Cerdulatinib (PRT062070)

For research use only.

Catalog No.S7634 Synonyms: PRT2070

6 publications

Cerdulatinib (PRT062070) Chemical Structure

CAS No. 1369761-01-2

Cerdulatinib (PRT-062070) 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.

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Selleck's Cerdulatinib (PRT062070) has been cited by 6 publications

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Biological Activity

Description Cerdulatinib (PRT-062070) 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
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 Recruiting 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

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID