Home DNA Damage/DNA Repair Topoisomerase inhibitor Epirubicin HCl

nur für Forschungszwecke

Epirubicin HCl Topoisomerase inhibitor

Kat.-Nr.: S1223

Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.
Epirubicin HCl Topoisomerase inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 579.98

Springe zu

Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.95%
99.95

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
NCI-H460 Cytotoxicity assay 48 hrs Cytotoxicity against human NCI-H460 cells after 48 hrs by MTT assay, IC50=0.02μM. 29767975
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=0.1μM. 29767975
MCF10A Cytotoxicity assay 48 hrs Cytotoxicity against human MCF10A cells after 48 hrs by MTT assay, IC50=0.1μM. 29767975
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
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
MCF10A Cytotoxicity assay 48 hrs Cytotoxicity against human MCF10A cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.13μM. 28119026
MCF-7 Function assay Compound was tested for its toxicity against human breast cancer cells(MCF-7), IC50=0.2μM. 9548820
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
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
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.32μM. 28119026
HCT116 Cytotoxicity assay 48 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.37μM. 28119026
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
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
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
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
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
Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 579.98 Formel

C27H29NO11.HCl

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 56390-09-1 SDF herunterladen Lagerung von Stammlösungen

Synonyme IMI 28 HCl, NSC 256942 HCl, 4'-epidoxorubicin HCl 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

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 100 mg/mL (172.41 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

Targets/IC50/Ki
Topoisomerase
(Cell-free assay)
In vitro

Epirubicin, like doxorubicin, exerts its antitumor effects by complex with DNA, resulting in damage to DNA and interference with the synthesis of DNA, RNA, and proteins. Epirubicin may also affect the integrity and activity of cellular membranes. Maximal cell kill caused by Epirubicin occurs during the S phase of the cell cycle. With higher concentrations effects are also seen in early G2 as well as G1 and M phases. Epirubicin display antineoplastic activity against most cancer cells. Epirubicin is cytotoxic to Hepatoma G2 cells with IC50 of 1.6 μg/mL at 24hr. 1.6 μg/mL Epirubicin induces apoptosis of Hep G2 cells, and higher activity of catalase by 50%, Se-dependent glutathione peroxidase by 110%, Cu, Zn-superoxide dismutase by 172% and Mn-superoxide dismutase by 135%. Epirbicin increases the cellular expression of NADPH-CYP 450 reductase, and reduces GST-π expression.

In vivo

Epirubicin are clinically active against a broad range of tumor types, including breast cancer, malignant lymphomas, soft tissue sarcomas, lung cancer, pleural mesothelioma, gastrointestinal cancer, head and neck cancer, ovarian cancer, prostatic carcinoma, transitional bladder carcinoma and so on. Epirubicin at a dose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by 74.4 %.

Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/9821299/

Anwendungen (Applications)

Methoden Biomarker Bilder PMID
Western blot HIF-1α / GLUT1 / PDK1 FOXM1 / Cyclin B1 / PLK E2F1 / p-p53 / p53 / Caspase-7 PARP / E2F1 / p-E2F1 / p-MK2 / p-Chk2
S1233-WB1
28339028
Growth inhibition assay Cell death
S1233-viability1
24158003

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
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