- 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)
- 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
- 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。
输入产品批号：
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
