Patupilone (Epothilone B)
别名: EPO906 中文名称：埃博霉素B，帕土匹龙
Patupilone (EPO906, Epothilone B)是一种紫杉醇样microtubule稳定剂，EC0.01为1.8 μM。Phase 2。
Patupilone (Epothilone B) Chemical Structure
CAS: 152044-54-7
产品质控
批次：
纯度：
99.95%
99.95
Patupilone (Epothilone B)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| human NCI-H2009 cell | Growth inhibition assay | Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=0.862 μM | SANGER | ||
| human HT-1080 cell | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=0.842 μM | SANGER | ||
| human A427 cell | Growth inhibition assay | Inhibition of human A427 cell growth in a cell viability assay, IC50=0.828 μM | SANGER | ||
| human ST486 cell | Growth inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50=0.721 μM | SANGER | ||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=0.721 μM | SANGER | ||
| human HCT-15 cell | Growth inhibition assay | Inhibition of human HCT-15 cell growth in a cell viability assay, IC50=0.717 μM | SANGER | ||
| human SW620 cell | Growth inhibition assay | Inhibition of human SW620 cell growth in a cell viability assay, IC50=0.648 μM | SANGER | ||
| human SK-LMS-1 cell | Growth inhibition assay | Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=0.646 μM | SANGER | ||
| human NB13 cell | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50=0.447 μM | SANGER | ||
| human KYSE-270 cell | Growth inhibition assay | Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=0.445 μM | SANGER | ||
| human SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=0.436 μM | SANGER | ||
| human CAL-39 cell | Growth inhibition assay | Inhibition of human CAL-39 cell growth in a cell viability assay, IC50=0.411 μM | SANGER | ||
| human NCI-H2122 cell | Growth inhibition assay | Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=0.41 μM | SANGER | ||
| human COLO-679 cell | Growth inhibition assay | Inhibition of human COLO-679 cell growth in a cell viability assay, IC50=0.394 μM | SANGER | ||
| human HMV-II cell | Growth inhibition assay | Inhibition of human HMV-II cell growth in a cell viability assay, IC50=0.394 μM | SANGER | ||
| human IA-LM cell | Growth inhibition assay | Inhibition of human IA-LM cell growth in a cell viability assay, IC50=0.393 μM | SANGER | ||
| human HSC-2 cell | Growth inhibition assay | Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=0.363 nM | SANGER | ||
| human HGC-27 cell | Growth inhibition assay | Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=0.338 μM | SANGER | ||
| human NCI-H460 cell | Growth inhibition assay | Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=0.333 μM | SANGER | ||
| human HUTU-80 cell | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.328 μM | SANGER | ||
| human NCI-H810 cell | Growth inhibition assay | Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=0.322 μM | SANGER | ||
| human LCLC-103H cell | Growth inhibition assay | Inhibition of human LCLC-103H cell growth in a cell viability assay, IC50=0.31 nM | SANGER | ||
| human KYSE-450 cell | Growth inhibition assay | Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50=0.267 μM | SANGER | ||
| human T84 cell | Growth inhibition assay | Inhibition of human T84 cell growth in a cell viability assay, IC50=0.24 μM | SANGER | ||
| human CAL-12T cell | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=0.239 μM | SANGER | ||
| human LXF-289 cell | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=0.277 μM | SANGER | ||
| human TE-15 cell | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay, IC50=0.225 μM | SANGER | ||
| human ES1 cell | Growth inhibition assay | Inhibition of human ES1 cell growth in a cell viability assay, IC50=0.221 μM | SANGER | ||
| human 639-V cell | Growth inhibition assay | Inhibition of human 639-V cell growth in a cell viability assay, IC50=0.218 μM | SANGER | ||
