Cerdulatinib
货号：
20076-5mg 基本售价：
686.0 元 规格：
5 mg
产品信息
概述| 货号 | 20076-5mg |
| 描述 | 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 |
| 别名 | PRT062070;PRT2070; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Coffey, G.,Betz, A.,DeGuzman, F., et al. The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J. Pharmacol. Exp. Ther. 351(3), 538-548 (2014).
2.Ma, J.,Xing, W.,Coffey, G., et al. Cerdulatinib, a novel dual SYK/JAK kinase inhibitor, has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphoma. Oncotarget 6(41), 43881-43896 (2015).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 445.5 |
| 分子式 | C20H27N7O3S |
| CAS号 | 1198300-79-6 |
| 稳定性 | ≥ 2 years |
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