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Cerdulatinib

CAS No. : 1198300⁻⁷9-6

MCE 国际站：Cerdulatinib

产品活性：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。

研究领域：Epigenetics | Stem Cell/Wnt | JAK/STAT Signaling | Protein Tyrosine Kinase/RTK

作用靶点：JAK | Syk

In Vitro: 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 marker CD69 (IC₅₀=0.11 µM). PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways. PRT062070 (1 or 3 µM) induces apoptosis in BCR-signaling competent NHL cell lines. Cerdulatinib demonstrates inhibitory activity against both ABC ａnd GCB subtypes of DLBCL cells. Cerdulatinib also induces apoptosis in both GCB ａnd ABC subtypes of DLBCL cell lines via caspase 3 ａnd PARP cleavage. And cerdulatinib blocks cell cycle in both ABC ａnd GCB subtypes of DLBCL via inhibition of RB phosphorylation ａnd down-regulation of cyclin E. Cerdulatinib induces cell cycle arrest ａnd apoptosis under the condition of BCR stimulation in all DLBCL cell lines. Besides, cerdulatinib blocks JAK/STAT ａnd BCR signaling in both ABC ａnd GCB DLBCL cell lines. Cerdulatinib induces cell death in primary human DLBCL samples. Cerdulatinib inhibits BCR-induced signals in a dose-dependent manner ａnd most strongly between 0.3 to 1 μM. ａnd particularly in IGHV-unmutated samples with greater BCR signaling capacity ａnd response to IL4, or samples expressing higher levels of sIgM, CD49d⁺, or ZAP70⁺. Cerdulatinib overcomes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing upregulation of MCL-1 ａnd BCL-X_L; however, BCL-2 expression is unaffected. Furthermore, in samples treated with IL4/CD40L, cerdulatinib synergizes with venetoclax in vitro to induce greater apoptosis than either drug alone.

In Vivo: 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.

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