Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ixabepilone (Azaepothilone B) 是一种可口服的微管抑制剂,能够与微管蛋白结合,促进微管蛋白的聚合和微管的稳定,使细胞停滞在 G2-M 期,诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 528 | 现货 | ||
2 mg | ¥ 778 | 现货 | ||
5 mg | ¥ 1,330 | 现货 | ||
10 mg | ¥ 1,990 | 现货 | ||
25 mg | ¥ 3,380 | 现货 | ||
50 mg | ¥ 4,820 | 现货 | ||
100 mg | ¥ 6,680 | 现货 | ||
200 mg | ¥ 8,850 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,480 | 现货 |
产品描述 | Ixabepilone (Azaepothilone B) is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. |
体外活性 | BMS-247550 is a highly potent cytotoxic agent capable of killing cancer cells at low nanomolar concentrations as well as retains its antineoplastic activity against human cancers that are naturally insensitive to paclitaxel or that have developed resistance to paclitaxel[1]. |
体内活性 | In vivo, BMS-247550 has clearly demonstrated antitumor activity that is superior to paclitaxel in both paclitaxel-resistant and -sensitive tumors. BMS-247550 is more efficacious compared to paclitaxel in all five paclitaxel-resistant tumors evaluated in this study (four human and one murine): i.e., 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: i.e., A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma[1]. |
激酶实验 | 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, 1 mM?EGTA, 0.5 mM?MgCl2 (pH 6.6)] are added to tubulin in polymerization buffer at 37°C in microcuvette wells of a Beckman. Model DU 7400 UV spectrophotometer. A final microtubule protein concentration of 1.0 mg/mL and compound concentrations of generally 2.5, 5.0, and 10 μM?are used. Initial slopes of absorbance (A280 nM) change, measured every 10 s, are calculated by the software program accompanying the instrument. |
细胞实验 | HCT116 cells from cultures are collected by trypsinization after 1, 2, 4, 8, 16, and 24 h exposure to 7.5 nm of BMS-247550. Cells are pelleted and fixed in 80% ethanol at −20°C. After an overnight storage at −20°C, cells are rehydrated with PBS buffer and DNA stain by incubation with propidium iodide (5 μg/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. (Only for Reference) |
别名 | BMS 247550, Ixempra, Azaepothilone B, 伊沙匹隆, BMS 247550-1 |
分子量 | 506.7 |
分子式 | C27H42N2O5S |
CAS No. | 219989-84-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 93 mg/mL (183.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (183.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.9736 mL | 9.8678 mL | 19.7355 mL | 49.3389 mL |
5 mM | 0.3947 mL | 1.9736 mL | 3.9471 mL | 9.8678 mL | |
10 mM | 0.1974 mL | 0.9868 mL | 1.9736 mL | 4.9339 mL | |
20 mM | 0.0987 mL | 0.4934 mL | 0.9868 mL | 2.4669 mL | |
50 mM | 0.0395 mL | 0.1974 mL | 0.3947 mL | 0.9868 mL | |
100 mM | 0.0197 mL | 0.0987 mL | 0.1974 mL | 0.4934 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。
Ixabepilone 219989-84-1 Apoptosis Cytoskeletal Signaling Microtubule Associated inhibit BMS247550 Inhibitor Aza-epothilone B BMS 247550 Ixempra Azaepothilone B Microtubule/Tubulin 伊沙匹隆 BMS-247550 BMS 247550-1 inhibitor