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主营:分子类,蛋白类,抗体类,生化类试剂
℡ 4000-520-616
℡ 4000-520-616
Selleck Chemicals/Cerdulatinib (PRT062070)/S7634
产品编号:S7634
市  场 价:¥19940.00
场      地:美国(厂家直采)
产品分类: 蛋白类>多肽>多肽合成>
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电话号码:4000-520-616
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美  元  价:$997.00
品      牌: Selleck Chemicals
公      司:Selleckchem
公司分类:
Selleck Chemicals/Cerdulatinib (PRT062070)/S7634
商品介绍
DescriptionCerdulatinib (PRT-062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
Targets
TYK2 [1](Cell-free assay)MST1 [1](Cell-free assay)ARK5 [1](Cell-free assay)MLK1 [1](Cell-free assay)Fms [1](Cell-free assay)
0.5 nM4 nM4 nM5 nM5 nM
In vitro

In human whole blood from normal donors, Cerdulatinib affects BCR-mediated B-cell activation by dual inhibition of SYK and JAK. As a dual SYK/JAK inhibitor, Cerdulatinib significantly reduces cell viability in a subset of NHL cell lines, and induces apoptosis in BCR-signaling competent NHL cell lines. [1]

Assay
MethodsTest IndexPMID
Western blot
Mcl-1 / PARP ;

PubMed: 28088788

Immunoblots of MCL-1 and PARP. Following cerdulatinib treatment for 48 hrs at indicated concentrations, MCL-1 and PARP1 cleavage were measured by Western blot in whole cell lysates. GAPDH was included as the loading control.

p-SYK / SYK / p-BTK / BTK ;

PubMed: 28088788

Immunoblots for early BCR components SYK and BTK following cerdulatinib treatment. Freshly isolated CLL cells (N= 6) were treated with increasing doses of cerdulatinib in the presence of combined stimulation with soluble anti-IgM, CD40L and CpG. p-SYK, total SYK, p-BTK and total BTK were blotted in whole cell extracts. GAPDH served as a loading control.

p-JAK1 / JAK1 / p-JAK3 / JAK3 / p-STAT6 / STAT6 / p-JAK2 / JAK2 / p-STAT3;

PubMed: 28088788

C. Immunoblots for JAK-STAT following IL4 stimulation and cerdulatinib treatment. Freshly isolated CLL cells (N= 6) were treated with increasing concentrations of cerdulatinib in the presence of combined stimulation with anti-IgM, CD40L and CpG. p-JAK1, total JAK1, p-JAK3, total JAK3, p-STAT6 and t-STAT6 were blotted in whole cell extracts. D.Immunoblots for JAK-STAT following IL6 stimulation and cerdulatinib treatment. Freshly isolated CLL cells (N= 4) were treated with increasing doses of cerdulatinib in the presence of IL-6. P-JAK1, total JAK1, p-JAK2, total JAK2, p-STAT3 and t-STAT3 were blotted in whole cell extracts.

28088788
Growth inhibition assay
Cell metabolic activity;

PubMed: 26575169

A.DLBCL cell lines were treated with various concentrations of cerdulatinib for 72 h followed by MTT assay. GCB are highlighted in blue and ABC in red.B.IC50values were calculated.

26575169
In vivoIn a rat collagen-induced arthritis model, Cerdulatinib (5 mg/kg p.o.) significantly improves inflammatory infiltrate within the synovium and the integrity of the articular cartilage. In addition, Cerdulatinib also blocks BCR-induced B-cell activation and splenomegaly in mice. [1]
品牌介绍

Selleck Chemicals提供了超过120,000种用于细胞信号通路研究的抑制剂。我们积极跟踪最新科学,因此我们的客户可以依靠我们成为最新抑制剂的领先供应商。

Selleck的生物活性化合物库由8,000多个具有经过验证的生物学和药理活性的小分子组成。这些分子的安全性和有效性已通过临床前和临床研究证明,其中许多是FDA批准的化合物。


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