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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
CAS: 56390-09-1
相關(guān)靶點 | Topo I Topo II Topo IV | 點擊展開 |
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相關(guān)產(chǎn)品 | (S)-10-Hydroxycamptothecin Beta-Lapachone Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Genz-644282 Hydroxy Camptothecine Rubitecan | 點擊展開 |
相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 凋亡分子化合物庫 DNA損傷/ DNA修復(fù)化合物庫 細胞周期化合物庫 | 點擊展開 |
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 | ||
點擊查看更多細胞系數(shù)據(jù) |
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。 | |
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靶點 |
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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] |
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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。 |
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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 |
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22802261 | |
Growth inhibition assay | Cell death |
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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] |
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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 |
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 |
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 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 |
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)
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)
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,注: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:取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:取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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