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Mocetinostat (MGCD0103) HDAC inhibiteur

Name: Mocetinostat (MGCD0103)
Brand: Selleck Chemicals
SKU: S1122
Rating: 5 (118 reviews)

N° Cat.S1122

Le Mocetinostat (MGCD0103, MG0103) est un puissant inhibiteur de HDAC avec la plus grande puissance pour HDAC1 avec une IC50 de 0,15 μM dans un essai sans cellules, une sélectivité de 2 à 10 fois contre HDAC2, 3 et 11, et aucune activité envers HDAC4, 5, 6, 7 et 8. Mocetinostat (MGCD0103) induit l'apoptosis et l'autophagy. Phase 2.

Mocetinostat (MGCD0103) HDAC inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 396.44

Aller à

Contrôle qualité

Lot : Pureté : 99.93%

99.93

Cibles apparentées	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Autre HDAC Inhibiteurs	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A HCl Tubastatin A Ricolinostat (ACY-1215) PCI-34051

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Formulation	Description de lactivité	PMID
PBMC	Apoptosis Assay	0.5/2/3 μM	24/48 h		induces apoptosis dose and time dependently	20406947
HeLa	Function Assay	10 μM	7 h	DMSO	disrupts normal spindle checkpoint function	20538840
HeLa	Function Assay	10 μM	6/12/24 h	DMSO	induces mitotic accumulation and delayed p21 expression	20538840
HeLa	Function Assay	0.3-10 μM	8 h	DMSO	increases caspase 3 and 7 activation dose dependently	20538840
HeLa	Function Assay	0.3-10 μM	8 h	DMSO	increases acetylated H3 K9 (H3K9Ac) at 10 μM	20538840
DMS114	Growth Inhibition Assay				IC50=640 nM	20682643
H82	Growth Inhibition Assay				IC50=250 nM	20682643
H146	Growth Inhibition Assay				IC50=35 nM	20682643
H526	Growth Inhibition Assay				IC50=480 nM	20682643
KM-H2	Function Assay	1 μM	0.25-48 h	DMSO	activates NF-kB	20880107
L428	Function Assay	1 μM	0.25-48 h	DMSO	activates NF-kB	20880107
HD-LM2	Function Assay	1 μM	0.25-48 h	DMSO	activates NF-kB	20880107
KM-H2	Function Assay	0.5/1 μM	24/48 h	DMSO	upregulates TNF-α dose and time dependently	20880107
L428	Function Assay	0.5/1 μM	24/48 h	DMSO	upregulates TNF-α dose and time dependently	20880107
HD-LM2	Function Assay	0.5/1 μM	24/48 h	DMSO	upregulates TNF-α dose and time dependently	20880107
KM-H2	Function Assay	1 μM	24/48 h	DMSO	downregulates XIAP, activated caspases 9 and 3	20880107
L428	Function Assay	1 μM	24/48 h	DMSO	downregulates XIAP, activated caspases 9 and 3	20880107
HD-LM2	Function Assay	1 μM	24/48 h	DMSO	downregulates XIAP, activated caspases 9 and 3	20880107
KM-H2	Apoptosis Assay	0.1/0.5/1 μM	48 h	DMSO	induces apoptosis dose dependently	20880107
L428	Apoptosis Assay	0.1/0.5/1 μM	48 h	DMSO	induces apoptosis dose dependently	20880107
HD-LM2	Apoptosis Assay	0.1/0.5/1 μM	48 h	DMSO	induces apoptosis dose dependently	20880107
KM-H2	Function Assay	0.1-2 μM	24 h	DMSO	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
L428	Function Assay	0.1-2 μM	24 h	DMSO	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
HD-LM2	Function Assay	0.1-2 μM	24 h	DMSO	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
KM-H2	Growth Inhibition Assay		72 h	DMSO	IC50=2.86 μM	20880107
L428	Growth Inhibition Assay		72 h	DMSO	IC50=1.96 μM	20880107
HD-LM2	Growth Inhibition Assay		72 h	DMSO	IC50=1.88 μM	20880107
LP1	Function Assay	1 μM	24 h		enhances 5-AC-induced MAGE-A3 gene expression	21171821
ANBL6	Function Assay	1 μM	24 h		enhances 5-AC-induced MAGE-A3 gene expression	21171821
HMEC	Growth Inhibition Assay				IC50=19 μM	21317455
SW620	Growth Inhibition Assay				IC50=1 μM	21317455
SW48	Growth Inhibition Assay				IC50=0.8 μM	21317455
HT-29	Growth Inhibition Assay				IC50=0.7 μM	21317455
HCT15	Growth Inhibition Assay				IC50=0.7 μM	21317455
PAXF 1657L†	Growth Inhibition Assay				EC50=0.3 μM	21375679
PAXF 546L†	Growth Inhibition Assay				EC50=1.5 μM	21375679
Panc-1	Growth Inhibition Assay				EC50=1.8 μM	21375679
MiaPaca-2	Growth Inhibition Assay				EC50=0.6 μM	21375679
AsPC-1	Growth Inhibition Assay				EC50=3.9 μM	21375679
BxPC-3	Growth Inhibition Assay				EC50=1.1 μM	21375679
MMCs	Function Assay	1 μM	6-24 h		dose-dependently inhibits the trimethylation level of H3-K9 (H3-K9me3)	24451378
MMCs	Function Assay	1 μM	24 h		augments global acetylation levels of histone H3-K9/14 (H3-K9/14ac) and H4-K12 (H4-K12ac)	24451378
