Biological Activity
Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an orally active multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 for JAK1/JAK2/JAK3/TYK2 and Syk, respectively nM and 32 nM. Also inhibits 19 other kinases tested with IC50s below 200 nM.
in vitro
Cerdulatinib affects BCR-mediated B cell activation through dual inhibition of SYK and JAK in human whole blood from normal donors. As a dual SYK/JAK inhibitor, Cerdulatinib significantly reduced cell viability in a subset of NHL cell lines and induced apoptosis in NHL cell lines with BCR signaling.
in vivo
In a rat collagen-induced arthritis model, Cerdulatinib (5 mg/kg po) significantly improved inflammatory infiltration of synovium and articular cartilage integrity. In addition, cerdulatinib also blocked BCR-induced B cell activation and splenomegaly in mice.
target
| Target | Value |
TYK2
(Cell-free assay) | 0.5 nM |
MST1
(Cell-free assay) | 4 nM |
< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> ARK5
(Cell-free assay) 4 nM |
MLK1
(Cell-free assay) | 5 nM |
Fms
(Cell-free assay) | 5 nM |
