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CEP-33779
CEP-33779
CEP-33779
商品货号:MB3929
CAS 号:1257704-57-6
英文名字:CEP33779
质量标准:>98%,选择性JAK2抑制剂
分子式:C24H26N6O2S
  • 包装规格:
    规格 库存 发货时间
    5MG [¥1800.00]15 现货,一周内发货
    10MG [¥2600.00]15 现货,一周内发货
    50MG [¥6800.00]15 现货,一周内发货
  • 购买数量:
  • 会员尊享价:

    商品信息

    质检证书(coa)

    说明书下载

     CEP33779

    分子式:C24H26N6O2S   分子量:462.57

     

    产品描述

    CEP33779是选择性JAK2抑制剂,IC501.8 nM, 比作用于JAK1TYK2选择性高40多倍和800多倍。

    靶点

    JAK2

             

    IC50

    1.8 nM

             

    体外研究

    CEP33779(< 3 μM) inhibits phosphorylation of downstream target signal transducer and activator of transcription 5(pSTAT5) of JAK2 in a concentration dependent manner in HEL92 cells.

    体内研究

    CEP33779 orally administrated with 55 mg/kg inhibits phosphorylation of STAT5 in HEL92 tumor extracts from HEL92 xenograft mice. CEP33779 orally administered twice daily at dose of 55 mg/kg reduces mean paw edema and clinical scores in mice with collagen-antibody induced arthritis (CAIA) or collagen-induced arthritis (CIA). CEP33779 orally administered twice daily at dose of 55 mg/kg totally inhibits paw phospho-STAT3 expression in CAIA or CIA mice, associated with decreased cytokines including IL-12, IFNγ, IL-2, IL-1β, TNFα and GM-CSF. CEP33779 results in reduced bone degradation, reduced tissue destruction, and reduced osteoarthritis in dose-dependent manner in CAIA or CIA mice.CEP33779 orally administrated at 100 mg/kg extends survival and reduces splenomegaly/lymphomegaly in MRL/lpr systemic lupus erythematosus mice, thus protect mice from developing glomerulonephritis. CEP33779 orally administrated at 100 mg/kg decreases several SLE-associated proinflammatory cytokines and reduces levels of a bone resorption biomarker associated with increased osteoclast activity in MRL/lpr systemic lupus erythematosus mice.CEP33779 orally administered twice daily at dose of 55 mg/kg induces regression of established colorectal tumors, reduces angiogenesis, and reduces proliferation of tumor cells in a mouse model of colitis-induced colorectal cancer. Tumor regression correlated with inhibition of STAT3 and NF-κB (RelA/p65) activation, and decreased the expression of proinflammatory, tumor-promoting cytokines interleukin (IL)-6 and IL-1β.

    临床实验

    DMSO 93 mg/mL,水 <1 mg/mL,乙醇 <1 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

             
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