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

Cerdulatinib hydrochloride (Synonyms: PRT062070 hydrochloride; PRT2070 hydrochloride)

Cat. No.: HY-15999A
Handling Instructions

Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with the 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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Top Publications Citing Use of Products

    Cerdulatinib hydrochloride purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    Cerdulatinib hydrochloride purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    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.

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    Description

    Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with the 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].

    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].

    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.
    Molecular Weight

    482.00

    Formula

    C₂₀H₂₈ClN₇O₃S

    CAS No.

    1369761-01-2

    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

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    CerdulatinibPRT062070PRT2070PRT 062070PRT-062070PRT 2070PRT-2070SykJAKSpleen tyrosine kinaseJanus kinaseTyk2dualSYKautoimmuneB-cellmalignanciesInhibitorinhibitorinhibit

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    Product Name:
    Cerdulatinib hydrochloride
    Cat. No.:
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