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别名 埃博霉素 D, Utidelone, UTD1, UTD 1, KOS862, KOS 862
Epothilone D 是一种来源于黏细菌 Sorangium cellulosum 的天然多酮化合物,可与微管蛋白结合并抑制微管解聚,从而阻断有丝分裂、细胞增殖及细胞运动。Epothilone D 广泛用于肿瘤研究,以探索微管动力学、有丝分裂阻滞及细胞骨架靶向的抗癌机制。

Epothilone D 是一种来源于黏细菌 Sorangium cellulosum 的天然多酮化合物,可与微管蛋白结合并抑制微管解聚,从而阻断有丝分裂、细胞增殖及细胞运动。Epothilone D 广泛用于肿瘤研究,以探索微管动力学、有丝分裂阻滞及细胞骨架靶向的抗癌机制。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 497 | 6-8周 | |
| 5 mg | ¥ 1,590 | 现货 |
| 产品描述 | Epothilone D is a natural polyketide compound isolated from the myxobacterium Sorangium cellulosum that binds to tubulin and inhibits microtubule disassembly, thereby blocking mitosis, cellular proliferation, and cell motility, Epothilone D is extensively utilized in cancer research to study microtubule dynamics, mitotic arrest, and cytoskeleton-targeted anticancer mechanisms. |
| 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 | 在模拟阿尔茨海默病特征的 Tauopathy 转基因小鼠模型 (PS19 小鼠) 中,每周腹腔注射 (i.p.) 一次 Epothilone D(1 mg/kg 或 3 mg/kg,持续 3 个月)影响了微管密度和轴突完整性。这些结构变化与处理后小鼠认知指标的改善相关。在这些剂量下,小鼠未表现出体重减轻或中性粒细胞减少,显示出与更高化疗剂量不同的耐受特征 [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 | 埃博霉素 D, Utidelone, UTD1, UTD 1, KOS862, KOS 862 |
| 分子量 | 489.72 |
| 分子式 | C28H43NO4S |
| CAS No. | 189453-10-9 |
| Smiles | CC(C)(C([C@@H]([C@H]([C@H](CCC/C(C)=C/C[C@H](O1)/C(C)=C/C2=CSC(C)=N2)C)C)C)=O)[C@H](CC1=O)O |
| 密度 | 1.084 g/cm3 (Predicted) |
| 存储 | ||||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 80 mg/mL (163.36 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.74 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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对于不同动物的给药剂量换算,您也可以参考 更多