Mocetinostat (MGCD0103)

別名：MG0103

製品コード：S1122 純度：99.93%

Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.

CAS No. 726169-73-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 37000	国内在庫あり
5mg	JPY 25500	国内在庫あり
10mg	JPY 40500	国内在庫あり
50mg	JPY 115500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（107）

製品安全説明書

現在のバッチを見る：純度： 99.93%

99.93

Mocetinostat (MGCD0103)関連製品

関連ターゲット	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	もっと見る
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関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ	もっと見る

シグナル伝達経路

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
LP1	Function Assay	1 μM	24 h	enhances 5-AC-induced MAGE-A3 gene expression	21171821
HD-LM2	Function Assay	0.1-2 μM	24 h	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
L428	Function Assay	0.1-2 μM	24 h	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
KM-H2	Function Assay	0.1-2 μM	24 h	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
HD-LM2	Apoptosis Assay	0.1/0.5/1 μM	48 h	induces apoptosis dose dependently	20880107
L428	Apoptosis Assay	0.1/0.5/1 μM	48 h	induces apoptosis dose dependently	20880107
KM-H2	Apoptosis Assay	0.1/0.5/1 μM	48 h	induces apoptosis dose dependently	20880107
HD-LM2	Function Assay	1 μM	24/48 h	downregulates XIAP, activated caspases 9 and 3	20880107
L428	Function Assay	1 μM	24/48 h	downregulates XIAP, activated caspases 9 and 3	20880107
KM-H2	Function Assay	1 μM	24/48 h	downregulates XIAP, activated caspases 9 and 3	20880107
HD-LM2	Function Assay	0.5/1 μM	24/48 h	upregulates TNF-α dose and time dependently	20880107
L428	Function Assay	0.5/1 μM	24/48 h	upregulates TNF-α dose and time dependently	20880107
KM-H2	Function Assay	0.5/1 μM	24/48 h	upregulates TNF-α dose and time dependently	20880107
HD-LM2	Function Assay	1 μM	0.25-48 h	activates NF-kB	20880107
L428	Function Assay	1 μM	0.25-48 h	activates NF-kB	20880107
KM-H2	Function Assay	1 μM	0.25-48 h	activates NF-kB	20880107
HeLa	Function Assay	0.3-10 μM	8 h	increases acetylated H3 K9 (H3K9Ac) at 10 μM	20538840
HeLa	Function Assay	0.3-10 μM	8 h	increases caspase 3 and 7 activation dose dependently	20538840
HeLa	Function Assay	10 μM	6/12/24 h	induces mitotic accumulation and delayed p21 expression	20538840
HeLa	Function Assay	10 μM	7 h	disrupts normal spindle checkpoint function	20538840
PBMC	Apoptosis Assay	0.5/2/3 μM	24/48 h	induces apoptosis dose and time dependently	20406947
ANBL6	Function Assay	1 μM	24 h	enhances 5-AC-induced MAGE-A3 gene expression	21171821
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	enhances gemcitabine-induces cell viability decrease	25872941
Panc1	Apoptosis Assay	1 μM	72 h	sensitizes Panc1 cells for gemcitabine-induced apoptosis	25872941
Panc1	Function Assay	0.5/1/2.5 μM	48 h	reduces expression of ZEB1 on both mRNA and protein level	25872941
Panc1	Function Assay	0.5/1/2.5 μM	48 h	upregulates miR-203	25872941
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
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
HCT116	Apoptosis assay	1 uM		Induction of apoptosis in HCT116 cells at 1 uM	18570366
HD-LM2	Growth Inhibition Assay		72 h	IC50=1.88 μM	20880107
L428	Growth Inhibition Assay		72 h	IC50=1.96 μM	20880107
KM-H2	Growth Inhibition Assay		72 h	IC50=2.86 μM	20880107
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
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.29μM	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	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
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
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
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
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
H526	Growth Inhibition Assay			IC50=480 nM	20682643
H146	Growth Inhibition Assay			IC50=35 nM	20682643
H82	Growth Inhibition Assay			IC50=250 nM	20682643
DMS114	Growth Inhibition Assay			IC50=640 nM	20682643
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
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	Function assay			Induction of p21cip/waf1 protein expression in human HCT116 cells relative to MS275, EC50=0.45μM	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	Antiproliferative assay			Antiproliferative activity against human HCT116 cells by MTT assay, IC50=0.3μM	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
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
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生物活性

製品説明

Targets

HDAC1 ^[1] (Cell-free assay)	HDAC2 ^[1] (Cell-free assay)	HDAC11 ^[1] (Cell-free assay)	HDAC3 ^[1] (Cell-free assay)
0.15 μM	0.29 μM	0.59 μM	1.66 μM

