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Epirubicin HCl Topoisomerase Inhibiteur

Name: Epirubicin HCl
Brand: Selleck Chemicals
SKU: S1223
Rating: 5 (49 reviews)

Réf. Catalogue: S1223

Epirubicin HCl, un dérivé semisynthétique L-arabino de la doxorubicine, est un agent antinéoplasique qui inhibe Topoisomerase. L'épirubicine induit l'apoptose.

Epirubicin HCl Topoisomerase Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 579.98

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.95%

99.95

Cibles apparentées	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Autre Topoisomerase Inhibiteurs	Camptothecin (CPT) Betulinic acid (S)-10-Hydroxycamptothecin Beta-Lapachone Ellagic acid Amonafide Voreloxin (SNS-595) hydrochloride Hydroxy Camptothecine Cu(II)-Elesclomol 7-Ethylcamptothecin

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Description de l'activité	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
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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	579.98	Formule	C₂₇H₂₉NO₁₁.HCl	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	56390-09-1	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	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

Solubilité (Solubility)

In vitro
Lot:

DMSO : 100 mg/mL (172.41 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : 100 mg/mL

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (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 %.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/3005521/ [2] https://pubmed.ncbi.nlm.nih.gov/15520498/ [3] https://pubmed.ncbi.nlm.nih.gov/8353070/ [4] https://pubmed.ncbi.nlm.nih.gov/9821299/

Applications (Applications)

Méthodes	Biomarqueurs	Images	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		28339028
Growth inhibition assay	Cell death		24158003

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):