Cerdulatinib (PRT062070) hydrochloride

Synonyms: PRT2070 hydrochloride

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

Cerdulatinib (PRT062070) hydrochloride Chemical Structure

CAS: 1369761-01-2

Selleck's Cerdulatinib (PRT062070) hydrochloride has been cited by 17 publications

Purity & Quality Control

Batch: Purity: 99.66%
99.66

Cerdulatinib (PRT062070) hydrochloride Related Products

Signaling Pathway

Choose Selective JAK Inhibitors

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 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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images 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 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]
Animal Research Animal Models Rat collagen-induced arthritis model
Dosages ~5 mg/kg twice daily
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04103060 Completed
Vitiligo
Dermavant Sciences GmbH|Dermavant Sciences Inc.
September 27 2019 Phase 2
NCT01994382 Completed
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 Inc.|Portola Pharmaceuticals
August 30 2013 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 482 Formula

C20H28ClN7O3S

CAS No. 1369761-01-2 SDF Download Cerdulatinib (PRT062070) hydrochloride SDF
Smiles CCS(=O)(=O)N1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4CC4)C(=O)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 20 mg/mL ( (41.49 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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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