Cerdulatinib HCl salt

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

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> ARK5
(Cell-free assay)

Target	Value
TYK2 (Cell-free assay)	0.5 nM
MST1 (Cell-free assay)	4 nM
4 nM
MLK1 (Cell-free assay)	5 nM
Fms (Cell-free assay)	5 nM