Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Epothilone D (KOS 862) is an effective microtubule stabilizer.
产品描述 | Epothilone D (KOS 862) is an effective microtubule stabilizer. |
体外活性 | Epothilone D is a more potent microtubule stabilizer in vitro than epothilone A or B. In vitro, Epothilone D has shown potent cytotoxicity in a panel of human tumor cell lines, with similar potency to paclitaxel. Epothilone D also shows a definite advantage over paclitaxel in drug-resistant cell lines and retained its cytotoxicity against a multidrug-resistant cell line over-expressing P-glycoprotein [1]. |
体内活性 | To evaluate whether Epothilone D improves MT and axonal function in PS19 mice, groups of 3-month old male PS19 mice received weekly i.p. injections of vehicle or Epothilone D (1 mg/kg or 3 mg/kg) for a total of 3 months. In addition, 3-month old non-Tg littermates received 3 mg/kg Epothilone D or vehicle. The 3 mg/kg Epothilone D dose corresponds to ~10-fold less than that used in Phase II clinical study, which should minimize side-effects such as neutropenia that are observed with MT-stabilizing drugs in human subjects. PS19 and WT mice that receive Epothilone D show no signs of drug intolerance. Indeed, all drug-treated mice exhibited weight gain that is indistinguishable from vehicle-treated animals. Likewise, relative organ weights are similar in vehicle- and Epothilone D-treated mice. The motor performance of Epothilone D-treated mice, assessed using a standard rotarod test, is not significantly different from vehicle-treated cohorts [2]. |
动物实验 | Groups of mice (n=3) receive intraperitoneal (i.p.) injections of 3.7 mg/kg of Epothilone D (epoD) dissolved in 100% DMSO, followed by euthanization using approved at times ranging from 0.25 h to 24 h. In another study, groups of mice (n=3) receive injections of 3 mg/kg of epoD in 100% DMSO followed by euthanization 4, 6 and 10 days later. The Epothilone D (epoD) levels in the brain and blood samples are determined using LC-MS/MS protocols. Groups (n=10-13) of 3-month old PS19 tau Tg mice or 3-month old non-Tg littermates are administered weekly i.p. injections of 1 mg/kg epoD, 3 mg/kg of Epothilone D (epoD) or vehicle (DMSO), for a total of 3 months. Animals are monitored for signs of abnormal behavior or distress and are weighed weekly. After final dosing, the mice undergo motor function and cognitive testing. After euthanization, brains and optic nerve (ON) are recovered for immunohistochemical analyses. A subset of mice from each group also undergo necropsy evaluation with organ weights recorded [2]. |
别名 | KOS 862, 埃博霉素 |
分子量 | 491.68 |
分子式 | C27H41NO5S |
CAS No. | 189453-10-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 300 mg/mL (610.15 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0338 mL | 10.1692 mL | 20.3384 mL | 50.8461 mL |
5 mM | 0.4068 mL | 2.0338 mL | 4.0677 mL | 10.1692 mL | |
10 mM | 0.2034 mL | 1.0169 mL | 2.0338 mL | 5.0846 mL | |
20 mM | 0.1017 mL | 0.5085 mL | 1.0169 mL | 2.5423 mL | |
50 mM | 0.0407 mL | 0.2034 mL | 0.4068 mL | 1.0169 mL | |
100 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5085 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。
Epothilone D 189453-10-9 Cytoskeletal Signaling Microtubule Associated KOS-862 KOS862 KOS 862 埃博霉素 Inhibitor inhibitor inhibit