Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-580 (MLN2480) 是一种可口服的选择性Raf 广谱抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
2 mg | ¥ 673 | 现货 | ||
5 mg | ¥ 997 | 现货 | ||
10 mg | ¥ 1,790 | 现货 | ||
25 mg | ¥ 3,250 | 现货 | ||
50 mg | ¥ 4,750 | 现货 | ||
100 mg | ¥ 6,770 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,180 | 现货 |
产品描述 | TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials. |
体外活性 | MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preClinicalal cancer models at concentrations that are tolerated in vivo. It is found to activate phosphorylated MEK at very low concentrations, but inhibits this same activity at higher concentrations. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts. In vitro analysis of this drug combination of MLN2480 and TAK-733(an investigational allosteric MEK kinase inhibitor) in cell proliferation assays demonstrates synergistic activity. In addition, western blot analysis demonstrates the effect of MLN2480 in reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition.MLN-2480 only modestly inhibits PRAK. |
体内活性 | In vivo, MLN2480 shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models.MLN-2480 (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of MLN-2480 (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produces negligible effects. |
动物实验 | [4]Animal Models: C57BL/6J miceFormulation: 100% PEG400Dosages: 12.5 mg/kgAdministration: oral gavage |
别名 | MLN2480, BIIB-024 |
分子量 | 506.29 |
分子式 | C17H12Cl2F3N7O2S |
CAS No. | 1096708-71-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (183.7 mM)
Ethanol: 93 mg/mL (183.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.9752 mL | 9.8758 mL | 19.7515 mL | 49.3788 mL |
5 mM | 0.395 mL | 1.9752 mL | 3.9503 mL | 9.8758 mL | |
10 mM | 0.1975 mL | 0.9876 mL | 1.9752 mL | 4.9379 mL | |
20 mM | 0.0988 mL | 0.4938 mL | 0.9876 mL | 2.4689 mL | |
50 mM | 0.0395 mL | 0.1975 mL | 0.395 mL | 0.9876 mL | |
100 mM | 0.0198 mL | 0.0988 mL | 0.1975 mL | 0.4938 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。
TAK-580 1096708-71-2 MAPK Raf MLN 2480 BIIB 024 Raf kinases inhibit MLN-2480 TAK 580 BIIB024 MLN2480 Inhibitor TAK580 BIIB-024 inhibitor