Cerdulatinib (hydrochloride)

Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC₅₀s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies^[1][2]. IC50 & Target:IC50: 0.5 nM (SYK); 32 nM (SYK); 12 nM (JAK1); 6 nM (JAK2); 8 nM (JAK3)^[1] In Vitro: Cerdulatinib (0.03-4 μM) inhibits ERK Y204 phosphorylation with an IC₅₀ of 0.5 μM and reduces the ability to upregulate cellsurface expression of the early activation marker CD69 with an IC₅₀ of 0.11 μM in B cells in human whole blood^[1].
Cerdulatinib (0.015-2 μM) inhibits FcεRI-mediated basophil degranulation with an IC₅₀ of 0.12 μM^[1].
Cerdulatinib (0.5-4 μM) exhibits differential potency against cytokine JAK/STAT signaling pathways^[1].
Cerdulatinib (0-15 μM; 72 hours) results in viability effects similar to that of the combines SYK plus JAK-selective inhibition^[1].
Cerdulatinib (1-3 μM; 48 hours) induces apoptosis in BCR-signaling competent non-Hodgkin lymphoma (NHL) cell lines^[1]. In Vivo: Cerdulatinib (0.5-5 mg/kg; twice daily p.o. for 2 weeks) elicits dose-dependent efficacy in the rat collagen-induced arthritis (CIA) model^[1].
Cerdulatinib ( mg/kg; twice daily p.o. for 5 days) blocks BCR-induced B-cell activation and splenomegaly in mice^[1].