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Mocetinostat (MGCD0103)

別名: MG0103

Mocetinostat (MGCD0103, MG0103) 是一種有效的HDAC抑制劑，對HDAC1抑制作用最強，無細(xì)胞試驗中IC50為0.15 μM，比作用于HDAC2， 3，和11選擇性高2到10倍，對HDAC4， 5， 6， 7，和8沒有抑制活性。Mocetinostat (MGCD0103) 可誘導(dǎo)凋亡和自噬。Phase 2。

Mocetinostat (MGCD0103) Chemical Structure

Mocetinostat (MGCD0103) Chemical Structure

CAS: 726169-73-9

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1563.11 現(xiàn)貨
5mg 1382.65 現(xiàn)貨
50mg 6314.53 現(xiàn)貨
1g 24488.1 現(xiàn)貨
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Mocetinostat (MGCD0103)相關(guān)產(chǎn)品

相關(guān)信號通路圖

HDAC Signaling Pathways

HDAC信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Mocetinostat (MGCD0103, MG0103) 是一種有效的HDAC抑制劑，對HDAC1抑制作用最強，無細(xì)胞試驗中IC50為0.15 μM，比作用于HDAC2， 3，和11選擇性高2到10倍，對HDAC4， 5， 6， 7，和8沒有抑制活性。Mocetinostat (MGCD0103) 可誘導(dǎo)凋亡和自噬。Phase 2。
靶點
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
體外研究(In Vitro)
體外研究活性

MGCD0103按劑量依賴性在納摩爾濃度或低微摩爾濃度時只能抑制9個人類重組HDACs中的一部分，包括HDAC1, HDAC2, HDAC3, 和HDAC11。在體外，MGCD0103有效抑制人類HDAC1和HDAC2酶，但是不抑制二級HDACs。MGCD0103的外環(huán)氨基抑制酶時是必需的，因為作用于HDAC1和HDAC2的HDAC抑制活性已被desamino類似物全部消除。MGCD0103 6 μM時抑制活性達(dá)到最高狀態(tài)，在HCT116細(xì)胞中MGCD0103最高抑制全部酶活的75%，而NVP-LAQ824抑制幾乎達(dá)到100%。MGCD0103抑制A549細(xì)胞時也顯示出劑量依賴性。[1]
激酶實驗 體外HDAC酶實驗
根據(jù)均相熒光釋放法進行脫乙酰化酶活性測定。在實驗buffer（包括25 mM HEPES，pH 為8.0, 137 mM NaCl, 1 mM MgCl2, 2.7 mM KCl）中，純化的重組HDAC酶和稀釋成不同濃度的MGCD0103一起在室溫下溫育10分鐘。加入底物Boc-Lys(ε-Ac)-AMC，在37oC進一步溫育。作用于不同亞型HDAC酶則底物濃度和溫育時間都不同。加入胰蛋白酶室溫下溫育20分鐘，脫乙?；孜镝尫艧晒?。在360 , 470, 435 nm 波長處測定熒光信號。
細(xì)胞實驗 細(xì)胞系 人類乳腺上皮細(xì)胞(HMEC)和人類包皮成纖維細(xì)胞(MRHF)
濃度 0-60 μM
孵育時間 72小時
方法

人類乳腺上皮細(xì)胞(HMEC)和人類包皮成纖維細(xì)胞(MRHF)接種在96孔板上，加入不同濃度MGCD0103，在含5% CO2環(huán)境37oC下溫育72小時。加入3-(4,5-二甲基-2-噻唑基)-2,5-二苯基溴化四唑（MTT），最終濃度為0.5 mg/ml，和細(xì)胞一起溫育4小時，然后加入同體積溶解buffer。溫育過夜，在630 nm 處標(biāo)記，在570 nm 處讀數(shù)，測量溶解的染料。根據(jù)相關(guān)細(xì)胞系的標(biāo)準(zhǔn)生長曲線計算細(xì)胞的吸光值。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

在裸鼠中，MGCD0103明顯抑制人類移植瘤的生長，及抑制腫瘤中組蛋白乙?；T導(dǎo)的的相關(guān)抗癌活性。MGCD0103每天口服處理攜帶移植的晚期 A549腫瘤 的裸鼠，13天后，明顯降低生長，這種作用存在劑量依賴性。MGCD0103與對照組相比，明顯阻斷腫瘤生長，且體重沒有改變。此外, MGCD0103不會使WBC數(shù)降低，且耐受性很好。 MGCD0103 作用于許多 其他人類移植瘤模型包括NSCLC H1437，是口服有效的。MGCD0103按80 mg/kg 劑量每天口服給藥攜帶H1437腫瘤的動物，13天后，完全抑制腫瘤生長，且動物體重沒有下降。 [1]MGCD0103降低肺動脈高血壓癥的效果好。此外, MGCD0103提高肺動脈加速時間，且降低肺動脈的收縮，說明HDAC 抑制劑作用于肺血管具有很好效果。[2]
動物實驗 Animal Models 攜帶H1437腫瘤的雌性CD-1裸鼠
Dosages 80 mg/kg
Administration 口服處理
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

化學(xué)信息&溶解度

分子量 396.44 分子式

C23H20N6O
CAS號 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
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 60 mg/mL ( (151.34 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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