Epirubicin HCl
别名: IMI 28 HCl, NSC 256942 HCl, 4'-epidoxorubicin HCl 中文名称：盐酸表阿霉素,表柔比星
Epirubicin HCl是阿霉素的半合成L-阿拉伯糖衍生物，通过抑制拓扑异构酶而具有抗肿瘤作用。Epirubicin 可诱导凋亡。
Epirubicin HCl Chemical Structure
CAS: 56390-09-1
客户使用Selleck的Epirubicin HCl发表文献36篇
产品质控
批次：
纯度：
99.82%
99.82
Epirubicin HCl相关产品
相关信号通路图
Topoisomerase抑制剂选择性比较
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 |
|---|---|---|---|---|---|
| MDA-MB-231 | Cytotoxicity assay | 5 uM | 48 hrs | Cytotoxicity against drug-resistant human MDA-MB-231 cells assessed as change in cell viability at 5 uM after 48 hrs by MTT assay | 23287057 |
| T47D | Cytotoxicity assay | 5 uM | 48 hrs | Cytotoxicity against human T47D cells assessed as change in cell viability at 5 uM after 48 hrs by MTT assay | 23287057 |
| MCF7 | Cytotoxicity assay | 5 uM | 48 hrs | Cytotoxicity against human MCF7 cells assessed as change in cell viability at 5 uM after 48 hrs by MTT assay | 23287057 |
| SGC7901 | Function assay | 1 and 10 uM | 24 to 72 hrs | Induction of morphological changes in human SGC7901 cells assessed as induction of cell break at 1 and 10 uM after 24 to 72 hrs by inverted microscopic analysis | 29903662 |
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.37μM. | 28119026 | |
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.32μM. | 28119026 | |
| MDA-MB-435 | Cytotoxicity assay | 72 hrs | Cytotoxicity in human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.26μM. | 31251621 | |
| MDA-MB-435 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.26μM. | 28119026 | |
| MCF10A | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF10A cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.13μM. | 28119026 | |
| NCI-H460 | Cytotoxicity assay | 72 hrs | Cytotoxicity in human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.12μM. | 31251621 | |
| NCI-H460 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.12μM. | 28119026 | |
| MCF10A | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF10A cells after 48 hrs by MTT assay, IC50=0.1μM. | 29767975 | |
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=0.1μM. | 29767975 | |
| NCI-H460 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NCI-H460 cells after 48 hrs by MTT assay, IC50=0.02μM. | 29767975 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity in human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.37μM. | 31251621 | |
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay, IC50=0.4μM. | 29767975 | |
| HeLa | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 72 hrs by MTS assay, IC50=0.42μM. | 27560695 | |
| PC3 | Cytotoxicity assay | 6 days | Cytotoxicity against human PC3 cells after 6 days by MTT assay, IC50=0.46μM. | 22276679 | |
| HEK293T | Cytotoxicity assay | 72 hrs | Cytotoxicity against HEK293T cells assessed as decrease in cell viability after 72 hrs by MTS assay, IC50=0.47μM. | 27560695 | |
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTS assay, IC50=0.63μM. | 27560695 | |
| MDA-MB-435 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-435 cells after 48 hrs by MTT assay, IC50=0.7μM. | 29767975 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTS assay, IC50=0.71μM. | 27560695 | |
| HCT116 | Cytotoxicity assay | 6 days | Cytotoxicity against human HCT116 cells after 6 days by MTT assay, IC50=0.82μM. | 22276679 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=0.9μM. | 29767975 | |
| Hep3B | Cytotoxicity assay | 6 days | Cytotoxicity against human Hep3B cells after 6 days by MTT assay, IC50=0.96μM. | 22276679 | |
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTS assay, IC50=1.3μM. | 27560695 | |
| HepG2 | Cytotoxicity assay | 6 days | Cytotoxicity against human HepG2 cells after 6 days by MTT assay, IC50=1.65μM. | 22276679 | |
| SNB19 | Cytotoxicity assay | 72 hrs | Cytotoxicity in human SNB19 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=2.3μM. | 31251621 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50=3.7μM. | 23287057 | |
| NIH/3T3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse NIH/3T3 cells after 48 hrs by MTT assay, IC50=4.2μM. | 23287057 | |
