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Epirubicin HCl

別名: IMI 28 HCl, NSC 256942 HCl, 4'-epidoxorubicin HCl 中文名稱:鹽酸表阿霉素,表柔比星

Epirubicin HCl是阿霉素的半合成L-阿拉伯糖衍生物,通過抑制拓撲異構(gòu)酶而具有抗腫瘤作用。Epirubicin 可誘導(dǎo)凋亡。

Epirubicin HCl Chemical Structure

Epirubicin HCl Chemical Structure

CAS: 56390-09-1

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1301.52 現(xiàn)貨
5mg 566.18 現(xiàn)貨
25mg 2207.25 現(xiàn)貨
1g 22219.47 現(xiàn)貨
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Epirubicin HCl相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Epirubicin HCl是阿霉素的半合成L-阿拉伯糖衍生物,通過抑制拓撲異構(gòu)酶而具有抗腫瘤作用。Epirubicin 可誘導(dǎo)凋亡。
靶點
Topoisomerase [1]
(Cell-free assay)
體外研究(In Vitro)
體外研究活性

Epirubicin,與doxorubicin一樣,通過與DNA形成復(fù)合物而發(fā)揮抗腫瘤作用,它會損傷DNA,干擾DNA,RNA以及蛋白質(zhì)的合成。Epirubicin可能也影響細胞膜的完整性和活性。Epirubicin引起的最大細胞死亡發(fā)生在細胞周期的S期。更高濃度下的作用也可見于早期G2以及G1和M期。[1] Epirubicin對大多數(shù)癌細胞表現(xiàn)出抗腫瘤活性。Epirubicin對肝癌G2期細胞具有細胞毒性,在24小時時,IC50為1.6 微克/毫升。1.6 微克/毫升 Epirubicin引起Hep G2細胞凋亡,使過氧化氫酶活性增加50%,Se-依賴性谷胱甘肽過氧化物酶活性增加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還原酶在細胞中的表達,并減少GST-π的表達。[2]

細胞實驗 細胞系 人類肝腫瘤細胞Hep G2
濃度 0.05-12微克/毫升
孵育時間 1天
方法

Hep G2細胞(500細胞/孔,單層)接種于96孔板中。第二天細胞在培養(yǎng)基中用Epirubicin處理。在培養(yǎng)期結(jié)束時,加入15%體積的MTT染液。在37℃下培養(yǎng)1小時后,每孔中加入等體積的增溶/終止溶液(dimethylsul-foxide),再培養(yǎng)1小時。記錄反應(yīng)液在570 nm下的吸光度。

實驗圖片 檢測方法 檢測指標 實驗圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Epirubicin對很多類型的腫瘤,包括乳腺癌,惡性淋巴瘤,軟組織肉瘤,肺癌,胸膜間皮瘤,胃腸癌,頭頸癌,卵巢癌,前列腺癌,移行膀胱癌等都具有臨床活性。[3] Epirubicin在3.5毫克/千克劑量下,抑制74.4 %人類乳腺腫瘤異種移植的R-27的腫瘤塊。[4]

動物實驗 Animal Models 人類乳腺異種瘤 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

化學信息&溶解度

分子量 579.98 分子式

C27H29NO11.HCl

CAS號 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
儲存條件(自收到貨起)

體外溶解度
批次:

DMSO : 100 mg/mL ( (172.41 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO)

Water : 100 mg/mL (172.41 mM)

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次:

現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器(澄清溶液)

第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)

mg/kg g μL

第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果:

工作液濃度: mg/ml;

DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);

體內(nèi)配方配制方法:μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。

體內(nèi)配方配制方法:μL DMSO母液,加入μL Corn oil,混勻澄清。

注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。

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