Ixabepilone
(Synonyms: 伊沙匹隆; BMS-247550; Aza-epothilone B) 目录号 : GC16869
A broad-spectrum anticancer agent
Cas No.:219989-84-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | 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. |
Cell experiment: | 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. |
References: [1]. John T. Hunt Discovery of Ixabepilone. Mol Cancer Ther February 2009 8; 275 | |
Ixabepilone(BMS-247550), an epothilone B analog, is an orally bioavailable microtubule inhibitor [1]. It could bind to tubulin and promote tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis[2].
In vitro: In a large panel of tumor cell lines, BMS-247550 was as active as epothilone B in inducing cytotoxicity. Of the 21 cells lines tested, the IC50 values were in the range of 1.4–34.5 nm. BMS-247550 almost completely blocked cells in mitosis as early as 8 h after the initiation of drug exposureat a concentration close to the IC90 (7.5 nm, clonogenic cytotoxicity assay) [2].
In vivo: BMS-247550 has clearly demonstrated antitumor activity that is superior to paclitaxel in both paclitaxel-sensitive and -resistant tumors. BMS-247550 was more efficacious than paclitaxel in all five paclitaxel-resistant tumors such as 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. BMS-247550 produced antitumor activity equivalent to paclitaxel against three paclitaxel-sensitive human tumor xenografts such as A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma [2].
Clinical trials:Numerous phase I trials have evaluated the optimum dose and toxicity associated with ixabepilone. Various phase II studies were designed for patients with varying levels of previous therapies based on ample evidence of response and safety in early trials such as patients with taxane-refractory breast cancer, taxane-naive patients, both taxane-naive and taxane-refractory patients, taxane refractory patients[3].
References:
[1]. Lee FY1, Borzilleri R,Fairchild CR, Kim SH, Long BH, Reventos-Suarez C, Vite GD, Rose WC, Kramer RA.BMS-247550: a novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy. Clin Cancer Res.2001 May;7(5):1429-37
[2]. Denduluri N, Low J A, Lee J J, et al. Phase II trial of ixabepilone, an epothilone B analog, in patients with metastatic breast cancer previously untreated with taxanes[J]. Journal of clinical oncology, 2007, 25(23): 3421-3427.
[3]. Shannon Puhalla, Adam Brufsky. Ixabepilone: a new chemotherapeutic option for refractory metastatic breast cancer. Biologics. 2008 Sep; 2(3): 505–515.
| Cas No. | 219989-84-1 | SDF | |
| 别名 | 伊沙匹隆; BMS-247550; Aza-epothilone B | ||
| 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 | ||
| Canonical SMILES | CC1CCCC2(C(O2)CC(NC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C | ||
| 分子式 | C27H42N2O5S | 分子量 | 506.7 |
| 溶解度 | ≥ 22.25 mg/mL in DMSO, ≥ 41.3 mg/mL in EtOH with gentle warming | 储存条件 | 4°C, protect from light |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9736 mL | 9.8678 mL | 19.7355 mL |
| 5 mM | 0.3947 mL | 1.9736 mL | 3.9471 mL |
| 10 mM | 0.1974 mL | 0.9868 mL | 1.9736 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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