Cerdulatinib (PRT062070) hydrochloride

Catalog No.S7634 Batch:S763401

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Technical Data

Formula

C20H28ClN7O3S
Molecular Weight 482 CAS No. 1369761-01-2
Solubility (25°C)* In vitro DMSO 20 mg/mL (41.49 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
Targets
TYK2 [1]
(Cell-free assay)		 MST1 [1]
(Cell-free assay)		 ARK5 [1]
(Cell-free assay)		 MLK1 [1]
(Cell-free assay)		 Fms [1]
(Cell-free assay)		 View More
0.5 nM 4 nM 4 nM 5 nM 5 nM
In vitro 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. [1]
In vivo In 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. [1]

Protocol (from reference)

Kinase Assay:[1]
  • Purified Kinase Assays

    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:[1]
  • Cell lines

    Ramos RA-1, Daudi, Toledo, SU-DHL4 and SU-DHL6 cells

  • Concentrations

    ~15 μM

  • Incubation Time

    72 hours

  • Method

    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.

Animal Study:[1]
  • Animal Models

    Rat collagen-induced arthritis model

  • Dosages

    ~5 mg/kg twice daily

  • Administration

    p.o.

Selleck's Cerdulatinib (PRT062070) hydrochloride has been cited by 19 publications

A panel of janus kinase inhibitors identified with anti-inflammatory effects protect mice from lethal influenza virus infection [ Antimicrob Agents Chemother, 2024, 68(4):e0135023.] PubMed: 38470034
Naegleria fowleri Extracellular Vesicles Induce Proinflammatory Immune Responses in BV-2 Microglial Cells [ Int J Mol Sci, 2023, 24(17)13623] PubMed: 37686429
Immunomodulation of Natural Killer Cell Function by Ribavirin Involves TYK-2 Activation and Subsequent Increased IFN-γ Secretion in the Context of In Vitro Hepatitis E Virus Infection [ Cells, 2023, 12(3)453] PubMed: 36766795
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] PubMed: 35868306
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] PubMed: 35118583
Constitutive JAK/STAT signaling is the primary mechanism of resistance to JAKi in TYK2-rearranged acute lymphoblastic leukemia [ Cancer Lett, 2021, 512:28-37] PubMed: 33971281
Feed-forward activation of STAT3 signaling limits the efficacy of c-Met inhibitors in esophageal squamous cell carcinoma (ESCC) treatment [ Mol Carcinog, 2021, 60(7):481-496] PubMed: 34018249
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] PubMed: 34304386
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] PubMed: 34383271

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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