| human HOS cell | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay, IC50=0.215 μM | SANGER | ||
| human BB30-HNC cell | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=0.201 μM | SANGER | ||
| human BHY cell | Growth inhibition assay | Inhibition of human BHY cell growth in a cell viability assay, IC50=0.195 nM | SANGER | ||
| KB-31 cells | Growth inhibition assay | 72 h | Concentration required to inhibit the growth of human epidermoid carcinoma cells KB-31 by 50 percent (72 hr exposure) | 11133086 | |
| KB-8511 cells | Growth inhibition assay | 72 h | Concentration required to inhibit the growth of human epidermoid carcinoma cells KB-8511 by 50 percent (72 hr exposure), IC50=0.18 μM | 11133086 | |
| human PA-1 cell | Growth inhibition assay | Inhibition of human PA-1 cell growth in a cell viability assay, IC50=0.174 μM | SANGER | ||
| human PSN1 cell | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay, IC50=0.173 μM | SANGER | ||
| human NCI-H650 cell | Growth inhibition assay | Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=0.17 μM | SANGER | ||
| human SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=0.169 μM | SANGER | ||
| human MG-63 cell | Growth inhibition assay | Inhibition of human MG-63 cell growth in a cell viability assay, IC50=0.165 μM | SANGER | ||
| human IGROV-1 cell | Growth inhibition assay | Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=0.156 μM | SANGER | ||
| human VMRC-RCZ cell | Growth inhibition assay | Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.136 μM | SANGER | ||
| human PANC-03-27 cell | Growth inhibition assay | Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50=0.132 μM | SANGER | ||
| ovarian carcinoma 1A9 cell | Growth inhibition assay | Inhibitory concentration against ovarian carcinoma 1A9 cell growth | 16134928 | ||
| human TE-8 cell | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50=0.111 nM | SANGER | ||
| human 786-0 cell | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.11 nM | SANGER | ||
| human MCF7 cell | Growth inhibition assay | Inhibition of human MCF7 cell growth in a cell viability assay, IC50=8.66e-05 μM | SANGER | ||
| human HLE cell | Growth inhibition assay | Inhibition of human HLE cell growth in a cell viability assay, IC50=8.26e-05 μM | SANGER | ||
| human KYSE-510 cell | Growth inhibition assay | Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50=7.38e-05 μM | SANGER | ||
| human RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=6.47e-05 μM | SANGER | ||
| human A375 cell | Growth inhibition assay | Inhibition of human A375 cell growth in a cell viability assay, IC50=5e-05 μM | SANGER | ||
| human BFTC-905 cell | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=4.99e-05 μM | SANGER | ||
| human Daoy cell | Growth inhibition assay | Inhibition of human Daoy cell growth in a cell viability assay， IC50=2.73e-05 μM | SANGER | ||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.14e-05 μM | SANGER | ||
| human A431 cell | Growth inhibition assay | Inhibition of human A431 cell growth in a cell viability assay, IC50=9.86e-06 μM | SANGER | ||
| human LC-2-ad cell | Growth inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=3.77e-06 μM | SANGER | ||
| human LCLC-97TM1 cell | Growth inhibition assay | Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=0.444 μM | SANGER | ||
| human SK-LU-1 cell | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=0.866 μM | SANGER | ||
| human SCC-4 cell | Growth inhibition assay | Inhibition of human SCC-4 cell growth in a cell viability assay, IC50=0.877 μM | SANGER | ||
| human NCI-H1299 cell | Growth inhibition assay | Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=0.88 μM | SANGER | ||
