| 中文名称: | 伊沙匹隆 | ||||
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| 英文名称: | Ixabepilone | ||||
| 别名: | 伊沙匹隆;依沙匹隆 BMS-247550; Aza-epothilone B | ||||
| CAS No: | 219989-84-1 | 分子式: | C27H42N2O5S | 分子量: | 506.7 |
| CAS No: | 219989-84-1 | ||||
| 分子式: | C27H42N2O5S | ||||
| 分子量: | 506.7 | ||||
基本信息
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产品编号：I10255 |
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产品名称：Ixabepilone |
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CAS: |
219989-84-1 |
储存条件 |
粉末 |
2-8℃ 避光 |
四年 |
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分子式： |
溶于液体 |
-80℃(避光) |
六个月 |
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分子量： |
506.70 |
-20℃(避光) |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
100mg/mL (197.35mM) |
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Ethanol |
47mg/mL (92.75mM) |
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Water |
Insoluble |
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体内（现配现用） |
2% DMSO+30% PEG 300+2% Tween 80+ddH2O |
7mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.9736mL |
9.8678mL |
19.7355mL |
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5mM |
0.3947mL |
1.9736mL |
3.9471mL |
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10mM |
0.1974mL |
0.9868mL |
1.9736mL |
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50mM |
0.0395mL |
0.1974mL |
0.3947mL |
生物活性
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产品描述 |
一种可口服的 microtubule抑制剂，能够与微管蛋白结合，促进微管蛋白的聚合和微管的稳定，因此使细胞停滞在 G2-M 期，诱导细胞凋亡。 |
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靶点/IC50 |
microtubule(tubulin stabilising) |
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体外研究 |
BMS-247550 is a highly potent cytotoxic agent capable of killing cancer cells at low nanomolar concentrations and retains its antineoplastic activity against human cancers that are naturally insensitive to paclitaxel or that have developed resistance to paclitaxel. |
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体内研究 |
BMS-247550 demonstrates antitumor activity that is superior to paclitaxel in both paclitaxel-resistant and -sensitive tumors.BMS-247550 is more efficacious than paclitaxel in all five paclitaxel-resistant tumors evaluated in this study (four human and one murine): the clinically derived paclitaxel resistant Pat-7 ovarian carcinoma, the A2780Tax ovarian carcinoma that is resistant to paclitaxel because of tubulin mutations, the HCT116/VM46 MDR colon carcinoma, the clinically derived paclitaxel-resistant Pat-21 breast carcinoma, and the murine fibrosarcoma M5076.Against three paclitaxel-sensitive human tumor xenografts, BMS-247550 produces antitumor activity equivalent to paclitaxel: A2780 human ovarian carcinoma,HCT116, and LS174T human colon carcinoma. |
推荐实验方法(仅供参考)
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激酶实验： |
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The potency with which BMS-247550 and paclitaxel polymerize tubulin isolated from calf brain is evaluated by Published techniques. Briefly, different concentrations of paclitaxel or BMS-247550 in polymerization buffer [0.1 M mes, 1mM EGTA,0.5mM MgCl2 (pH 6.6)] are added to tubulin in polymerization buffer at 37℃ in microcuvette wells of a Beckman. Model DU 7400 UV spectrophotometer. A final microtubule protein concentration of 1.0mg/mL and compound concentrations of generally 2.5, 5.0, and 10μM are used. Initial slopes of absorbance (A280nM) change, measured every 10 s, are calculated by the software program accompanying the instrument. |
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细胞实验: |
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HCT116 cells from cultures are collected by trypsinization after 1, 2, 4, 8, 16, and 24h exposure to 7.5nm of BMS-247550.Cells are pelleted and fixed in 80% ethanol at −20℃. After an overnight storage at −20℃, cells are rehydrated with PBS buffer and DNA stain by incubation with propidium iodide (5μg/mL) in 0.1% RNase for 15-30 min. Fluorescence-activated cell sorter acquisition is performed using the FACS Calibur instrument and analysis is done using Cellquest and Modfit software. |
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动物实验: |
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动物模型 |
人类肿瘤异种移植模型（BALB/c nu/nu 裸鼠） |
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剂量 |
不同的浓度 |
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给药处理 |
静脉注射或口服 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