| T47D | Antiproliferative assay | 48 hrs | Antiproliferative activity against human T47D cells after 48 hrs by MTT assay, IC50=4.3μM. | 23287057 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=4.6μM. | 23287057 | |
| SGC7901 | Anticancer assay | 72 hrs | Anticancer activity against human SGC7901 cells after 72 hrs by MTT assay, IC50=5.16μM. | 29903662 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50=5.6μM. | 23287057 | |
| MDA-MB-231 | Cytotoxicity assay | 72 hrs | Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=5.6μM. | 31251621 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50=5.7μM. | 23287057 | |
| PC3 | Cytotoxicity assay | 72 hrs | Cytotoxicity in human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=5.7μM. | 31251621 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=9.6μM. | 23287057 | |
| DU145 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay, IC50=9.9μM. | 23287057 | |
| C6 | Cell cycle assay | 24 hrs | Cell cycle arrest in rat C6 cells assessed as increase in cell population at sub G0 phase measured after 24 hrs by propidium iodide staining based flow cytometry analysis | 31447082 | |
| C6 | Cell cycle assay | 24 hrs | Cell cycle arrest in rat C6 cells assessed as decrease in cell population at G2/M phase measured after 24 hrs by propidium iodide staining based flow cytometry analysis | 31447082 | |
| C6 | Cell cycle assay | 24 hrs | Cell cycle arrest in rat C6 cells assessed as decrease in cell population at S phase measured after 24 hrs by propidium iodide staining based flow cytometry analysis | 31447082 | |
| MCF-7 | Function assay | Compound was tested for its toxicity against human breast cancer cells(MCF-7), IC50=0.2μM. | 9548820 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells | 29435139 | ||
| Daoy | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Epirubicin HCl是阿霉素的半合成L-阿拉伯糖衍生物，通过抑制拓扑异构酶而具有抗肿瘤作用。Epirubicin 可诱导凋亡。 | |
|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Epirubicin，与doxorubicin一样，通过与DNA形成复合物而发挥抗肿瘤作用，它会损伤DNA，干扰DNA，RNA以及蛋白质的合成。Epirubicin可能也影响细胞膜的完整性和活性。Epirubicin引起的最大细胞死亡发生在细胞周期的S期。更高浓度下的作用也可见于早期G2以及G1和M期。[1] Epirubicin对大多数癌细胞表现出抗肿瘤活性。Epirubicin对肝癌G2期细胞具有细胞毒性，在24小时时，IC50为1.6 微克/毫升。1.6 微克/毫升 Epirubicin引起Hep G2细胞凋亡，使过氧化氢酶活性增加50%，Se-依赖性谷胱甘肽过氧化物酶活性增加110%，Cu, Zn-超氧化物歧化酶活性增加172%,Mn-超氧化物歧化酶活性增加135%。Epirbicin增加NADPH-CYP 450还原酶在细胞中的表达，并减少GST-π的表达。[2] |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | 人类肝肿瘤细胞Hep G2 | ||
| 浓度 | 0.05-12微克/毫升 | |||
| 孵育时间 | 1天 | |||
| 方法 | Hep G2细胞（500细胞/孔，单层）接种于96孔板中。第二天细胞在培养基中用Epirubicin处理。在培养期结束时，加入15%体积的MTT染液。在37℃下培养1小时后，每孔中加入等体积的增溶/终止溶液(dimethylsul-foxide)，再培养1小时。记录反应液在570 nm下的吸光度。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | PARP / E2F1 / p-E2F1 / p-MK2 / p-Chk2 E2F1 / p-p53 / p53 / Caspase-7 FOXM1 / Cyclin B1 / PLK HIF-1α / GLUT1 / PDK1 |
|
22802261 | |
| Growth inhibition assay | Cell death |
|
24158003 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
Epirubicin对很多类型的肿瘤，包括乳腺癌，恶性淋巴瘤，软组织肉瘤，肺癌，胸膜间皮瘤，胃肠癌，头颈癌，卵巢癌，前列腺癌，移行膀胱癌等都具有临床活性。[3] Epirubicin在3.5毫克/千克剂量下，抑制74.4 %人类乳腺肿瘤异种移植的R-27的肿瘤块。[4] |
|
|---|---|---|
| 动物实验 | Animal Models | 人类乳腺异种瘤 R-27 |
| Dosages | 3.5毫克/千克 | |
| Administration | i.v.每4天3次 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05128617 | Completed | Breast Cancer |
Institut de cancérologie Strasbourg Europe|Université de Strasbourg - Unité de Recherche 3072 - Mitochondries Stress oxydant Protection musculaire |
November 4 2021 | -- |
| NCT01740271 | Recruiting | Breast Neoplasms |
AHS Cancer Control Alberta |
December 2012 | Phase 2 |
化学信息&溶解度
| 分子量 | 579.98 | 分子式 | C27H29NO11.HCl |
| CAS号 | 56390-09-1 | SDF | Download Epirubicin HCl SDF |
| Smiles | CC1C(C(CC(O1)OC2CC(CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(C(=O)CO)O)N)O.Cl | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (172.41 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 100 mg/mL Ethanol : Insoluble |
摩尔浓度计算器 |
|
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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