Mocetinostat (MGCD0103)

别名: MG0103

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

Mocetinostat (MGCD0103) Chemical Structure

CAS: 726169-73-9

规格 价格 库存 购买数量
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
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客户使用Selleck的Mocetinostat (MGCD0103)发表文献108

产品质控

批次: 纯度: 99.93%
99.93

Mocetinostat (MGCD0103)相关产品

相关信号通路图

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 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。
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
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37oC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37oC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。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好。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
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

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)

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

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)

mg/kg g μL

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,: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: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: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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