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

Cerdulatinib (Synonyms: PRT062070; PRT2070)

Cat. No.: HY-15999 Purity: 99.00%
Handling Instructions

Cerdulatinib is a novel, orally available, ATP-competitive JAK and SYK inhibitor that demonstrates selective inhibition of TYK2 and SYK with an IC50 of 0.5 nM and 32 nM.

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

Cerdulatinib Chemical Structure

Cerdulatinib Chemical Structure

CAS No. : 1198300-79-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 744 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg USD 1104 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    Cerdulatinib 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.

    View All JAK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Cerdulatinib is a novel, orally available, ATP-competitive JAK and SYK inhibitor that demonstrates selective inhibition of TYK2 and SYK with an IC50 of 0.5 nM and 32 nM.

    IC50 & Target[2]

    Tyk2

    0.5 nM (IC50)

    JAK2

    6 nM (IC50)

    JAK3

    8 nM (IC50)

    JAK1

    12 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 shows inhibitory effect on 60 CLL with IC50 ranging from 0.37 to 10.02 µM. Cerdulatinib induces apoptosis in CLL in association with MCL-1 down-regulation and PARP cleavage. Cerdulatinib (2μM) is able to overcome the support of the microenvironment and induces CLL cell death. Cerdulatinib (250-500 nM) blocks proliferation of ibrutinib-sensitive and ibrutinib-resistant primary CLL cells. Cerdulatinib also blocks proliferation of both ibrutinib-sensitive and ibrutinib-resistant primary CLL cells as well as BTKC481S-transfected cell lines, and blocks BCR and JAK-STAT signaling pathways. Furthermore, inhibition of SYK and JAK by cerdulatinib translates to downstream inhibition of AKT and ERK. Cerdulatinib inhibits the activity of NF-kB pathway[1]. PRT062070 reduces the ability of stimulated B cells to upregulate cell-surface expression of the early activation marker CD69 (IC50=0.11 µM). PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways. PRT062070 (1 or 3 µM) induces apoptosis in BCR-signaling competent NHL cell lines[2]. Cerdulatinib demonstrates inhibitory activity against both ABC and GCB subtypes of DLBCL cells. Cerdulatinib also induces apoptosis in both GCB and ABC subtypes of DLBCL cell lines via caspase 3 and PARP cleavage. And cerdulatinib blocks cell cycle in both ABC and GCB subtypes of DLBCL via inhibition of RB phosphorylation and down-regulation of cyclin E. Cerdulatinib induces cell cycle arrest and apoptosis under the condition of BCR stimulation in all DLBCL cell lines. Besides, cerdulatinib blocks JAK/STAT and BCR signaling in both ABC and GCB DLBCL cell lines. Cerdulatinib induces cell death in primary human DLBCL samples[3]. Cerdulatinib inhibits BCR-induced signals in a dose-dependent manner and most strongly between 0.3 to 1 μM. and particularly in IGHV-unmutated samples with greater BCR signaling capacity and response to IL4, or samples expressing higher levels of sIgM, CD49d+, or ZAP70+. Cerdulatinib overcomes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing upregulation of MCL-1 and BCL-XL; however, BCL-2 expression is unaffected. Furthermore, in samples treated with IL4/CD40L, cerdulatinib synergizes with venetoclax in vitro to induce greater apoptosis than either drug alone[4].

    In Vivo

    PRT062070 (0.5 mg/kg) results in a nonstatistically significant trend toward reduced ankle inflammation, whereas significant reductions in inflammation are achieved with the 1.5, 3, and 5 mg/kg doses. PRT062070 also affects anticollagen antibody formation. PRT062070 (15 mg/kg) suppresses upregulation of splenic B-cell surface CD80/86 and CD69, and inhibits BCR signaling and activation in the spleen after oral dosing in mice[2].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.2445 mL 11.2223 mL 22.4447 mL
    5 mM 0.4489 mL 2.2445 mL 4.4889 mL
    10 mM 0.2244 mL 1.1222 mL 2.2445 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    Cerdulatinib is dissolved in DMSO.

    TMD8 cells are transfected with constructs of WT BTK or BTKC481S mutants using kit V, Program U-13 on Amaxa Nucleofector. After transfection, the cells are co-cultured with NKTert cells in a 24-well plate for 24 hrs for recovery. Ibrutinib, cerdulatinib and vehicle (DMSO) are then added into the transfected TMD8 cells and cellular viability is determined with MuseTM Count & Viability kit using Muse Cell Analyzer. The cell survival is determined by flow cytometry using the Annexin V/7-AAD Apoptosis Detection Kit I on freshly isolated CLL cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    445.54

    Formula

    C₂₀H₂₇N₇O₃S

    CAS No.

    1198300-79-6

    SMILES

    O=S(N(CC1)CCN1C2=CC=C(NC3=NC=C(C(N)=O)C(NC4CC4)=N3)C=C2)(CC)=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

    Solvent & Solubility

    DMSO: ≥ 30 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.00%

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    Inquiry Information

    Product Name:
    Cerdulatinib
    Cat. No.:
    HY-15999
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