Reagents and instruments for immunology, cell biology and molecular biology.
 
> Ruxolitinib [941678-49-5]

Ruxolitinib [941678-49-5]

Print Print
Please log in

Cat# HY-50856-50mg

Size : 50mg

Brand : MedChemExpress

Contact local distributor :


Phone : +1 850 650 7790

Ruxolitinib (INCB18424) est un inhibiteur de JAK1/2 qui est puissant et sélectif avec des IC50s de 3,3 nM et 2,8 nM dans les tests sans cellules, et a une sélectivité de 130 fois pour JAK1/2 sur JAK3. Ruxolitinib induit l'autophagie et tue les cellules tumorales par une mitophagie toxique.

Ruxolitinib (INCB18424) ist ein potenter und selektiver JAK1/2-Inhibitor mit IC50s von 3,3 nM und 2,8 nM in zellfreien Assays und hat eine 130-fache Selektivität für JAK1/2 gegenüber JAK3. Ruxolitinib induziert autophagy und tötet Tumorzellen durch toxische mitophagy ab.

Ruxolitinib (INCB18424) is a potent 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. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.

For research use only. We do not sell to patients.

Ruxolitinib Chemical Structure

CAS No. : 941678-49-5

*

This product is a controlled substance and not for sale in your territory.

Ruxolitinib Related Antibodies

Proliferation Assay
IF
WB
RT-PCR
    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.
    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.
    The expression of phosphorylated (p-) and unphosphorylated STAT1 and STAT6 in macrophages is assessed by western blotting.
    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.
    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.
    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.
    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.
    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.
    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.
    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.
    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).
    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.
    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.
    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).
    Analysis of PIM1 RNA and protein expression in HOXA9 positive patient derived xenograft (PDX) samples ex vivo after 1 μM Ruxolitinib over 6 hours.
    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.
    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.
    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 decreases spleen weight. Mice are sacrificed on day 21 or 24 to evaluate spleen size.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Ruxolitinib (INCB18424) is a potent 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. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.

    JAK2

    2.8 nM (IC50)

    JAK1

    3.3 nM (IC50)

    Tyk2

    19 nM (IC50)

    JAK3

    428 nM (IC50)

    In Vitro

    Ruxolitinib 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.

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

    Ruxolitinib Related Antibodies

      In Vivo Dissolution Calculator
      Please enter the basic information of animal experiments:

      Dosage

      mg/kg

      Animal weight
      (per animal)

      g

      Dosing volume
      (per animal)

      μL

      Number of animals

      Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
      Please enter your animal formula composition:
      %
      DMSO +
      % 
      +
      %
      Tween-80 +
      %
      Saline
      Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
      The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
      Calculation results:
      Working solution concentration: mg/mL
      Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
      The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
      Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
       If the continuous dosing period exceeds half a month, please choose this protocol carefully.
      Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

    • [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.  [Content Brief]

      [2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807.  [Content Brief]

      [3]. Tavallai M, et al. Rationally Repurposing Ruxolitinib (Jakafi (®)) as a Solid Tumor Therapeutic.Front Oncol. 2016 Jun 13;6:142.  [Content Brief]

    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.

    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.

    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.

    • [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.  [Content Brief]

      [2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807.  [Content Brief]

      [3]. Tavallai M, et al. Rationally Repurposing Ruxolitinib (Jakafi (®)) as a Solid Tumor Therapeutic.Front Oncol. 2016 Jun 13;6:142.  [Content Brief]

    • [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]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807.

      [3]. Tavallai M, et al. Rationally Repurposing Ruxolitinib (Jakafi (®)) as a Solid Tumor Therapeutic.Front Oncol. 2016 Jun 13;6:142.

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Autophagy Apoptosis
    • JAK Autophagy Mitophagy Apoptosis
    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.

    Keywords:

    Ruxolitinib941678-49-5INCB18424INCB 18424INCB-18424JAKAutophagyMitophagyApoptosisJanus kinaseMitochondrial AutophagyInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Ruxolitinib
    Cat. No.:
    HY-50856
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.

    You might also be interested by the following products:



    Cat#
    Description
    Cond.
    Price Bef. VAT