Home JAK/STAT JAK inhibitor - Syk inhibitor Cerdulatinib (PRT062070) hydrochloride For research use only.

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 18 publications

Purity & Quality Control

Batch: Purity: 99.66%
99.66

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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 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 lnformation & 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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