Mocetinostat (MGCD0103)

目录号:S1122 别名: MG0103

仅限科研使用

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 购买数量
10mM (1mL in DMSO) RMB 1563.11 现货
RMB 1382.65 现货
RMB 6314.53 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Mocetinostat (MGCD0103)发表文献97篇:

产品安全说明书

HDAC抑制剂选择性比较

相关HDAC产品

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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PBMC  NHy1fIRCeG:ydH;zbZMhSXO|YYm= MkPXNE42NzJxMzFOwG0> NGjLN3QzPC92ODDo MmHwbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M3vu[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNEC2PVQ4Lz5{MESwOlk1PzxxYU6=
HeLa  M2[0fWZ2dmO2aX;uJGF{e2G7 NVfBb|J4OTBizszNxsA> MUe3JIg> MXnEUXNQ NY[1foNS\Gm|coXweJMhdm:{bXHsJJNxcW6mbHWgZ4hm[2uyb3nueEBnfW6ldHnvci=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa MVXGeY5kfGmxbjDBd5NigQ>? MkPCNVAh|ryPwrC= NEjG[Yk3NzF{L{K0JIg> NXjzSYNjTE2VTx?= NH3afINqdmS3Y3XzJI1qfG:2aXOgZYNkfW23bHH0bY9vKGGwZDDk[YxigWWmIICyNUBmgHC{ZYPzbY9v NHfTbpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWzPFg1OCd-MkC1N|g5PDB:L3G+
HeLa NHP1eoJHfW6ldHnvckBCe3OjeR?= MofINE4{NTFyIN88US=> MWi4JIg> NH3MW49FVVOR M2roSYlv[3KnYYPld{Bk[XOyYYPlJFMh[W6mIEegZYN1cX[jdHnvckBld3OnIHTldIVv\GWwdHz5 Mn;aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3M{i4OFAoRjJyNUO4PFQxRC:jPh?=
HeLa NUiwUXc1TnWwY4Tpc44hSXO|YYm= MnvNNE4{NTFyIN88US=> MY[4JIg> NXHmOGp2TE2VTx?= NFna[|dqdmO{ZXHz[ZMh[WOndInsZZRm\CCKMzDLPUApUDONOVHjLUBifCBzMDFOwG0> NYPMcnRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N|g5PDBpPkKwOVM5QDRyPD;hQi=>
DMS114 NWHwXnpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljXTWM2OD14NECgcm0> NYTiRldnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFI3PDNpPkKwOlgzPjR|PD;hQi=>
H82 NIrhSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\CTWM2OD1{NUCgcm0> M{HFXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H146 NETmSmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\YeJc{UUN3ME2zOUBvVQ>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ6Mk[0N{c,OjB4OEK2OFM9N2F-
H526 NU[5N4JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjYelZVUUN3ME20PFAhdk1? MnXLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEK2OFMoRjJyNkiyOlQ{RC:jPh?=
KM-H2 MWjGeY5kfGmxbjDBd5NigQ>? MVSxxsDPxE1? NV62e5VsOC5{NT20PEBp NWnaUZRRTE2VTx?= MVThZ5RqfmG2ZYOgUmYuc0J? M{X6elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428 MVvGeY5kfGmxbjDBd5NigQ>? MUWxxsDPxE1? M2HDOlAvOjVvNEigbC=> NWHwbVY6TE2VTx?= NH7MeXBi[3SrdnH0[ZMhVkZva1K= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2 M1zNcWZ2dmO2aX;uJGF{e2G7 MXSxxsDPxE1? NFr6SYsxNjJ3LUS4JIg> NX7NOWZOTE2VTx?= M1jXVoFkfGm4YYTld{BPTi2tQh?= M4\RPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 Moi0SpVv[3Srb36gRZN{[Xl? NIfmVlYxNjVxMTFOwG0> M3nPclI1NzR6IHi= M3HNW2ROW09? M2\LW5VxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NYDLcnV4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 MkLkSpVv[3Srb36gRZN{[Xl? NGi3Zm0xNjVxMTFOwG0> NFHONWMzPC92ODDo NUHXVZJFTE2VTx?= MnK4eZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= M4HWW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
HD-LM2 Mlv6SpVv[3Srb36gRZN{[Xl? NHjTNIYxNjVxMTFOwG0> MoPxNlQwPDhiaB?= MXvEUXNQ M1T0TJVxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NVnhU|JxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2 MljISpVv[3Srb36gRZN{[Xl? MUWxxsDPxE1? NYn6UodSOjRxNEigbC=> NXrMbJY1TE2VTx?= MXfkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
L428 MmL6SpVv[3Srb36gRZN{[Xl? NIra[YYyyqEQvF2= M2PISFI1NzR6IHi= MVPEUXNQ NV3XS4d2\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? Mm\FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2 M1;INWZ2dmO2aX;uJGF{e2G7 MUCxxsDPxE1? M13nS|I1NzR6IHi= M1LoUWROW09? M{W5OIRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> M37SbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 M4H2OWFxd3C2b4Ppd{BCe3OjeR?= M1;SXFAvOS9yLkWvNUDPxE1? MV:0PEBp NGP3XYFFVVOR M3\qcolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M1P3W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428 MWDBdI9xfG:|aYOgRZN{[Xl? M3LOeFAvOS9yLkWvNUDPxE1? MnHROFghcA>? NIjSeGlFVVOR Ml3JbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M3;1N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
HD-LM2 MoLMRZBweHSxc3nzJGF{e2G7 MXKwMlEwOC53L{Gg{txO NF\Vc2k1QCCq NVntcZhOTE2VTx?= MXjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NETBWIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
KM-H2 MnzHSpVv[3Srb36gRZN{[Xl? NHe4NJIxNjFvMjFOwG0> NIHZNG4zPCCqwrC= NV;LbXE6TE2VTx?= NEX3Wot{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx MlvWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 M1PQSWZ2dmO2aX;uJGF{e2G7 Mmm2NE4yNTJizszN MX[yOEBpyqB? NWTpNnliTE2VTx?= MVnzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz MmLZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2 NUHRSIdTTnWwY4Tpc44hSXO|YYm= M3q0PVAvOS1{IN88US=> NU\6dIdmOjRiaNMg NYDOfZRuTE2VTx?= M1z6UpNpd3e|IHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhOyCjbnSgeZBz\We3bHH0bY9vKG:oIITo[UBk\WyuIHP5Z4xmKHKnZ4XsZZRwenlicILveIVqdiCyMkG= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2 NUHIWml{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX63NuKhcA>? MnrISG1UVw>? MUjJR|UxRTJwOE[g{txO MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
