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S84867

Talmapimod

源叶(MedMol) 98%
  • 英文名:
  • Talmapimod
  • 别名:
  • CAS号:
  • 309913-83-5
  • 分子式:
  • C27H30ClFN4O3
  • 分子量:
  • 513
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S84867-5mg 98% ¥990.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S84867-10mg 98% ¥1720.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S84867-25mg 98% ¥3600.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S84867-50mg 98% ¥5200.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs
  • 靶点: p38α:9 nM (IC50);p38β:90 nM (IC50);p38MAPK
  • 体内研究:
    Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease. Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models. Talmapimod (10-90 mg/kg; p.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination Animal Model: Six-week-old male triple immune-deficient BNX mice (RPMI-8226 MM palpable tumors) Dosage: P.o.; twice daily orally for 14 days Administration: 10, 30, 90 mg/kg Result: Dose-dependently reduced tumor growth.
  • 参考文献:
    1. Hideshima T et al. p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene. 2004 Nov 18, 23(54), 8766-76. 2. Navas T, et al. Inhibition of p38alpha MAPK disrupts the pathological loop of proinflammatory factor production in the myelodysplastic syndrome bone marrow microenvironment. Leuk Lymphoma. 2008 Oct;49(10):1963-75. 3. Vanderkerken K et al. Inhibition of p38alpha mitogen-activated protein kinase prevents the development of osteolytic bone disease,reduces tumor burden, and increases survival in murine models of multiple myeloma. Cancer Res. 2007 May 15;67(10):4572-7. 4. Medicherla S, et al. p38alpha-selective MAP kinase inhibitor reduces tumor growth in mouse xenograft models of multiple myeloma. Anticancer Res. 2008 Nov-Dec;28(6A):3827-33.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: 2-8℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.949 ml 9.747 ml 19.493 ml
    5 mM 0.39 ml 1.949 ml 3.899 ml
    10 mM 0.195 ml 0.975 ml 1.949 ml
    50 mM 0.039 ml 0.195 ml 0.39 ml
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