In Vitro
In vitro	MGCD0103 inhibits only a subset of the nine human recombinant HDACs, including HDAC1, HDAC2, HDAC3, and HDAC11 at nanomolar or low micromolar concentrations, in a dose-dependent manner. MGCD0103 reveals most potent inhibitory activity against human HDAC1 and HDAC2 enzymes in vitro, and it does not inhibit class II HDACs. The exocyclic amino group in MGCD0103 is necessary for enzyme inhibitory activity because HDAC-inhibitory activity against HDAC1 and HDAC2 is completely abolished with the desamino analogue. The inhibitory activity of MGCD0103 reaches the maximum plateau at 6 μM, and the maximal inhibitable enzyme pool affected by MGCD0103 is 75% of the total enzyme activity in HCT116 cells whereas NVP-LAQ824 inhibits almost 100% of that in these cells. In A549 cells, MGCD0103 also exhibits dose-dependent inhibition of HDAC activity in whole cells. ^[1]
Kinase Assay	HDAC enzyme assay in vitro
Kinase Assay	The deacetylase enzyme assay is based on a homogeneous fluorescence release assay. Purified recombinant HDAC enzymes are incubated with MGCD0103 diluted in various concentrations for 10 minutes in assay buffer [25 mM HEPES (pH 8.0), 137 mM NaCl, 1 mM MgCl₂, 2.7 mM KCl] at room temperature. The substrate Boc-Lys(ε-Ac)-AMC is added to the reaction for further incubation at 37 °C. The concentration of the substrate and the incubation time varies for different isotypes of HDAC enzymes. A 20-min trypsin incubation at room temperature allows the release of the fluorophore from the deacetylated substrate. The fluorescent signal is detected by fluorometer at excitation of 360 nm, emission of 470 nm, and cutoff at 435 nm.
細胞実験	細胞株	Human mammary epithelial cells (HMEC), human foreskin fibroblasts (MRHF) cells
	濃度	0-60 μM
	反応時間	72 hours
	実験の流れ	Human mammary epithelial cells (HMEC) and human foreskin fibroblasts (MRHF) cells in 96-well plates are incubated with MGCD0103 at various concentrations for 72 hours at 37 °C in 5% CO₂. MTT is added at a final concentration of 0.5 mg/ml and incubated with the cells for 4 hours before an equal volume of solubilization buffer [50% N,N-dimethylformamide, 20% SDS (pH 4.7)] is added. After overnight incubation, solubilized dye is quantified by reading at 570 nm using a reference at 630 nm. Absorbance values are converted to cell numbers according to a standard growth curve of the relevant cell line. The concentration which reduces cell numbers to 50% relative to DMSO-treated cells is determined as MTT IC5
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
In Vivo	MGCD0103 significantly inhibites growth of human tumor xenografts in nude mice and the antitumor activity correlated with induction of histone acetylation in tumors. P.O. administration of MGCD0103 (2HBr salt) significantly decreases growth of implanted advanced A549 tumors in nude mice in a dose-dependent manner after 13 days of daily administration. MGCD0103 (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blockes growth of tumors compared with vehicle treatment alone with no change in body weight. In addition, MGCD0103 does not reduce WBC counts and is well tolerated. MGCD0103 is also orally active in many other human tumor xenograft models including NSCLC H1437. MGCD0103 at 80 mg/kg (free base) almost completely blocks the growth of H1437 tumors after 13 days of daily p.o. administration with no reduction of body weight in animals. ^[1] MGCD0103 reduces pulmonary arterial pressure more dramatically than tadalafil, a standard-of-care therapy for human pulmonary hypertension that functions as a vasodilator. Moreover, MGCD0103 improves pulmonary artery acceleration time and reduced systolic notching of the pulmonary artery flow envelope, which suggests a positive impact of the HDAC inhibitor on pulmonary vascular remodeling and stiffening. ^[2]
動物実験	動物モデル	Female CD-1 nude mice bearing H1437 tumors
	投与量	80 mg/kg
	投与経路	Administered via p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

参考
[1] Fournel M, et al. Mol Cancer Ther. 2008, 7(4), 759-768. [2] Cavasin MA, et al. Circ Res. 2012, 110(5), 739-748.

参考

化学情報

分子量	396.44	化学式	C₂₃H₂₀N₆O
CAS No.	726169-73-9	SDF	Download Mocetinostat (MGCD0103) SDFをダウンロードする
Smiles	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 60 mg/mL ( (151.34 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):