Ixabepilone (Microtubule Associated抑制剂)
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产品编号 SC7988-5mg
数量
¥ 1336.00
产品包装:
10mM×0.2ml 5mg 25mg
产品简介
使用说明
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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.
参考文献:
1. Lee FY, et al. Clin Cancer Res. 2001, 7(5):1429-1437.
包装清单:
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。

注意事项:
本产品对人体有害,操作时请小心,并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。
使用说明:
1.收到产品后请立即按照说明书推荐的条件保存。使用前可以在2,000-10,000g离心数秒,以使液体或粉末充分沉降至管底后再开盖使用。
2.对于10mM溶液,可直接稀释使用。对于固体,请根据本产品的溶解性及实验目的选择相应溶剂配制成高浓度的储备液(母液)后使用。
3.具体的最佳工作浓度请参考本说明书中的体外、体内研究结果或其它相关文献,或者根据实验目的,以及所培养的特定细胞和组织,通过实验进行摸索和优化。
4.不同实验动物依据体表面积的等效剂量转换表请参考如下网页:http://www.beyotime.com/support/animal-dose.htm
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