埃博霉素
埃博霉素 性质
| 熔点 | 63-66°C |
|---|---|
| 比旋光度 | D22 -61.3° (c = 2.5 in methanol) |
| 沸点 | 663.7±55.0 °C(Predicted) |
| 密度 | 1.084±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C Freezer |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.47±0.70(Predicted) |
| 颜色 | 白色至类白色 |
| InChIKey | XOZIUKBZLSUILX-GIQCAXHBSA-N |
| SMILES | O1[C@H](/C(/C)=C/C2=CSC(C)=N2)CC=C(C)CCC[C@H](C)[C@H](O)[C@@H](C)C(=O)C(C)(C)[C@@H](O)CC1=O |t:13| |
埃博霉素 用途与合成方法
图1为埃博霉素B结构式 生物发酵法
培养基：CNST 培养基：KNO30.05%，Na2HPO40.025%，MgSO4·7H2O 0.1%，FeC30.001%，琼脂 2%，微量元素液 1 mL/L，pH7.2。1×105Pa 高压蒸汽灭菌 20 min。
M26培养基：土豆淀粉 8.0 g/L，大豆蛋白胨 2.0g/L，葡萄糖 2.0 g/L，酵母粉 2.0 g/L，MgSO4·7H2O1.0 g/L，CaCl21.0 g/L，EDTA-Fe3+1 mL/L，微量元素1 mL/L，以 KOH 调节 pH 值为 7.2。
初始发酵培养基：糊精 0.3%，蔗糖 0.07%，葡萄糖 0.02%，豆饼粉 0.17%，七水硫酸镁 0.17%，无水氯化钙 0.3%，EDTA-Fe3+2 mL/L，微量元素（TE）0.5 mL/L，pH7.2，树脂 XAD-16 2%。1×105Pa 高压蒸汽灭菌 20 min。
培养方法
种子培养：：将保藏在固体斜面培养基的菌种接入放有已灭菌滤纸片的 CNST 平板上，倒置于恒温培养箱中在 30℃条件下培养 5-7 d 后，转接于 M26 培养基中，装液量为 50 mL/250 mL 三角瓶，在 30℃、170 r/min 的条件下摇床培养 72 h 后，得到作为发酵培养的种子液。
发酵培养：以 5%（V/V）接种量将所得种子液接种到发酵培养基中进行摇床培养，发酵体系为300 mL 三角瓶装液量为 50 mL，在 30℃、170 r/min的条件下摇床培养 5 d。 用于结肠癌、乳腺癌、卵巢癌的治疗。
有关埃博霉素B的概述、制备方法、应用是由Chemicalbook的丁红编辑整理。（2015-12-21） Epothilone D (KOS 862) 是有效的微管稳定剂。
Microtubule/Tubulin
Epothilone D (KOS-862) 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. Epothilone D (EpoD) is a microtubules (MTs)-stabilizing agent.
To evaluate whether Epothilone D (EpoD) 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 (EpoD) (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 (EpoD) or vehicle. The 3 mg/kg Epothilone D (EpoD) dose corresponds to ~10-fold less than that used in a 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 (EpoD) 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 (EpoD)-treated mice. The motor performance of Epothilone D (EpoD)-treated mice, assessed using a standard rotarod test, is not significantly different from vehicle-treated cohorts. Finally, although there is minor group-to-group variability, there are no significant differences in white blood cell counts or neutrophil content between any of the treatment cohorts. Thus, the low doses of Epothilone D (EpoD) utilized in these studies appeared to be well tolerated.
埃博霉素 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-15278 | 埃博霉素 | 189453-10-9 | 2mg | 900 |
| 2024-11-08 | HY-15278 | 埃博霉素 | 189453-10-9 | 5mg | 1950 |
