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

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Kwaliteitscontrole

Batch: Zuiverheid: 99.94%

99.94

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

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Incubatietijd	Activiteitsbeschrijving
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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	517.4	Formule	C₂₂H₂₉ClN₄O_6.2HCl	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	70476-82-3	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NSC-301739 2HCl, Mitozantrone 2HCl			Smiles	C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl

Oplosbaarheid

In vitro
Batch:

DMSO : 104 mg/mL (201.0 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 104 mg/mL

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	Topoisomerase II PKC (Cell-free assay) 8.5 μM
In vitro	Mitoxantrone induceert DNA-fragmentatie en de proteolytische splitsing van poly(ADP-ribose) polymerase (PARP), een marker van de activering van caspasen, bij alle bestudeerde patiënten, wat aantoont dat het cytotoxische effect van mitoxantrone te wijten is aan inductie van apoptose. Mitoxantrone activeert NFkappaB en stimuleert IkappaBalpha-degradatie in de promyelocytische leukemiecellijn HL60 maar niet in de variantcellen, HL60/MX2-cellen, die de bèta-isoform van topoisomerase II missen en een afgeknotte alfa-isoform tot expressie brengen die resulteert in een veranderde subcellulaire distributie. Mitoxantrone remt de proliferatie van geactiveerde PBMC's, B-lymfocyten of antigeenspecifieke T-cellijnen (TCL's) gestimuleerd op antigeenpresenterende cellen (APC's) op een dosisafhankelijke manier. Mitoxantrone induceert apoptose van PBMC's, monocyten en DC's bij lage concentraties, terwijl hogere doses celdood veroorzaken.
In vivo	Mitoxantrone vermindert tijdelijk de groeisnelheid van HID-xenografts bij muizen, maar beïnvloedt die van PAC120-xenografts niet. Mitoxantrone resulteert in de ernst van de hartlaesies en de nefropathie en de intestinale toxiciteit bij spontaan hypertensieve ratten. Mitoxantrone en ijzer(III) vormen een sterk 2:1-complex, waarin mitoxantrone mogelijk als een tridentaat ligand fungeert.
Referenties	[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/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK		30108778
Growth inhibition assay	Cell number		24349321

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

Technische ondersteuning

Gebruiksaanwijzing

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

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Mitoxantrone Dihydrochloride (NSC 301739) PKC/Topoisomerase II-remmer

Chemische structuur

Moleculair gewicht: 517.4