L428 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v0e|czyqCq MVzEUXNQ NIDkS4JKSzVyPUGuPVYh|ryP NHn5eYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
HD-LM2 M17LNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVW3NuKhcA>? M2\LRmROW09? NUS3XYRzUUN3ME2xMlg5KM7:TR?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
LP1 MnntSpVv[3Srb36gRZN{[Xl? NIHGd4syyqEQvF2= MUiyOEBp Mmq1[Y5p[W6lZYOgOU1CSy2rbnT1Z4VlKE2DR1WtRVMh\2WwZTDlfJBz\XO|aX;u MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF5MUiyNUc,OjFzN{G4NlE9N2F-
ANBL6  M3P1VGZ2dmO2aX;uJGF{e2G7 M{\ocFHDqM7:TR?= MnHDNlQhcA>? NHjnPZRmdmijbnPld{A2NUGFLXnu[JVk\WRiTVHHSU1COyCpZX7lJIV5eHKnc4Ppc44> NIPQNHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUG3NVgzOSd-MkGxO|E5OjF:L3G+
HMEC NEjUPWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDsTY9KSzVyPUG5JO69VQ>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF|MUe0OVU9N2F-
SW620 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[4VmlEPTB;MTFOwG0> Ml;uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MUe0OVUoRjJzM{G3OFU2RC:jPh?=
SW48 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LtU2lEPTB;MD64JO69VQ>? MmHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MUe0OVUoRjJzM{G3OFU2RC:jPh?=
HT-29 MlPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnmyTWM2OD1yLkeg{txO MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF|MUe0OVU9N2F-
HCT15 MkThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwNzFOwG0> NHf6dIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO|Q2PSd-MkGzNVc1PTV:L3G+
PAXF 1657L† NHfUSZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHQSWM2OD1yLkOg{txO M2jHRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
PAXF 546L† NInZbFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELxVYlGSzVyPUGuOUDPxE1? NWPMdJNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|U3PzlpPkKxN|c2Pjd7PD;hQi=>
Panc-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfyb|RuTUN3ME2xMlgh|ryP M3KwUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
MiaPaca-2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3:5[2VEPTB;MD62JO69VQ>? NV3X[3JnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|U3PzlpPkKxN|c2Pjd7PD;hQi=>
AsPC-1 MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXwfnRGSzVyPUOuPUDPxE1? M{DpVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
BxPC-3 M3LM[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XEfWVEPTB;MT6xJO69VQ>? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
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HepG2 MWXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MlHxNlQhcHK| NUi5[FR5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02Njd7zszN NXzlTmRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
A549 M3j4dWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYS0fVhCPzJiaILz NEjPS4hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NVEvQDgQvF2= M13uUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4Ojl6MD:nQmNpTU2ETEyvZV4>
A549 MlL5RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NWnlcmFFPDhiaILz NXiybHZRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE1NjV5zszN NYfnU3FHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
HCT116 MYfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MV2yOEBpenN? NWHKT3ZySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDJ2IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OjlwNkpOwG0> NXH2TJFmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
HeLa NXezRZM3SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MlTnNlQhcHK| Mn65RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSzMljPxE1? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|I6QDBxJ{7DbGVOSkx:L3G+
Assay
Methods Test Index PMID
Western blot Bad / Bid / Bak / Puma / Bax / Cleaved caspase-9 / Cleaved caspase-3 / Cleaved PARP Ac-H3 / Ac-H4 / Ac-tubulin 27551526 29186204
Immunofluorescence E-cadherin / ZEB1 Nanog / MHC 25872941 26240433
Growth inhibition assay Cell viability 26378038
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
  • 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:[1]
  • Cell lines: 人类乳腺上皮细胞(HMEC)和人类包皮成纤维细胞(MRHF)
  • Concentrations: 0-60 μM
  • Incubation Time: 72小时
  • Method: 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,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。
动物实验:[1]
  • Animal Models: 携带H1437肿瘤的雌性CD-1裸鼠
  • Dosages: 80 mg/kg
  • Administration: 口服处理

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
30% PEG400+0.5% Tween80+5% Propylene glycol

30mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 396.44
化学式

C23H20N6O

CAS号 726169-73-9
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04299113 Recruiting Drug: Vinorelbine|Drug: Mocetinostat Rhabdomyosarcoma Jonsson Comprehensive Cancer Center|Mirati Therapeutics Inc.|Phase One Foundation May 14 2020 Phase 1
NCT02993991 Withdrawn Drug: Mocetinostat|Biological: Durvalumab 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 Drug: Mocetinostat Urothelial Carcinoma Mirati Therapeutics Inc. October 2014 Phase 2
NCT00666497 Terminated Drug: Azacitidine|Drug: MGCD0103 Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS) Mirati Therapeutics Inc. June 2008 Phase 2
NCT00511576 Terminated Drug: MGCD0103 & Docetaxel 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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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