Name: Mitoxantrone Dihydrochloride (NSC 301739)
Brand: Selleck Chemicals
SKU: S2485
Rating: 5 (57 reviews)

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Contrôle qualité

Lot : Pureté : 99.94%

99.94

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

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Temps dincubation	Description de lactivité
L1210 cell	Cytotoxicity assay	48 h	Cytotoxic potency required to inhibit L1210 cell growth by 50% after cell drug contact for 48 hrs, IC50=4e-05 μM
HL60 cells	Cytotoxicity assay	48 h	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 μM
MDA435/LCC6 cells	Proliferation assay		Antiproliferative activity against MDA435/LCC6 cells by ELISA, IC50=0.35 nM
A2780-cell	Growth inhibition assay		Concentration required to inhibit A2780-cell growth by 50%, IC50=0.55 nM
G-361 cell	Growth inhibition assay		Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM
human HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay, IC50=2.5 nM
human K562 cells	Cytotoxicity assay	5 days	Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=2.6 nM
CH1 cell	Cytotoxicity assay		Cytotoxic potency required to inhibit CH1 cell growth by 50%, IC50=2.65 nM
MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against MES-SA cells by MTT assay after 72 hrs, IC50=3 nM
A549 cells	Function assay		Activity against A549 cancer cell line, IC50=3.1 nM
LoVo cells	Cytotoxicity assay	144 h	Cytotoxicity against human LoVo cancer cell line was determined after 144 hr, IC50=3.3 nM
P388 cells	Proliferation assay		Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM
human Daudi cells	Proliferation assay	72 h	Antiproliferative activity against human Daudi cells after 72 hrs by MTT assay, IC50=5 nM
SKOV-3 cell	Cytotoxicity assay		Cytotoxic potency required to inhibit SKOV-3 cell growth 50%, IC50=5.3 nM
OVCAR-3 cell	Function assay		Antitumor activity against human ovarian OVCAR-3 cell lines, IC50=5.8 nM
human MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against human MES-SA cells after 72 hrs by MTT assay, IC50=6 nM
PC3 cancer cell	Cytotoxicity assay	144 h	Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM
MXF7 breast cell	Function assay		Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM
HT-29 cell	Cytotoxicity assay	144 h	Cytotoxic potency required to inhibit HT-29 cell growth by 50% after cell drug contact for 144 hrs, IC5=0.01 μM
HEK293 cells	Cytotoxicity assay	72 h	Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM
MKN45 cells	Cytotoxicity assay	144 h	Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM
MES-SA cells	Cytotoxicity assay	72 h	Cytotoxicity against human MES-SA cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.012 μM
FM3 cells	Proliferation assay	72 h	Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM
MCF-7 cells	Growth inhibition assay		Inhibitory activity against human tumor cell line MCF-7 breast adenocarcinoma, IC50=0.02 μM
human small-cell lung cancer	Cytotoxicity assay		Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM
human HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.022 μM
human HCT116 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.025 μM
NCI-H460 cells	Cytotoxicity assay	48 h	Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM
CCRF-CEM cells	Cytotoxicity assay	48 h	Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.036 μM
HeLa cells	Proliferation assay	72 h	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM
NCI60 cells	Function assay	48 h	Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=47.86 nM
UACC375 cell	Function assay		Antitumor activity against human melanoma UACC375 cell line, IC50=0.048 μM
HT1080 cell	Growth inhibition assay		Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM
MES-SA/Dx5 cells	Proliferation assay	72 h	Antiproliferative activity against human MES-SA/Dx5 cells after 72 hrs by MTT assay, IC50=0.073 μM
SF268 cells	Proliferation assay	48 h	Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM
KB/HeLa cells	Proliferation assay	48 h	Antiproliferative activity against human KB/HeLa cells after 48 hrs, EC50=0.36 μM
K562 cells	Growth inhibition assay	72 h	Growth inhibition of human K562 cells after 72 hrs by MTS method, IC50=0.42 μM
MDA-MB-231 cells	Proliferation assay	72 h	Antiproliferative activity against human MDA-MB-231 cells by WST-1 method after 72 hrs, IC50=0.96 μM
SF268 cells	Cytotoxicity assay	48 h	Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50=0.97 μM
HCT116 cells	Cytotoxicity assay		Cytotoxicity against human HCT116 cells by MTT assay, IC50=3.96 μM
U937 cells	Cytotoxicity assay		Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM
HepG2 cells	Proliferation assay	48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=11.05 μM
Cliquez pour voir plus de données expérimentales sur les lignées cellulaires

