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Mocetinostat (MGCD0103) HDAC inibitore

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

N. Cat.S1122

Mocetinostat (MGCD0103, MG0103) è un potente inibitore di HDAC con la massima potenza per HDAC1 con IC50 di 0,15 μM in un saggio senza cellule, una selettività da 2 a 10 volte superiore contro HDAC2, 3 e 11, e nessuna attività verso HDAC4, 5, 6, 7 e 8. Mocetinostat (MGCD0103) induce Apoptosis e Autophagy. Fase 2.

Mocetinostat (MGCD0103) HDAC inibitore Chemical Structure

Struttura chimica

Peso molecolare: 396.44

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Controllo Qualità

Lotto: Purezza: 99.93%

99.93

Target correlati	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Altro HDAC Inibitori	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

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dellattività	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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Informazioni chimiche, conservazione e stabilità

Peso molecolare	396.44	Formula	C₂₃H₂₀N₆O	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	726169-73-9	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	MG0103			Smiles	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4

Solubilità

In vitro
Lotto:

DMSO : 60 mg/mL (151.34 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 160 mg/mL (403.59 mM) Sonicato;
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

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	Mocetinostat (MGCD0103) inibisce solo un sottoinsieme delle nove HDAC ricombinanti umane, incluse HDAC1, HDAC2, HDAC3 e HDAC11 a concentrazioni nanomolari o micromolari basse, in modo dose-dipendente. Rivela la più potente attività inibitoria contro gli enzimi HDAC1 e HDAC2 umani in vitro e non inibisce le HDAC di classe II. Il gruppo amminico esociclico in questo composto è necessario per l'attività inibitoria dell'enzima perché l'attività inibitoria di HDAC contro HDAC1 e HDAC2 è completamente abolita con l'analogo desamminico. La sua attività inibitoria raggiunge il plateau massimo a 6 μM, e il pool enzimatico massimo inibibile influenzato da MGCD0103 è il 75% dell'attività enzimatica totale nelle cellule HCT116, mentre NVP-LAQ824 inibisce quasi il 100% di quella in queste cellule. Nelle cellule A549, mostra anche un'inibizione dose-dipendente dell'attività HDAC nelle cellule intere.
Saggio chinasico	Saggio enzimatico HDAC in vitro
Saggio chinasico	Il saggio enzimatico della deacetilasi si basa su un saggio omogeneo di rilascio di fluorescenza. Gli enzimi HDAC ricombinanti purificati vengono incubati con Mocetinostat (MGCD0103) diluito in varie concentrazioni per 10 minuti in tampone di saggio [25 mM HEPES (pH 8.0), 137 mM NaCl, 1 mM MgCl₂, 2.7 mM KCl] a temperatura ambiente. Il substrato Boc-Lys(ε-Ac)-AMC viene aggiunto alla reazione per un'ulteriore incubazione a 37 °C. La concentrazione del substrato e il tempo di incubazione variano per i diversi isotipi di enzimi HDAC. Un'incubazione con tripsina di 20 minuti a temperatura ambiente consente il rilascio del fluoroforo dal substrato deacetilato. Il segnale fluorescente viene rilevato da un fluorimetro con eccitazione a 360 nm, emissione a 470 nm e cut-off a 435 nm.
In vivo	Mocetinostat (MGCD0103) inibisce significativamente la crescita di xenotrapianti tumorali umani in topi nudi e l'attività antitumorale correlata all'induzione dell'acetilazione degli istoni nei tumori. L'amministrazione P.O. di questo composto (sale 2HBr) diminuisce significativamente la crescita dei tumori A549 avanzati impiantati in topi nudi in modo dose-dipendente dopo 13 giorni di somministrazione giornaliera. Esso (170 mg/kg per il sale 2HBr, corrispondente a 120 mg/kg di base libera) blocca significativamente la crescita dei tumori rispetto al solo trattamento con veicolo senza alcun cambiamento di peso corporeo. Inoltre, non riduce il numero di globuli bianchi ed è ben tollerato. Il composto è anche attivo per via orale in molti altri modelli di xenotrapianto tumorale umano, incluso l'NSCLC H1437. A 80 mg/kg (base libera), blocca quasi completamente la crescita dei tumori H1437 dopo 13 giorni di somministrazione giornaliera p.o. senza riduzione del peso corporeo negli animali. Riduce la pressione arteriosa polmonare in modo più drammatico. Inoltre, questo composto migliora il tempo di accelerazione dell'arteria polmonare e riduce l'incavo sistolico dell'inviluppo del flusso dell'arteria polmonare, il che suggerisce un impatto positivo dell'inibitore di HDAC sul rimodellamento e l'irrigidimento vascolare polmonare.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/18413790/ [2] https://pubmed.ncbi.nlm.nih.gov/22282194/

Applicazioni

Metodi	Biomarcatori	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

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

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