1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Autophagy
  2. JAK
    Autophagy
    Mitophagy

Ruxolitinib phosphate (Synonyms: INCB018424 phosphate)

Cat. No.: HY-50858 Purity: 99.89%
Handling Instructions

Ruxolitinib (phosphate) is the first potent JAK1/2 inhibitor with IC50 values of 3.3 nM/2.8 nM, more than 130-fold selectivity for JAK1/2 versus JAK3.

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

Ruxolitinib phosphate Chemical Structure

Ruxolitinib phosphate Chemical Structure

CAS No. : 1092939-17-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 72 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 132 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 180 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg USD 288 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
500 mg USD 528 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
1 g USD 768 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 g   Get quote  
10 g   Get quote  

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Other Forms of Ruxolitinib phosphate:

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

    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: Blood. 2013 Nov 21;122(22):3628-31.

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

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

    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: Clin Cancer Res. 2018 Apr 15;24(8):1917-1931.

    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: Nat Med. 2018 Aug;24(8):1143-1150.

    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).

    View All JAK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Ruxolitinib (phosphate) is the first potent JAK1/2 inhibitor with IC50 values of 3.3 nM/2.8 nM, more than 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)

    In Vitro

    Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC50 of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system, and inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples[1].

    In Vivo

    Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells without causing anemia or lymphopenia[1].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 31 mg/mL (76.66 mM)

    H2O : 5.4 mg/mL (13.35 mM; Need ultrasonic and warming)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2473 mL 1.2365 mL 2.4730 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Ruxolitinib phosphate is dissolved in 5% dimethyl acetamide, 0.5% methylcellulose[2].

    References
    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.

    References
    Molecular Weight

    404.36

    Formula

    C₁₇H₂₁N₆O₄P

    CAS No.

    1092939-17-7

    SMILES

    N#CC[[email protected]](C1CCCC1)N2N=CC(C3=C4C=CNC4=NC=N3)=C2.O=P(O)(O)O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.89%

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    Product Name:
    Ruxolitinib phosphate
    Cat. No.:
    HY-50858
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    Ruxolitinib phosphate

    Cat. No.: HY-50858