Epothilone B (EPO906, Patupilone)
(Synonyms: 埃博霉素B; EPO 906; Patupilone) 目录号 : GC17240Microtubule stabilizing agent
Cas No.:152044-54-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment [1]: | |
Tubulin polymerization assay |
Calf brain microtubule proteins (MTP) were purified, which included approximately 15% ~ 20% microtubule associated proteins. The buffer (MES buffer) used for the Epothilone B-microtubule studies contained 0.1 M 2-morpholinoethanesulfonic acid (MES), 1 mM EGTA, 0.5 mM MgCl2 and 3 M glycerol at pH 6.6. Samples for electron microscopy were placed on carbon-over-Parlodion-coated grids (300 mesh) and negatively stained with 2% uranyl acetate. Microtubule assembly in the presence or absence of Epothilone B was monitored spectrophotometrically by using a spectrophotometer equipped with a thermostatically regulated liquid circulator. The temperature was held at 35 °C and changes in turbidity (representative of polymer mass) were monitored at 350 nm. |
Cell experiment [2]: | |
Cell lines |
Hs578T and Hela cells |
Preparation method |
The solubility of this compound in DMSO is > 25.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition |
100 nM; 24 hrs |
Applications |
In Hs578T and Hela cells, Epothilone B arrested cells at the G2-M phase, causing cytotoxicity. In Hs578T cells treated with Epothilone B, there was a larger percentage (up to 38%) of cells showing multimininucleation. |
Animal experiment [3]: | |
Animal models |
Mouse xenograft models of RPMI 8226 cells |
Dosage form |
1-time dose at 4 mg/kg or weekly dose at 2.5 mg/kg (given on days 6, 13, 20 and 27); i.v. |
Applications |
In mouse xenograft models of RPMI 8226 cells, Epothilone B (2.5 ~ 4 mg/kg) prolonged survival and inhibited tumor growth. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Regueiro-Ren A1, Borzilleri RM, Zheng X, Kim SH, Johnson JA, Fairchild CR, Lee FY, Long BH, Vite GD. Synthesis and biological activity of novel epothilone aziridines. Org Lett. 2001 Aug 23;3(17):2693-6 [2]. Bollag DM, McQueney PA, Zhu J, Hensens O, Koupal L, Liesch J, Goetz M, Lazarides E, Woods CM. Epothilones, a new class of microtubule-stabilizing agents with a taxol-like mechanism of action. Cancer Res. 1995 Jun 1;55(11):2325-33. [3]. Lin B, Catley L, LeBlanc R, Mitsiades C, Burger R, Tai YT, Podar K, Wartmann M, Chauhan D, Griffin JD, Anderson KC. Patupilone (epothilone B) inhibits growth and survival of multiple myeloma cells in vitro and in vivo. Blood. 2005 Jan 1;105(1):350-7. |
Epothilone B (EPO906, Patupilone) is a naturally occurring microtubule-stabilizing macrolide that was first isolated from the myxobacterium Sorangium cellulosum. The EC0.01 value of Epothilone B is 1.8 nM [1].
Epothilone B exhibits the same mechanism of action as paclitaxel. More importantly, in cell culture, Epothilone B is active against paclitaxel-resistant cell lines that express P-glycoprotein. Furthermore, Epothilone B has better solubility in water than paclitaxel [1].
Epothilone B induced an increase in the level of the intracellular free calcium only during the longer times following the treatment in SKOV-3 cells. Besides, the ovarian cancer cells treated with Epothilone B showed a time course dependent increase in the cytosolic fraction of cytochrome c [2].
References:
[1] Regueiro-Ren A1, Borzilleri RM, Zheng X, Kim SH, Johnson JA, Fairchild CR, Lee FY, Long BH, Vite GD. Synthesis and biological activity of novel epothilone aziridines. Org Lett. 2001 Aug 23;3(17):2693-6.
[2] Rogalska A1, Gajek A2, Marczak A2. Epothilone B induces extrinsic pathway of apoptosis in human SKOV-3 ovarian cancer cells. Toxicol In Vitro. 2014 Jun;28(4):675-83.
Cas No. | 152044-54-7 | SDF | |
别名 | 埃博霉素B; EPO 906; Patupilone | ||
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]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione | ||
Canonical SMILES | CC1CCCC2(C(O2)CC(OC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C | ||
分子式 | C27H41NO6S | 分子量 | 507.68 |
溶解度 | ≥ 25.4mg/mL in DMSO | 储存条件 | Store at -20°C |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.9697 mL | 9.8487 mL | 19.6974 mL |
5 mM | 0.3939 mL | 1.9697 mL | 3.9395 mL |
10 mM | 0.197 mL | 0.9849 mL | 1.9697 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。