Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Talmapimod (SCIO-469) 是 选择性的,具有口服活性的,ATP 竞争性的 p38α抑制剂,对 p38α和 p38β的 IC50 值分别是 9 nM 和90 nM。Talmapimod 在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 497 | 现货 | ||
2 mg | ¥ 737 | 现货 | ||
5 mg | ¥ 996 | 现货 | ||
10 mg | ¥ 1,720 | 现货 | ||
25 mg | ¥ 3,650 | 现货 | ||
50 mg | ¥ 5,260 | 现货 | ||
100 mg | ¥ 7,430 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,190 | 现货 |
产品描述 | Talmapimod (SCIO-469) is an selective, orally active, and ATP-competitive p38α inhibitor with IC50 of 9 nM and 90 nM for p38α and p38β, respectively. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs. |
靶点活性 | p38β:90 nM, p38α:9 nM |
体外活性 | phosphorylation of p38 MAPK inhibited by Talmapimod (100-200 nM; 1 hour) in MM cells[1].In human whole blood, LPS-induced TNF-a production inhibited by Talmapimod [2]. Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells[3]. |
体内活性 | Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden,and preventing the development of myeloma bone disease[2]. In 5T2MM and 5T33MM models,Talmapimod inhibits the growth of multiple myeloma and prevents bone diseases[3]. 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[4]. |
别名 | 他匹莫德, SCIO-469 |
分子量 | 513 |
分子式 | C27H30ClFN4O3 |
CAS No. | 309913-83-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (185.19 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9493 mL | 9.7466 mL | 19.4932 mL | 48.7329 mL |
5 mM | 0.3899 mL | 1.9493 mL | 3.8986 mL | 9.7466 mL | |
10 mM | 0.1949 mL | 0.9747 mL | 1.9493 mL | 4.8733 mL | |
20 mM | 0.0975 mL | 0.4873 mL | 0.9747 mL | 2.4366 mL | |
50 mM | 0.039 mL | 0.1949 mL | 0.3899 mL | 0.9747 mL | |
100 mM | 0.0195 mL | 0.0975 mL | 0.1949 mL | 0.4873 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Talmapimod 309913-83-5 MAPK p38 MAPK cytotoxicity multiple inhibit 他匹莫德 tumor SCIO469 cells SCIO-469 Hsp27 Inhibitor phosphorylation SCIO 469 myeloma inhibitor