Informations chimiques, stockage et stabilité

Poids moléculaire	517.4	Formule	C₂₂H₂₉ClN₄O_6.2HCl	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	70476-82-3	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	NSC-301739 2HCl, Mitozantrone 2HCl			Smiles	C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl

Solubilité

In vitro
Lot:

DMSO : 104 mg/mL (201.0 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : 104 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.
Clear solution	Saline Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	30.000mg/ml (57.98mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

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

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny 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 dabord 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, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

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

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	Topoisomerase II PKC (Cell-free assay) 8.5 μM
In vitro	La mitoxantrone induit la fragmentation de l'ADN et le clivage protéolytique de la poly(ADP-ribose) polymérase (PARP), un marqueur de l'activation des caspases, chez tous les patients étudiés, démontrant que l'effet cytotoxique de la mitoxantrone est dû à l'induction de l'apoptose. La mitoxantrone active NFkappaB et stimule la dégradation de l'IkappaBalpha dans la lignée cellulaire de leucémie promyélocytaire HL60 mais pas dans les cellules variantes, les cellules HL60/MX2, qui n'ont pas l'isoforme bêta de la topoisomerase II et expriment une isoforme alpha tronquée qui entraîne une distribution subcellulaire altérée. La mitoxantrone inhibe la prolifération des PBMC activées, des lymphocytes B ou des lignées cellulaires T (TCL) spécifiques de l'antigène stimulées sur des cellules présentatrices d'antigène (APC) de manière dose-dépendante. La mitoxantrone induit l'apoptose des PBMC, des monocytes et des DC à de faibles concentrations, tandis que des doses plus élevées provoquent la lyse cellulaire.
In vivo	La mitoxantrone diminue transitoirement le taux de croissance des xénogreffes HID chez les souris mais n'affecte pas celui des xénogreffes PAC120. La mitoxantrone entraîne la gravité des lésions cardiaques, de la néphropathie et de la toxicité intestinale chez les rats spontanément hypertendus. La mitoxantrone et le fer(III) forment un complexe fort 2:1, dans lequel la mitoxantrone peut agir comme un ligand tridentate.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/10328583/ [2] https://pubmed.ncbi.nlm.nih.gov/2476134/ [3] https://pubmed.ncbi.nlm.nih.gov/2287944/ [4] https://pubmed.ncbi.nlm.nih.gov/2476134/ [5] https://pubmed.ncbi.nlm.nih.gov/9664073/ [6] https://pubmed.ncbi.nlm.nih.gov/8254024/ [7] https://pubmed.ncbi.nlm.nih.gov/1295884/

Applications

Méthodes	Biomarqueurs	Images	PMID
Western blot	p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK		30108778
Growth inhibition assay	Cell number		24349321

Informations sur lessai clinique

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

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	Phases
NCT06156761	Not yet recruiting	Breast Cancer	Cancer Institute and Hospital Chinese Academy of Medical Sciences\|CSPC Ouyi Pharmaceutical Co. Ltd.	November 28 2023	Not Applicable
NCT05875428	Recruiting	Diffuse Large B-Cell Lymphoma	CSPC ZhongQi Pharmaceutical Technology Co. Ltd.	July 10 2023	Phase 2
NCT05496894	Withdrawn	Relapsing Multiple Sclerosis	CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co. Ltd.	August 2022	Phase 2

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

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):

Mitoxantrone Dihydrochloride (NSC 301739) inhibiteur de PKC/Topoisomerase II

Structure chimique

Poids moléculaire: 517.4