1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  2. JAK Apoptosis
  3. XL019

XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.

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

XL019 Chemical Structure

XL019 Chemical Structure

CAS No. : 945755-56-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 94 In-stock
Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Solid
5 mg USD 85 In-stock
10 mg USD 150 In-stock
50 mg USD 495 In-stock
100 mg USD 825 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    XL019 purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2022 Nov 11;248:114268.  [Abstract]

    XL019 (10 μM) effectively attenuates the SCCP-mediated upregulation of iNOS and GFAP in C6 cells by Inhibiting JAK2.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2[1][2].

    IC50 & Target[1]

    JAK2

    2.2 nM (IC50)

    JAK3

    214.2 nM (IC50)

    In Vivo

    XL019 (100-300 mg/kg; p.o.; twice daily for 14 days) inhibits HEL.92.1.7 xenograft tumor growth[1].
    XL019 (10 mg/kg) treatment shows that the Cmax, t1/2 and Vd were 5.24 μM, 1.94 hours, 5.319 L/kg, respectively[1].

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

    Animal Model: Female nude mice (HEL.92.1.7 xenograft tumors)[1]
    Dosage: 100, 200, 300 mg/kg
    Administration: p.o.; twice daily for 14 days
    Result: Inhibition of HEL.92.1.7 xenograft tumor growth.
    Animal Model: Mouse[1]
    Dosage: 10 mg/kg
    Administration: p.o.(Pharmacokinetic Analysis)
    Result: The Cmax, t1/2 and Vd were 5.24 μM, 1.94 hours, and 5.319 L/kg, respectively.
    Clinical Trial
    Molecular Weight

    444.53

    Formula

    C25H28N6O2

    CAS No.
    Appearance

    Solid

    Color

    Green to yellow

    SMILES

    O=C([C@H]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (56.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2496 mL 11.2478 mL 22.4957 mL
    5 mM 0.4499 mL 2.2496 mL 4.4991 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    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: ≥ 2.5 mg/mL (5.62 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    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.
    Purity & Documentation

    Purity: ≥98.0%

    References

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2496 mL 11.2478 mL 22.4957 mL 56.2392 mL
    5 mM 0.4499 mL 2.2496 mL 4.4991 mL 11.2478 mL
    10 mM 0.2250 mL 1.1248 mL 2.2496 mL 5.6239 mL
    15 mM 0.1500 mL 0.7499 mL 1.4997 mL 3.7493 mL
    20 mM 0.1125 mL 0.5624 mL 1.1248 mL 2.8120 mL
    25 mM 0.0900 mL 0.4499 mL 0.8998 mL 2.2496 mL
    30 mM 0.0750 mL 0.3749 mL 0.7499 mL 1.8746 mL
    40 mM 0.0562 mL 0.2812 mL 0.5624 mL 1.4060 mL
    50 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
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    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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    Product Name:
    XL019
    Cat. No.:
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