MMCs	Function Assay	1 μM	24 h		increases HAT activity	24451378
MMCs	Function Assay	0.5/1 μM	24 h		shows 45-fold stimulation in cGMP levels	24451378
MMCs	Function Assay	1 μm	0-48 h		increases NPRA protein expression 2.7–3.5 fold	24451378
Panc1	Cell Viability Assay	1 μM	72 h	DMSO	enhances gemcitabine-induces cell viability decrease	25872941
Panc1	Apoptosis Assay	1 μM	72 h	DMSO	sensitizes Panc1 cells for gemcitabine-induced apoptosis	25872941
Panc1	Function Assay	0.5/1/2.5 μM	48 h	DMSO	reduces expression of ZEB1 on both mRNA and protein level	25872941
Panc1	Function Assay	0.5/1/2.5 μM	48 h	DMSO	upregulates miR-203	25872941
MOLP8	Growth Inhibition Assay		48 h		IC50=0.6± 0.04μM	26091518
T47D	Growth Inhibition Assay		48 h		IC50=1.17 μM	26378038
MCF7	Growth Inhibition Assay		48 h		IC50=0.67 μM	26378038
BT549	Growth Inhibition Assay		48 h		IC50=4.38 μM	26378038
MDA-MB-231	Growth Inhibition Assay		48 h		IC50=3.04 μM	26378038
HEK293	Function assay				Inhibition of HDAC1 in HEK293 cells, IC50=0.13μM	18308563
HEK293	Function assay				Inhibition of HDAC3 in HEK293 cells, IC50=0.61μM	18308563
HCT116	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.29μM	18570366
HCT116	Function assay				Induction of p21cip/waf1 protein expression in human HCT116 cells relative to MS275, EC50=0.45μM	18570366
Du145	Antiproliferative assay		72 hrs		Antiproliferative activity against human Du145 cells after 72 hrs by MTT assay, IC50=0.67μM	18570366
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.9μM	18570366
HCT116	Cell cycle assay				Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase, EC50<1μM	18570366
T24	Function assay				Induction of H3 histone acetylation in human T24 cells relative to MS275, EC50=1.38μM	18570366
HCT116	Apoptosis assay	1 uM			Induction of apoptosis in HCT116 cells at 1 uM	18570366
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells by MTT assay, IC50=0.3μM	19114304
HCT116	Function assay		16 hrs		Induction of p21WAF1/CIP1 expression in human HCT116 cells assessed as tubulin level after 16 hrs by luciferase assay, EC50=0.6μM	19114304
T24	Function assay		16 hrs		Induction of histone H4 hyperacetylation in human T24 cells after 16 hrs by immunoblotting, EC50<1μM	19114304
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50=0.31μM	21650221
H1299	Antiproliferative assay				Antiproliferative activity against human H1299 cells, IC50=1.44μM	21650221
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells, IC50=0.31μM	21742496
Sf9	Function assay		2 hrs		Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50=0.102μM	23009203
HCT116	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.327μM	23206867
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=1.279μM	23206867
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50=4.807μM	23206867
HCT116	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCT116 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay, IC50=0.7μM	23829483
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay, IC50=1.26μM	23829483
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay, IC50=1.73μM	23829483
DU145	Cytotoxicity assay		72 hrs		Cytotoxicity against human DU145 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay, IC50=2.06μM	23829483
Jurkat	Apoptosis assay	1 to 10 uM	24 hrs		Induction of apoptosis in human Jurkat cells assessed as PARP cleavage at 1 to 10 uM after 24 hrs by Western blot analysis	23829483
HeLa	Function assay	1 to 10 uM	24 hrs		Inhibition of HDAC in human HeLa cells assessed as increase in H3K9Ac level at 1 to 10 uM after 24 hrs by Western blot analysis	23829483
Jurkat	Function assay	1 to 10 uM	24 hrs		Inhibition of HDAC in human Jurkat cells assessed as increase in H3K9Ac level at 1 to 10 uM after 24 hrs by Western blot analysis	23829483
High5	Function assay		3 to 24 hrs		Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay, IC50=0.95μM	24095018
HCT116	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay, IC50=1.57μM	24095018
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay, IC50=1.65μM	24095018
