 48. Patients in the ruxolitinib group has an improvement in overall quality-of-life measures and a reduction in symptoms associated with myelofibrosis[3].

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

    404.44

    Formula

    C17H20N6O4S
    CAS 号
    性状

    固体

    颜色

    Off-white to gray

    中文名称

    鲁索利替尼硫酸盐
    运输条件

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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    纯度 & 产品资料
    参考文献
    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 Ruxolitinib concentration required for inhibition of 50% of the fluorescent signal[1].

    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 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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[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 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[1].

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

    Ruxolitinib sulfate 相关分类

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    • 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.

    Keywords:

    Ruxolitinib1092939-16-6INCB018424鲁索利替尼硫酸盐INCB 018424INCB-018424JAKAutophagyJanus kinaseJAK1/2JAK3JAK2V617F-mediatedsignalingproliferationapoptosissplenomegalycirculatinginflammatorycytokinesInhibitorinhibitorinhibit

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