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
CAS: 726169-73-9
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
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 |
|
| 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] |
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|---|---|---|---|---|
| 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。 |
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| 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] |
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|---|---|---|
| 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 |
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 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
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
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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