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Epirubicin HCl Topoisomerase inhibitor

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

N. Cat.: 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

Struttura chimica

Peso molecolare: 579.98

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.95%

99.95

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

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dell'attività	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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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	579.98	Formula	C₂₇H₂₉NO₁₁.HCl	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	56390-09-1	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	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

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 100 mg/mL (172.41 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : 100 mg/mL

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC₅₀/Ki	Topoisomerase (Cell-free assay)
In vitro	L'epirubicina, come la doxorubicina, esercita i suoi effetti antitumorali complessandosi con il DNA, causando danni al DNA e interferendo con la sintesi di DNA, RNA e proteine. L'epirubicina può anche influenzare l'integrità e l'attività delle membrane cellulari. La massima uccisione cellulare causata dall'epirubicina si verifica durante la fase S del ciclo cellulare. A concentrazioni più elevate, gli effetti si osservano anche nella fase G2 precoce, così come nelle fasi G1 e M. L'epirubicina mostra attività antineoplastica contro la maggior parte delle cellule tumorali. L'epirubicina è citotossica per le cellule di epatoma G2 con IC50 di 1,6 μg/mL a 24 ore. 1,6 μg/mL di epirubicina induce l'apoptosi delle cellule Hep G2 e un'attività più elevata della catalasi del 50%, della glutatione perossidasi Se-dipendente del 110%, della Cu, Zn-superossido dismutasi del 172% e della Mn-superossido dismutasi del 135%. L'epirubicina aumenta l'espressione cellulare della NADPH-CYP 450 reduttasi e riduce l'espressione della GST-π.
In vivo	L'epirubicina è clinicamente attiva contro un'ampia gamma di tipi di tumori, inclusi il cancro al seno, i linfomi maligni, i sarcomi dei tessuti molli, il cancro ai polmoni, il mesotelioma pleurico, il cancro gastrointestinale, il cancro della testa e del collo, il cancro ovarico, il carcinoma prostatico, il carcinoma transizionale della vescica e così via. L'epirubicina a una dose di 3,5 mg/kg sopprime la massa tumorale dello xenotrapianto di tumore al seno umano R-27 del 74,4 %.
Riferimenti	[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/

Applicazioni (Applications)

Metodi	Biomarcatori	Immagini	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

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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):