Home JAK/STAT JAK inhibitor - Syk inhibitor Cerdulatinib (PRT062070) hydrochloride

Cerdulatinib (PRT062070) hydrochloride

Catalog No.S7634 Synonyms: PRT2070 hydrochloride

For research use only.

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.

Cerdulatinib (PRT062070) hydrochloride Chemical Structure

CAS No. 1369761-01-2

Selleck's Cerdulatinib (PRT062070) hydrochloride has been cited by 14 publications

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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)		 Click to View More Targets
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]
Assay
Methods Test Index PMID
Western blot Mcl-1 / PARP ; p-SYK / SYK / p-BTK / BTK ; p-JAK1 / JAK1 / p-JAK3 / JAK3 / p-STAT6 / STAT6 / p-JAK2 / JAK2 / p-STAT3 28088788
Growth inhibition assay Cell metabolic activity 26575169
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 Research:[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 Research:[1]
  • Animal Models: Rat collagen-induced arthritis model
  • Dosages: ~5 mg/kg twice daily
  • Administration: p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.

 3mg/mL

Chemical Information

Molecular Weight 482
Formula

C20H28ClN7O3S
CAS No. 1369761-01-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04103060 Completed Drug: Cerdulatinib 0.37% gel|Drug: Vehicle gel Vitiligo Dermavant Sciences GmbH|Dermavant Sciences Inc. September 27 2019 Phase 2
NCT01994382 Completed Drug: Cerdulatinib|Biological: Rituximab Follicular Lymphoma (FL/Indolent NHL)|Aggressive NHL (a NHL)|Chronic Lymphocytic Leukemia (CLL) / Small Lymphocytic Lymphoma (SLL)|T-cell Lymphoma (PTCL and CTCL)|B-cell Non Hodgkin Lymphoma (NHL) Alexion Pharmaceuticals|Portola Pharmaceuticals August 30 2013 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-11-29)

Tech Support

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