Cerdulatinib (PRT062070) hydrochloride

For research use only.

Catalog No.S7634 Synonyms: PRT2070 hydrochloride

10 publications

Cerdulatinib (PRT062070) hydrochloride Chemical Structure

CAS No. 1369761-01-2

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.

Selleck's Cerdulatinib (PRT062070) hydrochloride has been cited by 10 publications

Purity & Quality Control

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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)
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 ; 

PubMed: 28088788     


Immunoblots of MCL-1 and PARP. Following cerdulatinib treatment for 48 hrs at indicated concentrations, MCL-1 and PARP1 cleavage were measured by Western blot in whole cell lysates. GAPDH was included as the loading control.

p-SYK / SYK / p-BTK / BTK ; 

PubMed: 28088788     


Immunoblots for early BCR components SYK and BTK following cerdulatinib treatment. Freshly isolated CLL cells (N = 6) were treated with increasing doses of cerdulatinib in the presence of combined stimulation with soluble anti-IgM, CD40L and CpG. p-SYK, total SYK, p-BTK and total BTK were blotted in whole cell extracts. GAPDH served as a loading control.

p-JAK1 / JAK1 / p-JAK3 / JAK3 / p-STAT6 / STAT6 / p-JAK2 / JAK2 / p-STAT3; 

PubMed: 28088788     


C. Immunoblots for JAK-STAT following IL4 stimulation and cerdulatinib treatment. Freshly isolated CLL cells (N = 6) were treated with increasing concentrations of cerdulatinib in the presence of combined stimulation with anti-IgM, CD40L and CpG. p-JAK1, total JAK1, p-JAK3, total JAK3, p-STAT6 and t-STAT6 were blotted in whole cell extracts. D. Immunoblots for JAK-STAT following IL6 stimulation and cerdulatinib treatment. Freshly isolated CLL cells (N = 4) were treated with increasing doses of cerdulatinib in the presence of IL-6. P-JAK1, total JAK1, p-JAK2, total JAK2, p-STAT3 and t-STAT3 were blotted in whole cell extracts.

28088788
Growth inhibition assay
Cell metabolic activity; 

PubMed: 26575169     


A. DLBCL cell lines were treated with various concentrations of cerdulatinib for 72 h followed by MTT assay. GCB are highlighted in blue and ABC in red. B. IC50 values were calculated.

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

Kinase Assay:[1]
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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]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Rat collagen-induced arthritis model
  • Dosages: ~5 mg/kg twice daily
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 43 mg/mL warmed (89.21 mM)
Water Insoluble
Ethanol Insoluble
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

* 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.

Chemical Information

Molecular Weight 482
Formula

C20H28ClN7O3S
CAS No. 1369761-01-2
Storage powder
in solvent
Synonyms PRT2070 hydrochloride
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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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 September 27 2019 Phase 2
NCT01994382 Active not recruiting Drug: Cerdulatinib (PRT062070) 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) Portola Pharmaceuticals August 2013 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID