Cayman Cerdulatinib

Cerdulatinib is a dual inhibitor of spleen tyrosine kinase (Syk) and Janus kinases (JAK; IC₅₀s = 32, 12, 6, 8, and 0.5 nM for Syk, JAK1, JAK2, JAK3, and TYK2, respectively) and also exhibits nanomolar inhibition of other kinases.¹ Syk is involved in the B cell receptor (BCR) pathway, and cerdulatinib inhibits downstream Syk-mediated signaling of ERK Y204 phosphorylation (IC₅₀ = 0.5 μM), upregulates cell surface expression of CD69 (IC₅₀ = 0.11 μM), and inhibits FcεRI-mediated basophil degranulation (IC₅₀ = 0.12 μM).¹ JAK is involved in JAK-STAT regulation of cytokine receptors. Cerdulatinib inhibits STAT3, STAT5, and STAT6 phosphorylation by interleukin-activated JAK1/3 with IC₅₀ values ranging from 0.16 to 1 μM.¹ Cerdulatinib disrupts JAK1/3-mediated signaling more selectively than JAK2 signaling (IC₅₀ > 4 μM).¹ Cerdulatinib displays potent antitumor activity against ABC and GCB types of diffuse large B cell lymphoma (DLBCL) by inducing apoptosis via caspase-2 and poly(ADP-ribose) polymerase (PARP) cleavage.² Cerdulatinib exhibits IC₅₀ values ranging from 0.05 to 2.1 μM against a panel of DLBCL tumor cell lines.²

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