Cerdulatinib (PRT062070) 是一种有效的选择性 Tyk2 抑制剂，IC₅₀ 为 0.5 nM。Cerdulatinib (PRT062070) 是 JAK 和 SYK 的双抑制剂，抑制JAK1，2，3 和SYK的 IC₅₀ 分别为12，6，8 和 32。

Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC 50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC 50 s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.

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Tyk2 0.5 nM (IC50) JAK2 6 nM (IC50

Cerdulatinib shows inhibitory effect on 60 CLL with IC50 ranging from 0.37 to 10.02 μM. Cerdulatinib induces apoptosis in CLL in association with MCL-1 down-regulation and PARP cleavage. Cerdulatinib (2μM) is able to overcome the support of the microenvironment and induces CLL cell death. Cerdulatinib (250-500 nM) blocks proliferation of ibrutinib-sensitive and ibrutinib-resistant primary CLL cells. Cerdulatinib also blocks proliferation of both ibrutinib-sensitive and ibrutinib-resistant primary CLL cells as well as BTKC481S-transfected cell lines, and blocks BCR and JAK-STAT signaling pathways. Furthermore, inhibition of SYK and JAK by cerdulatinib translates to downstream inhibition of AKT and ERK. Cerdulatinib inhibits the activity of NF-kB pathway. PRT062070 reduces the ability of stimulated B cells to upregulate cell-surface expression of the early activation

PRT062070 (0.5 mg/kg) results in a nonstatistically significant trend toward reduced ankle inflammation, whereas significant reductions in inflammation are achieved with the 1.5, 3, and 5 mg/kg doses. PRT062070 also affects anticollagen antibody formation. PRT062070 (15 mg/kg) suppresses upregulation of splenic B-cell surface CD80/86 and CD69, and inhibits BCR signaling and activation in the spleen after oral dosing in mice. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Guo A, et al. Dual SYK/JAK inhibition overcomes ibrutinib resistance in chronic lymphocytic leukemia: Cerdulatinib, but not ibrutinib, induces apoptosis of tumor cells protected by the microenvironment. Oncotarget. 2017 Feb 21;8(8):12953-12967.
[2]. Coffey G, et al. The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther. 2014 Dec;351(3):538-48.

In Vitro: DMSO : ≥ 30 mg/mL (67.33 mM)配制储备液