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    Cerdulatinib HCl (PRT-2070; PRT-062070)
    Cerdulatinib HCl (PRT-2070; PRT-062070)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0325
    CAS #: 1369761-01-2Purity ≥98%

    Description: Cerdulatinib HCl (formerly PRT2070; PRT062070) is a novel, potent, selective orally bioactive, and multi-targeted tyrosine kinase inhibitor of JAK1/2/3/TYK2 and Syk with potential antitumor activity. It inhibits JAK1/JAK2/JAK3/TYK2 and Syk with IC50s of 12 nM/6 nM/8 nM/0.5 nM and 32 nM, respectively. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. Cerdulatinib also inhibits 19 other tested kinases with IC50 less than 200 nM. It is currently being studied in patients with genetically-defined hematologic cancers, as well as for patients who have failed therapy due to relapse or acquired mutations.

    References: J Pharmacol Exp Ther. 2014 Dec;351(3):538-48.

    Related CAS: 1198300-79-6 (free base); 1369761-01-2 (HCl);

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    Molecular Weight (MW)482 (HCl salt)
    FormulaC20H28ClN7O3S
    CAS No.1369761-01-2 (HCl salt)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 43 mg/mL (89.2 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo) 5% DMSO+corn oil: 3mg/mL 
    Synonyms

    PRT062070; PRT 062070; PRT062070, PRT2070; PRT2070; PRT-2070; PRT 2070; PRT-06270

    0Chemical Name: 4-(cyclopropylamino)-2-((4-(4-(ethylsulfonyl)piperazin-1-yl)phenyl)amino)pyrimidine-5-carboxamide hydrochloride

    InChi Key: BGLPECHZZQDNCD-UHFFFAOYSA-N

    InChi Code: InChI=1S/C20H27N7O3S/c1-2-31(29,30)27-11-9-26(10-12-27)16-7-5-15(6-8-16)24-20-22-13-17(18(21)28)19(25-20)23-14-3-4-14/h5-8,13-14H,2-4,9-12H2,1H3,(H2,21,28)(H2,22,23,24,25)

    SMILES Code: O=C(C1=CN=C(NC2=CC=C(N3CCN(S(=O)(CC)=O)CC3)C=C2)N=C1NC4CC4)N


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    In Vitro

    In vitro activity: In human whole blood from normal donors, Cerdulatinib affects BCR-mediated B-cell activation by dual inhibition of SYK and JAK. As a dual SYK/JAK inhibitor, Cerdulatinib significantly reduces cell viability in a subset of NHL cell lines, and induces apoptosis in BCR-signaling competent NHL cell lines.


    Kinase Assay: Potency against purified SYK is determined by fluorescence resonance energy transfer. A broader panel of 270 purified kinases is surveyed in which PRT062070 is tested at a fixed concentration of 300 nM. [33P]-labeled substrate is measured after incubation of purified kinase with peptide substrate and [33P]ATP at the Km concentration for the kinase. 


    Cell Assay: Cell lines (Ramos RA-1, Daudi, Toledo, SU-DHL4 and SU-DHL6) are cultured in RPMI media supplemented with 10% fetal bovine serum. Cells are treated with the indicated concentrations of PRT062070, the SYK-selective inhibitor PRT060318, the pan-JAK inhibitor 1, a 1:1 combination of PRT060318 and JAK inhibitor 1, or vehicle control (0.5% dimethylsulfoxide) for 72 hours. Cell viability assays are performed using CellTiter Glo in 384-well plates. Cells are seeded at a density of 5000 cells per well.

    In VivoIn a rat collagen-induced arthritis model, Cerdulatinib (5 mg/kg p.o.) significantly improves inflammatory infiltrate within the synovium and the integrity of the articular cartilage. In addition, Cerdulatinib also blocks BCR-induced B-cell activation and splenomegaly in mice.
    Animal modelRat collagen-induced arthritis model
    Formulation & DosageDissolved in 0.5% methylcellulose in water; 5 mg/kg; Oral administration
    References

    J Pharmacol Exp Ther. 2014 Dec;351(3):538-48.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Cerdulatinib HCl salt

    PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways. J Pharmacol Exp Ther. 2014 Dec;351(3):538-48. 

    Cerdulatinib HCl salt

    Dose responsive effect of PRT062070 in rat CIA treatment model. J Pharmacol Exp Ther. 2014 Dec;351(3):538-48. 

    Cerdulatinib HCl salt

    PRT062070 blocks BCR-induced B-cell activation and splenomegaly in mice. J Pharmacol Exp Ther.2014 Dec;351(3):538-48. 


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