Name: Menadione (Vitamin K3)
Brand: Selleck Chemicals
SKU: S1949
Rating: 5 (9 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.88%

99.88

Gerelateerde doelwitten	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase
Overig phosphatase Inhibitoren	Osunprotafib (ABBV-CLS-484) SHP099 Hydrochloride RMC-4550 SHP099 Batoprotafib (TNO155) GSK2830371 β-Glycerophosphate sodium salt hydrate NSC87877 TPI-1 Suramin sodium salt

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving
HT22 cells	Function assay			Neuroprotective activity in mouse HT22 cells assessed as prevention from glutamate-induced oxidative cell death by MTS assay, PD50=0.797 μM
HeLa cell	Cytotoxicity assay			Cytotoxicity against HeLa cell lines, EC50=3.7 μM
PaCa2 cell	Proliferation assay			Antiproliferative activity against human pancreatic carcinoma Mia PaCa2 cell line by colorimetric assay, IC50=6.2 μM
HT-29 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=9.69 μM
DU145 cells	Cytotoxicity assay		72 h	Cytotoxicity against human DU145 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=9.86 μM
MDA-MB-231 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTS assay, IC50=12.68 μM
human A2058 cells	Cytotoxicity assay			Cytotoxicity against human A2058 cells assessed as inhibition of formazan formation at day 5 by measuring absorbance at 430 nm, IC50=13.4 μM
SAS cells	Cytotoxicity assay		48 h	Cytotoxicity against human SAS cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=14 μM
HaCaT cells	Function assay		48 h	Antihyperproliferative activity against human HaCaT cells assessed as inhibition of cell growth after 48 hrs by phase contrast microscopy, IC50=15.8 μM
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=18 μM
CRL2796 cells	Cytotoxicity assay			Cytotoxicity against human CRL2796 cells assessed as inhibition of formazan formation at day 4 by measuring absorbance at 430 nm, IC50=21 μM
HL60 cells	Function assay	50 μM		Induction of necrosis in intact human HL60 cells assessed as cytosolic LDH release at 50 uM
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	172.18	Formule	C₁₁H₈O₂	Opslag (vanaf de datum van ontvangst)	3 years-20°C(in the dark) powder
CAS-nr.	58-27-5	SDF downloaden		Opslag van stamoplossingen	Oplossingen zijn instabiel. Bereid ze vers of koop kleine, voorverpakte formaten. Herverpakken na ontvangst.
Synoniemen	NSC 4170			Smiles	CC1=CC(=O)C2=CC=CC=C2C1=O

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 34 mg/mL (197.46 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 34 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.700mg/ml (9.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 34 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.700mg/ml (9.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 34 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met 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 de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

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

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

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. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	Cdc25 phosphatase DNA polymerase γ
In vitro	Menadione (Vitamin K3) prevents mitochondrial Ca(2+) uptake in normal pancreatic acinar cells, which permits rapid spread of Ca(2+) throughout the cell. Its-induced mitochondrial depolarisation is due to induction of the permeability transition pore. At nontoxic concentration, this compound results in a brief activation of extracellular signal-regulated kinase (ERK) and c-Jun N-terminal kinase (JNK) in the RALA255-10G rat hepatocyte cell line. It is equipotent against multidrug-resistant and parental leukemia cell lines with IC50 values of 13.5 mM and 18 mM, respectively. The compound inhibits the incorporation of radioactive thymidine, uridine and amino acids into DNA, RNA and protein, respectively, in three humancancer cell lines. At 1-20 mM, it dose- and time-dependently inhibits cell proliferation of AR4-2J cells. A concentration of 100 mM causes rapid cell death. This level (100 mM) induces DNA smear in electrophoresis indicative of necrosis, while lower concentrations (10-20 mM) induces a DNA ladder indicative of apoptosis. Concentrations of 1-20 mM induce wild-type P53, whereas 100 mM has a minor effect on wild-type P53. Treatment with it clearly affects the mitochondrial function of Jurkat T cells by inducing a collapse of the inner transmembrane potential (DeltaPsi(m)) and a decrease in inner membrane mass, which could be completely reversed by N-acetylcysteine.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/11861756/ [2] https://pubmed.ncbi.nlm.nih.gov/12774020/ [3] https://pubmed.ncbi.nlm.nih.gov/2018560/ [4] https://pubmed.ncbi.nlm.nih.gov/9378363/ [5] https://pubmed.ncbi.nlm.nih.gov/11726226/ [6] http://www.sciencedirect.com/science/article/pii/S0045206896910524 [7] https://pubmed.ncbi.nlm.nih.gov/24520419/

Toepassingen (Applications)

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	p-JNK / JNK / p-c-Jun / c-Jun / p-ERK / ERK Cyclin B1 / CDK1 / CDC25C c-Fos / HO-1		20578144

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2020-01-29)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT04247087	COMPLETED	Coronary Calcification	Instituto Mexicano del Seguro Social	2017-09-07
NCT03547895	COMPLETED	Decompensated Cirrhosis	Zagazig University	2015-06-01
NCT01094444	COMPLETED	Folliculitis	Per Pfeiffer	2010-05	PHASE2
NCT01393821	COMPLETED	Dermatologic Complications; Malignant Neoplasm; Pain	Mayo Clinic	2012-01-23
NCT01094444	Completed	Folliculitis	Per Pfeiffer\|Odense University Hospital	2010-05	Phase 2
NCT00656786	COMPLETED	EGFR Inhibitor-associated Rash	Spectrum Pharmaceuticals, Inc	2008-04-03	PHASE1

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Menadione (Vitamin K3) phosphatase Remmer

Molecuulgewicht: 172.18

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie over klinische proeven (Clinical Trial Information)

Menadione (Vitamin K3) phosphatase Remmer

Molecuulgewicht: 172.18

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie over klinische proeven (Clinical Trial Information)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)