Mocetinostat (MGCD0103)

别名: MG0103

目录号：S1122 Purity: 99.93%

Mocetinostat (MGCD0103, MG0103) 是一种有效的HDAC抑制剂，对HDAC1抑制作用最强，无细胞试验中IC50为0.15 μM，比作用于HDAC2， 3，和11选择性高2到10倍，对HDAC4， 5， 6， 7，和8没有抑制活性。Mocetinostat (MGCD0103) 可诱导凋亡和自噬。Phase 2。

Mocetinostat (MGCD0103) Chemical Structure

CAS: 726169-73-9

规格	价格	库存
10mM (1mL in DMSO)	RMB 1563.11	现货
5mg	RMB 1382.65	现货
50mg	RMB 6314.53	现货
1g	RMB 24488.1	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

客户使用Selleck的Mocetinostat (MGCD0103)发表文献107篇

产品质控

批次：纯度： 99.93%

99.93

Mocetinostat (MGCD0103)相关产品

相关靶点	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	点击展开
相关产品	Entinostat (MS-275) Panobinostat (LBH589) TSA (Trichostatin A) RGFP966 Belinostat Tubastatin A Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) 2HCl MC1568 Tubastatin A HCl PCI-34051 Tacedinaline (CI994) LMK-235 Fimepinostat (CUDC-907) Tubacin Valproic Acid sodium Givinostat (ITF2357) VPA (Valproic acid) TMP269 AR-42 Sodium butyrate Pracinostat (SB939) Santacruzamate A (CAY10683) Abexinostat (PCI-24781) (-)-Parthenolide CUDC-101 Dacinostat (LAQ824) CAY10603 RG2833 (RGFP109) Tasquinimod 4-PBA (Sodium Phenylbutyrate) Tucidinostat (Chidamide) TMP195 Nexturastat A Droxinostat Domatinostat (4SC-202) Scriptaid 4-PBA (4-Phenylbutyric acid) M344 Resminostat Citarinostat (ACY-241) BG45 WT161 ACY-738 HPOB ITSA-1 (ITSA1) Tubastatin A TFA TC-H 106 SIS17 ACY-775 BML-210 (CAY10433) TH34 Raddeanin A	点击展开
相关化合物库	激酶抑制剂库 FDA药物库天然产物库已知活性药物库-I 生物活性库Ⅱ	点击展开

HDAC抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
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
点击查看更多细胞系数据

生物活性

产品描述

靶点

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

体外研究(In Vitro)
体外研究活性	MGCD0103按剂量依赖性在纳摩尔浓度或低微摩尔浓度时只能抑制9个人类重组HDACs中的一部分，包括HDAC1, HDAC2, HDAC3, 和HDAC11。在体外，MGCD0103有效抑制人类HDAC1和HDAC2酶，但是不抑制二级HDACs。MGCD0103的外环氨基抑制酶时是必需的，因为作用于HDAC1和HDAC2的HDAC抑制活性已被desamino类似物全部消除。MGCD0103 6 μM时抑制活性达到最高状态，在HCT116细胞中MGCD0103最高抑制全部酶活的75%，而NVP-LAQ824抑制几乎达到100%。MGCD0103抑制A549细胞时也显示出剂量依赖性。^[1]
激酶实验	体外HDAC酶实验
激酶实验	根据均相荧光释放法进行脱乙酰化酶活性测定。在实验buffer（包括25 mM HEPES，pH 为8.0, 137 mM NaCl, 1 mM MgCl₂, 2.7 mM KCl）中，纯化的重组HDAC酶和稀释成不同浓度的MGCD0103一起在室温下温育10分钟。加入底物Boc-Lys(ε-Ac)-AMC，在37^oC进一步温育。作用于不同亚型HDAC酶则底物浓度和温育时间都不同。加入胰蛋白酶室温下温育20分钟，脱乙酰化底物释放荧光。在360 , 470, 435 nm 波长处测定荧光信号。
细胞实验	细胞系	人类乳腺上皮细胞(HMEC)和人类包皮成纤维细胞(MRHF)
	浓度	0-60 μM
	孵育时间	72小时
	方法	人类乳腺上皮细胞(HMEC)和人类包皮成纤维细胞(MRHF)接种在96孔板上，加入不同浓度MGCD0103，在含5% CO₂环境37^oC下温育72小时。加入3-(4,5-二甲基-2-噻唑基)-2,5-二苯基溴化四唑（MTT），最终浓度为0.5 mg/ml，和细胞一起温育4小时，然后加入同体积溶解buffer,buffer包含50% N,N-二甲基甲酰胺,及20% SDS(pH 为4.7)。温育过夜，在630 nm 处标记，在570 nm 处读数，测量溶解的染料。根据相关细胞系的标准生长曲线计算细胞的吸光值。
实验图片	检测方法	检测指标	实验图片	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

体内研究(In Vivo)
体内研究活性	在裸鼠中，MGCD0103明显抑制人类移植瘤的生长，及抑制肿瘤中组蛋白乙酰化诱导的的相关抗癌活性。MGCD0103每天口服处理携带移植的晚期 A549肿瘤的裸鼠，13天后，明显降低生长，这种作用存在剂量依赖性。MGCD0103与对照组相比，明显阻断肿瘤生长，且体重没有改变。此外, MGCD0103不会使WBC数降低，且耐受性很好。 MGCD0103 作用于许多其他人类移植瘤模型包括NSCLC H1437，是口服有效的。MGCD0103按80 mg/kg 剂量每天口服给药携带H1437肿瘤的动物，13天后，完全抑制肿瘤生长，且动物体重没有下降。 ^[1]MGCD0103降低肺动脉高血压症的效果比tadalafil好，tadalafil是治疗肺动脉高血压症的常规法，是一种血管舒张药。此外, MGCD0103提高肺动脉加速时间，且降低肺动脉的收缩，说明HDAC 抑制剂作用于肺血管具有很好效果。^[2]
动物实验	Animal Models	携带H1437肿瘤的雌性CD-1裸鼠
	Dosages	80 mg/kg
	Administration	口服处理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (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

参考文献
[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.

参考文献

化学信息&溶解度

分子量	396.44	分子式	C₂₃H₂₀N₆O
CAS号	726169-73-9	SDF	Download Mocetinostat (MGCD0103) SDF
Smiles	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 60 mg/mL ( (151.34 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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