High5	Function assay		3 to 24 hrs		Inhibition of human recombinant HDAC3 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay, IC50=1.67μM	24095018
SNU16	Cytotoxicity assay		72 hrs		Cytotoxicity against human SNU16 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.142μM	25805446
High5	Function assay		24 hrs		Inhibition of recombinant human HDAC2 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay, IC50=0.17μM	25805446
High5	Function assay		3 hrs		Inhibition of recombinant human HDAC3 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 hrs by fluorescence assay, IC50=0.36μM	25805446
High5	Function assay		24 hrs		Inhibition of recombinant human HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay, IC50=0.39μM	25805446
HCT116	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.396μM	25805446
SW620	Cytotoxicity assay		72 hrs		Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.419μM	25805446
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.61μM	25805446
Hep3B	Cytotoxicity assay		72 hrs		Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.823μM	25805446
HepG2	Cytotoxicity assay		72 hrs		Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.876μM	25805446
SNU5	Cytotoxicity assay		72 hrs		Cytotoxicity against human SNU5 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=1.009μM	25805446
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=2.08μM	25805446
SJSA1	Cytotoxicity assay		72 hrs		Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=3.624μM	25805446
MHCC97H	Cytotoxicity assay		72 hrs		Cytotoxicity against human MHCC97H cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=4.563μM	25805446
PANC1	Cytotoxicity assay		72 hrs		Cytotoxicity against human PANC1 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=26.774μM	25805446
U937	Function assay	10 uM	24 hrs		Inhibition of HDAC3 in human U937 cells assessed as increase in histone H3 lysine-9 acetylation at 10 uM incubated for 24 hrs by Western blotting method	26287310
PC3	Function assay	10 uM	24 hrs		Inhibition of HDAC3 in human PC3 cells assessed as increase in histone H3 lysine-9 acetylation at 10 uM incubated for 24 hrs by Western blotting method	26287310
U937	Function assay	10 uM	24 hrs		Inhibition of HDAC in human U937 cells assessed as reduction in cyclin E expression in at 10 uM incubated for 24 hrs by Western blotting method	26287310
Sf9	Function assay		10 mins		Inhibition of recombinant full length human C-terminal FLAG-tagged HDAC11 expressed in baculovirus infected Sf9 cells using Boc-Lys(epsilon-Ac)-AMC as substrate pretreated for 10 mins followed by substrate addition by fluorometric method, IC50=0.59μM	28501514
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
Sf9	Function assay				Inhibition Assay: HDAC inhibition assays were performed by Reaction Biology Corp. (Malvern, Pa.) using isolated human, recombinant full-length HDAC1 and -6 from a baculovirus expression system in Sf9 cells, IC50=0.102μM	ChEMBL
HCT116	Antiproliferative assay		48 hrs		Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=1.24μM	ChEMBL
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=2.49μM	ChEMBL
HeLa	Antiproliferative assay		48 hrs		Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=3.32μM	ChEMBL
HeLa	Antiproliferative assay		72 hrs		Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=3.42μM	ChEMBL
HCT116	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=3.51μM	ChEMBL
HepG2	Antiproliferative assay		48 hrs		Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=4.05μM	ChEMBL
HepG2	Antiproliferative assay		72 hrs		Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=4.25μM	ChEMBL
HepG2	Antiproliferative assay		24 hrs		Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=5.79μM	ChEMBL
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=11.87μM	ChEMBL
A549	Antiproliferative assay		48 hrs		Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=14.57μM	ChEMBL
HCT116	Antiproliferative assay		24 hrs		Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=29.69μM	ChEMBL
HeLa	Antiproliferative assay		24 hrs		Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=43.8μM	ChEMBL
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Informations chimiques, stockage et stabilité

