EPZ015666 (GSK3235025) Histone Methyltransferase remmer | CAS 1616391-65-1

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Batch: Zuiverheid: >97%

Geciteerd in Nature Medicine voor zijn topkwaliteit
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Datasheet
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Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
NMR
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Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
NMR
Microanalyse

Waarom microanalyse?
Datasheet
SDS

Geciteerd in Nature Medicine voor zijn topkwaliteit
COA
NMR
Microanalyse

Waarom microanalyse?
Datasheet
SDS

97

Gerelateerde doelwitten	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Overige Histone Methyltransferase Inhibitoren	Pinometostat (EPZ5676) 3-Deazaneplanocin A (DZNep) Hydrochloride BIX-01294 trihydrochloride UNC1999 EPZ004777 MM-102 (HMTase Inhibitor IX) Chaetocin SGC 0946 EPZ005687 UNC0638

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Incubatietijd	Activiteitsbeschrijving	PMID
MDA-MB-468	Function assay	48 h	inhibits PRMT5 activity	30957988
HCC1954	Cell viability assay		IC50=0.8 μM	30957988
MDA-MB-453	Cell viability assay		IC50=1 μM	30957988
HCC38	Cell viability assay		IC50=2.2 μM	30957988
MDA-MB-468	Cell viability assay		IC50=2.2 μM	30957988
MCF7	Cell viability assay		IC50=2.6 μM	30957988
SKBR3	Cell viability assay		IC50=3.9 μM	30957988
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [3H]-SAM by Topcount method, IC50=0.022μM	29628326
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [4H]-SAM by Topcount method, IC50=0.022μM	29628326
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [5H]-SAM by Topcount method, IC50=0.022μM	30366617
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [6H]-SAM by Topcount method, IC50=0.022μM	30366617
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [7H]-SAM by Topcount method, IC50=0.047μM	30366617
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [8H]-SAM by Topcount method, IC50=0.047μM	30366617
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [9H]-SAM by Topcount method, IC50=0.047μM	30605830
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [10H]-SAM by Topcount method, IC50=0.047μM	30605830
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [11H]-SAM by Topcount method, IC50=0.047μM	30605830
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [12H]-SAM by Topcount method, IC50=0.047μM	30605830
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [13H]-SAM by Topcount method, IC50=0.096μM	29870258
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [14H]-SAM by Topcount method, GI50=0.106μM	30605830
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [15H]-SAM by Topcount method, GI50=0.106μM	30605830
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [16H]-SAM by Topcount method, GI50=0.212μM	30605830
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [17H]-SAM by Topcount method, GI50=0.212μM	30605830
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [18H]-SAM by Topcount method, IC50=0.45μM	29870258
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [19H]-SAM by Topcount method, IC50=0.96μM	30366617
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [20H]-SAM by Topcount method, IC50=1.1μM	30366617
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [21H]-SAM by Topcount method, IC50=1.8μM	30366617
Sf9	Function assay		Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [22H]-SAM by Topcount method, IC50=2.6μM	30366617
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Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	383.44	Formule	C₂₀H₂₅N₅O₃	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	1616391-65-1	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel

Oplosbaarheid

In vitro
Batch:

DMSO : 77 mg/mL (200.81 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 26 mg/mL

Water : 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.

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	PRMT5 (Cell-free assay) 5 nM(Ki)
In vitro	EPZ015666 vertoont krachtige cellulaire activiteit die de symmetrische dimethylering van SmD3 blokkeert en de proliferatie van MCL-cellijnen (Z-138, Granta-519, Maver-1, Mino en Jeko-1) remt met een IC50 van 96-904 nM.
In vivo	EPZ015666 (200 mg/kg, p.o.) vertoont robuuste antitumoractiviteit in MCL-xenograftdiermodellen.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/25915199/