| human NH-12 cell | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50=0.891 μM | SANGER | ||
| human SK-UT-1 cell | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=0.892 μM | SANGER | ||
| human Bel7402 | Proliferation assay | 72 h | Antiproliferative activity against human Bel7402 after 72 hrs by CellTiter Glo assay, IC50=0.9 μM | 22320354 | |
| human A388 cell | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50=0.94 μM | SANGER | ||
| human SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.999 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Patupilone (EPO906, Epothilone B)是一种紫杉醇样microtubule稳定剂，EC0.01为1.8 μM。Phase 2。 | ||
|---|---|---|---|
| 特性 | Epothilone B是类似紫杉醇的抗癌常规化合物，诱导微管蛋白聚合。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Epothilone B 比 Epothilone A活性高。Epothilone B 的EC0.01为1.8 nM。Epothilone B 作用于HCT116细胞，有效抑制细胞增殖，IC50为0.8 nM。[1] Epothilone B 作用于KB3-1, KBV-1, Hela,和 Hs578T细胞，诱导细胞周期停顿，且具有细胞毒性，IC50为3 nM 到92 nM。Epothilone B与紫杉醇竞争性与微管结合,IC50为3.3 μM。[2] 3.5 nM Epothilone B 作用于过量表达GFP-α-微管蛋白的MCF-7细胞， 充分抑制微管动力学。同时，Epothilone B诱导有丝分裂停滞，IC50 为3.5 nM。[3] Epothilone B 作用于多发性骨髓瘤(MM)细胞,包括RPMI 8226, U266, MM.1S, LR5,和 MR20,直接抑制细胞增殖,IC50为1 nM到 10 nM。10 nM Epothilone B也诱导细胞周期停滞和细胞凋亡。 [4]最新研究显示, 5 nM–100 nM Epothilone B作用于卵巢癌 Hey细胞,增强表面上皮细胞粘附抗原(EpCAM)。[5] |
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|---|---|---|---|---|
| 激酶实验 | 微管蛋白聚合实验 | |||
| 纯化牛脑微管蛋白(MTP), 包含约15%–20%微管相关蛋白。用于 Epothilone B-微管研究的buffer (MES buffer)含 0.1 M 2-吗啉乙磺酸(MES), 1 mM EGTA, 0.5 mM MgCl2, 和3 M 甘油，pH 为6.6。电子显微镜观察的样本置于碳覆盖火棉胶片包被的网格上(300 个网孔)，用2%乙酸铀酰进行负染色。在有或无Epothilone B存在时， 使用分光光度计和恒温调节液体循环器。检测微管装配。温度维持在35oC，350 nm处检测到变浑浊状态(代表聚合物规模)。计算EC0.01。 | ||||
| 细胞实验 | 细胞系 | KB3-1, KBV-1, Hela, 和Hs578T细胞 | ||
| 浓度 | 0–1 μM | |||
| 孵育时间 | 24 小时测定有丝分裂停顿,72 小时测定细胞毒性。 | |||
| 方法 | 为了测定有丝分裂受阻和畸变，细胞接种在48孔板中(用台酚蓝染色，测定细胞数)或置于盖玻片上。24小时后,用 Epothilone B处理细胞，在固定时间间隔记录。为了分析毒性, 测定细胞数，用台酚蓝染色记录阳性和阴性。 同时, 盖玻片和培养基上清液中等分的细胞混合，用溶于PBS的Hoechst 33342 染色。在有丝分裂受阻（停在G2-M期）和畸变的时候记录细胞。 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | Epothilone B 按 2.5 mg/kg–4 mg/kg 剂量作用于携带RPMI 8226细胞移植瘤的小鼠，延长小鼠寿命且抑制肿瘤生长。[4]Epothilone B 作用于携带前列腺癌细胞，包括DU145和PC3的移植瘤小鼠，也抑制肿瘤生长。[6] |
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|---|---|---|
| 动物实验 | Animal Models | 携带RPMI 8226 细胞移植瘤的小鼠 |
| Dosages | 2.5 mg/kg–4 mg/kg | |
| Administration | 静脉注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00496600 | Completed | Refractory Malignancy |
University of Medicine and Dentistry of New Jersey|Novartis Pharmaceuticals|National Cancer Institute (NCI)|Rutgers The State University of New Jersey |
July 2007 | Phase 1 |
| NCT00442741 | Withdrawn | Solid Tumors |
Novartis Pharmaceuticals|Novartis |
July 2007 | Phase 1 |
| NCT00468260 | Terminated | Advanced Malignancies |
Novartis Pharmaceuticals|Novartis |
May 2007 | Phase 1 |
| NCT00448396 | Completed | Advanced Malignancies |
Novartis Pharmaceuticals|Novartis |
March 2007 | Phase 1 |
| NCT00426140 | Completed | Advanced Malignancies|Solid Tumors |
Novartis Pharmaceuticals|Novartis |
August 2006 | Phase 1 |
化学信息&溶解度
| 分子量 | 507.68 | 分子式 | C27H41NO6S |
| CAS号 | 152044-54-7 | SDF | Download Patupilone (Epothilone B) SDF |
| Smiles | CC1CCCC2(C(O2)CC(OC(=O)CC(C(C(=O)C(C1O)C)(C)C)O)C(=CC3=CSC(=N3)C)C)C | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 102 mg/mL ( (200.91 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 102 mg/mL (200.91 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
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）
mg/kg
g
μL
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Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
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 ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：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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