化学信息：
| 化学名 | (1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione |
|
| 简称 | Ixabepilone | |
| 别名 |
Azaepothilone B, BMS 247550, BMS-247550, BMS247550 |
|
| 中文名 | 伊沙匹隆 | |
| 化学式 | C27H42N2O5S | |
| 分子量 | 506.7 | |
| CAS号 | 219989-84-1 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO100mg/ml; Ethanol100mg/ml |
|
| 溶液配制 | 5mg加入0.99ml DMSO，或者每5.07mg加入1ml DMSO，配制成10mM溶液。SC7988-10mM用DMSO配制。 |
生物信息：
| 产品描述 | Ixabepilone 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. | ||||
| 信号通路 | Cytoskeletal Signaling | ||||
| 靶点 | Microtubule(tubulin stabilising) | － | － | － | － |
| IC50 | － | － | － | － | － |
| 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. | ||||
| 体内研究 | 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 than 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. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | HCT116 human carcinoma cell lines |
| 浓度 | 7.5nM |
| 处理时间 | 1, 2, 4, 8, 16, and 24h |
| 方法 | 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. |
| 动物实验 | |
| 动物模型 | Human tumor xenografts (BALB/c nu/nu nude mice) |
| 配制 | (a) ethanol:water (1:9, v/v), (b) Cremophor:ethanol:water (1:1:8, v/v) or (c)0.25M sodium phosphate buffer (pH 8.0) at a ratio of 30:70, v/v. |
| 剂量 | various concentrations |
| 给药方式 | i.v. or p.o. |
| 产品编号 | 产品名称 | 包装 |
| SC7988-10mM | Ixabepilone (Microtubule Associated抑制剂) | 10mM×0.2ml |
| SC7988-5mg | Ixabepilone (Microtubule Associated抑制剂) | 5mg |
| SC7988-25mg | Ixabepilone (Microtubule Associated抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
