2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling Epigenetics
  3. Syk JAK
  4. Cerdulatinib hydrochloride

Cerdulatinib hydrochloride  (Synonyms: PRT062070 hydrochloride; PRT2070 hydrochloride)

Cat. No.: HY-15999A Purity: 99.89%
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Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.

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

Cerdulatinib hydrochloride Chemical Structure

Cerdulatinib hydrochloride Chemical Structure

CAS No. : 1369761-01-2

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10 mM * 1 mL in DMSO
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Based on 7 publication(s) in Google Scholar

Other Forms of Cerdulatinib hydrochloride:

Cerdulatinib hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Cerdulatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368.  [Abstract]

    Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.

    Cerdulatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368.  [Abstract]

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    View All JAK Isoform Specific Products:

    View All Isoforms
    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies[1][2].

    IC50 & Target[1]

    Tyk2

    0.5 nM (IC50)

    JAK1

    12 nM (IC50)

    JAK2

    6 nM (IC50)

    JAK3

    8 nM (IC50)

    SYK

    32 nM (IC50)

    MST1

    4 nM (IC50)

    ARK5

    4 nM (IC50)

    MLK1

    5 nM (IC50)

    FMS

    5 nM (IC50)

    AMPK

    6 nM (IC50)

    TBK1

    10 nM (IC50)

    MARK1

    10 nM (IC50)

    PAR1B-a

    13 nM (IC50)

    TSSK

    14 nM (IC50)

    MST2

    15 nM (IC50)

    GCK

    18 nM (IC50)

    JNK3

    18 nM (IC50)

    Rsk2

    20 nM (IC50)

    Rsk4

    28 nM (IC50)

    CHK1

    42 nM (IC50)

    Flt4

    51 nM (IC50)

    Flt3

    90 nM (IC50)

    Ret

    105 nM (IC50)

    Itk

    194 nM (IC50)

    In Vitro

    Cerdulatinib (0.03-4 μM) inhibits ERK Y204 phosphorylation with an IC50 of 0.5 μM and reduces the ability to upregulate cellsurface expression of the early activation marker CD69 with an IC50 of 0.11 μM in B cells in human whole blood[1].
    Cerdulatinib (0.015-2 μM) inhibits FcεRI-mediated basophil degranulation with an IC50 of 0.12 μM[1].
    Cerdulatinib (0.5-4 μM) exhibits differential potency against cytokine JAK/STAT signaling pathways[1].
    Cerdulatinib (0-15 μM; 72 hours) results in viability effects similar to that of the combines SYK plus JAK-selective inhibition[1].
    Cerdulatinib (1-3 μM; 48 hours) induces apoptosis in BCR-signaling competent non-Hodgkin lymphoma (NHL) cell lines[1].

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

    Cerdulatinib hydrochloride Related Antibodies

    Cell Viability Assay[1]

    Cell Line: SU-DHL4; SU-DHL6; Ramosand and Daudi cells
    Concentration: 0, 1, 3 μM
    Incubation Time: 48 hours
    Result: Inhibits cells viability with the IC50s of 0.73-1.39 μM.

    Apoptosis Analysis[1]

    Cell Line: SU-DHL4, SU-DHL6, and Ramos cells
    Concentration: 0, 1.6, 5.0, 15 μM
    Incubation Time: 72 hours
    Result: Induced SU-DHL4, SU-DHL6, and Ramos cells apoptosis.
    In Vivo

    Cerdulatinib (0.5-5 mg/kg; twice daily p.o. for 2 weeks) elicits dose-dependent efficacy in the rat collagen-induced arthritis (CIA) model[1].
    Cerdulatinib ( mg/kg; twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in mice[1].

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

    Animal Model: Female Lewis rats (7-8 weeks old; 159-187 g) are immunized[1]
    Dosage: 0, 0.5, 1.5, 3, 5 mg/kg
    Administration: Oral gavage twice daily for 2 weeks
    Result: Modulated inflammation in the rat CIA treatment model.
    Affected anticollagen antibody formation.
    Animal Model: Balb/c mice are received BCR stimulation[1]
    Dosage: 0, 1, 5, 15, 20, 30 mg/kg
    Administration: Oral gavage twice daily for 5 days
    Result: Suppressed upregulation of splenic B-cell surface CD80/86 and CD69 by＞60%.
    Inhibited mouse splenomegaly in a dose- and concentration-dependent manner.
    Clinical Trial
    Molecular Weight

    482.00

    Formula

    C20H28ClN7O3S
    CAS No.
    Appearance

    Solid

    Color

    Light brown to brown

    SMILES

    O=S(N(CC1)CCN1C2=CC=C(NC3=NC=C(C(N)=O)C(NC4CC4)=N3)C=C2)(CC)=O.Cl
    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 : 20 mg/mL (41.49 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0747 mL 10.3734 mL 20.7469 mL
    5 mM 0.4149 mL 2.0747 mL 4.1494 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)

    Mass
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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

    ×
    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 mg/mL (4.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
    • Protocol 2

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

      Solubility: ≥ 2 mg/mL (4.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
    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
    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 2.0747 mL 10.3734 mL 20.7469 mL 51.8672 mL
    5 mM 0.4149 mL 2.0747 mL 4.1494 mL 10.3734 mL
    10 mM 0.2075 mL 1.0373 mL 2.0747 mL 5.1867 mL
    15 mM 0.1383 mL 0.6916 mL 1.3831 mL 3.4578 mL
    20 mM 0.1037 mL 0.5187 mL 1.0373 mL 2.5934 mL
    25 mM 0.0830 mL 0.4149 mL 0.8299 mL 2.0747 mL
    30 mM 0.0692 mL 0.3458 mL 0.6916 mL 1.7289 mL
    40 mM 0.0519 mL 0.2593 mL 0.5187 mL 1.2967 mL
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    Cerdulatinib hydrochloride Related Classifications

    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:

    Cerdulatinib1369761-01-2PRT062070PRT2070PRT 062070PRT-062070PRT 2070PRT-2070SykJAKSpleen tyrosine kinaseJanus kinaseTyk2dualSYKautoimmuneB-cellmalignanciesInhibitorinhibitorinhibit

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