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

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Lot : Pureté: >97%

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NMR
Microanalyse

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NMR
Microanalyse

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97

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

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Temps dincubation	Description de lactivité	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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Informations chimiques, stockage et stabilité

Poids moléculaire	383.44	Formule	C₂₀H₂₅N₅O₃	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	1616391-65-1	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant

Solubilité

In vitro
Lot:

DMSO : 77 mg/mL (200.81 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 26 mg/mL

Water : 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.

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	PRMT5 (Cell-free assay) 5 nM(Ki)
In vitro	EPZ015666 montre une activité cellulaire puissante qui bloque la diméthylation symétrique de SmD3 et inhibe la prolifération des lignées cellulaires MCL (Z-138, Granta-519, Maver-1, Mino et Jeko-1) avec une IC50 de 96-904 nM.
In vivo	EPZ015666 (200 mg/kg, p.o.) présente une activité anti-tumorale robuste dans les modèles animaux de xénogreffe MCL.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/25915199/