Poids moléculaire	396.44	Formule	C₂₃H₂₀N₆O	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	726169-73-9	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	MG0103			Smiles	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4

Solubilité

In vitro
Lot:

DMSO : 60 mg/mL (151.34 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 160 mg/mL (403.59 mM) Ultrasonifié;
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

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.
Clear solution	5%DMSO 1 Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	2.000mg/ml (5.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	8.000mg/ml (20.18mM)	Taking the 1 mL working solution as an example, add 50 μL 160 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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	HDAC1 (Cell-free assay) 0.15 μM HDAC2 (Cell-free assay) 0.29 μM HDAC11 (Cell-free assay) 0.59 μM HDAC3 (Cell-free assay) 1.66 μM
In vitro	Le Mocetinostat (MGCD0103) n'inhibe qu'un sous-ensemble des neuf HDAC recombinantes humaines, y compris HDAC1, HDAC2, HDAC3 et HDAC11, à des concentrations nanomolaires ou micromolaires faibles, de manière dose-dépendante. Il révèle l'activité inhibitrice la plus puissante contre les enzymes HDAC1 et HDAC2 humaines in vitro et n'inhibe pas les HDAC de classe II. Le groupe amino exocyclique de ce composé est nécessaire à l'activité inhibitrice enzymatique car l'activité inhibitrice de la HDAC contre HDAC1 et HDAC2 est complètement abolie avec l'analogue désamino. Son activité inhibitrice atteint le plateau maximal à 6 μM, et le pool d'enzymes maximalement inhibable affecté par le MGCD0103 représente 75% de l'activité enzymatique totale dans les cellules HCT116, tandis que le NVP-LAQ824 inhibe presque 100% de celle-ci dans ces cellules. Dans les cellules A549, il présente également une inhibition dose-dépendante de l'activité HDAC dans les cellules entières.
Kinase Assay	Essai enzymatique HDAC in vitro
Kinase Assay	L'essai enzymatique de désacétylase est basé sur un essai homogène de libération de fluorescence. Des enzymes HDAC recombinantes purifiées sont incubées avec du Mocetinostat (MGCD0103) dilué à diverses concentrations pendant 10 minutes dans un tampon d'essai [25 mM HEPES (pH 8,0), 137 mM NaCl, 1 mM MgCl₂, 2,7 mM KCl] à température ambiante. Le substrat Boc-Lys(ε-Ac)-AMC est ajouté à la réaction pour une incubation supplémentaire à 37 °C. La concentration du substrat et le temps d'incubation varient pour les différents isotypes des enzymes HDAC. Une incubation à la trypsine de 20 minutes à température ambiante permet la libération du fluorophore à partir du substrat désacétylé. Le signal fluorescent est détecté par fluoromètre à une excitation de 360 nm, une émission de 470 nm et une coupure à 435 nm.
In vivo	Le Mocetinostat (MGCD0103) inhibe significativement la croissance des xénogreffes de tumeurs humaines chez les souris nues et l'activité antitumorale est corrélée à l'induction de l'acétylation des histones dans les tumeurs. L'administration P.O. de ce composé (sel de 2HBr) diminue significativement la croissance des tumeurs A549 avancées implantées chez les souris nues de manière dose-dépendante après 13 jours d'administration quotidienne. Il (170 mg/kg pour le sel de 2HBr, correspondant à 120 mg/kg de base libre) bloque significativement la croissance des tumeurs par rapport au traitement par véhicule seul sans changement de poids corporel. De plus, il ne réduit pas la numération des globules blancs et est bien toléré. Le composé est également actif par voie orale dans de nombreux autres modèles de xénogreffes de tumeurs humaines, y compris le NSCLC H1437. À 80 mg/kg (base libre), il bloque presque complètement la croissance des tumeurs H1437 après 13 jours d'administration p.o. quotidienne sans réduction du poids corporel chez les animaux. Il réduit la pression artérielle pulmonaire de manière plus spectaculaire. De plus, ce composé améliore le temps d'accélération de l'artère pulmonaire et réduit l'encoche systolique de l'enveloppe du flux de l'artère pulmonaire, ce qui suggère un impact positif de l'inhibiteur de HDAC sur le remodelage et le raidissement vasculaire pulmonaire.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/18413790/ [2] https://pubmed.ncbi.nlm.nih.gov/22282194/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	Ac-H3 / Ac-H4 / Ac-tubulin Bad / Bid / Bak / Puma / Bax / Cleaved caspase-9 / Cleaved caspase-3 / Cleaved PARP	29186204
Immunofluorescence	Nanog / MHC E-cadherin / ZEB1	26240433
Growth inhibition assay	Cell viability	26378038

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
NCT04299113	Recruiting	Rhabdomyosarcoma	Jonsson Comprehensive Cancer Center\|Mirati Therapeutics Inc.\|Phase One Foundation	May 14 2020	Phase 1
NCT02993991	Withdrawn	Squamous Cell Carcinoma Head And Neck\|Squamous Cell Carcinoma Mouth\|Resectable Squamous Cell Carcinoma of Oral Cavity	University Health Network Toronto\|Mirati Therapeutics Inc.\|AstraZeneca	October 10 2017	Phase 1
NCT02236195	Completed	Urothelial Carcinoma	Mirati Therapeutics Inc.	October 2014	Phase 2
NCT00666497	Terminated	Acute Myeloid Leukemia (AML)\|Myelodysplastic Syndrome (MDS)	Mirati Therapeutics Inc.	June 2008	Phase 2
NCT00511576	Terminated	Breast Cancer\|Lung Cancer\|Pulmonary Cancer\|Non-Small-Cell Lung Carcinoma\|Prostate Cancer\|Prostatic Cancer\|Gastric Cancer\|Stomach Cancer	Mirati Therapeutics Inc.	August 2007	Phase 1

Support technique

Instructions de manipulation

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