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> Ruxolitinib [941678-49-5]

Ruxolitinib [941678-49-5]

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Conditionnement : 50mg

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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 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. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.

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Ruxolitinib Chemical Structure

Ruxolitinib Chemical Structure

CAS No. : 941678-49-5

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

Based on 158 publication(s) in Google Scholar

Other Forms of Ruxolitinib:

  • Ruxolitinib (S enantiomer) In-stock
  • Ruxolitinib phosphate In-stock
  • Deuruxolitinib Obtenir un devis
  • (Rac)-Ruxolitinib-d9 Obtenir un devis
  • Ruxolitinib sulfate Obtenir un devis
  • Ruxolitinib (Standard) Obtenir un devis

    Ruxolitinib purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

    Voir tous les produits spécifiques à Isoform JAK:

    Voir toutes les isoformes
    JAK1 JAK2 JAK3 Tyk2 JAK
    Description

    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)

    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[1].

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

    Ruxolitinib Related Antibodies
    In Vivo

    Ruxolitinib (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].

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

    306.37

    Formule

    C17H18N6
    CAS No.

    941678-49-5
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    N#CC[C@H](C1CCCC1)N2N=CC(C3=C4C=CNC4=NC=N3)=C2
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvant et solubilité
    In Vitro: 

    DMSO : ≥ 100 mg/mL (326.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * 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.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% Methylcellulose/saline water

      Solubility: 5 mg/mL (16.32 mM); Clear solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  5% DMAc in 0.5% Methyl cellulose/Saline water

      Solubility: 5 mg/mL (16.32 mM); Suspended solution; Need ultrasonic

    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.
    Pureté et documentation

    Purity: 99.99%

    COA (254 KB) HNMR (213 KB) LCMS (336 KB) Elemental Analysis Report (111 KB)

    Instruction de manipulation (2659 KB)
    Références

    • [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]

    Essai de kinase
    [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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Test cellulaire
    [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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Administration animale
    [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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
    Références

    • [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]

    Complete Stock Solution Preparation Table

    * 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
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    Ruxolitinib Related Classifications

    Help & FAQs

    Keywords:

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

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