Cerdulatinib (PRT062070, PRT2070) 1369761-01-2

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Molecular Weight:

482 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.


Biological Activity


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.


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.


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.

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.

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Product Categories : Epigenetics > JAK Inhibitor