Cerdulatinib hydrochloride (PRT062070) is a potent, ATP-competitive, orally active dual SYK/JAK inhibitor with IC50 of 32 nM (Syk), 0.5-12 nM (JAK1/2/3, Tyk2).
Cerdulatinib (PRT062070) has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphoma; Cerdulatinib (PRT062070) demonstrates specificity towards JAK1/JAK3 and TYK2, but not JAK2-mediated responses at cellular level, does not inhibit TCR signaling or PKC signaling in whole blood.
Cerdulatinib (PRT062070) blocks cell cycle in both ABC and GCB subtypes of DLBCL via inhibition of RB phosphorylation and down-regulation of cyclin E.
Cerdulatinib (PRT062070) induces cell cycle arrest and apoptosis under the condition of BCR stimulation in DLBCL cell lines.
Cerdulatinib (PRT062070) suppressed inflammation and autoantibody generation in a rat collagen-induced arthritis model and blocked B-cell activation and splenomegaly in a mouse model of chronic B-cell antigen receptor stimulation.
