Mocetinostat (MGCD0103)

For research use only. Not for use in humans.

目录号:S1122 别名: MG0103

Mocetinostat (MGCD0103) Chemical Structure

CAS No. 726169-73-9

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。

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
有超大折扣
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客户使用Selleck生产的Mocetinostat (MGCD0103)发表文献96篇:

产品安全说明书

HDAC抑制剂选择性比较

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  MlnjRZBweHSxc3nzJGF{e2G7 M4LiRVAvPS9{L{Og{txO NFGxb2ozPC92ODDo MX\pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODRyNkm0O{c,OjB2ME[5OFc9N2F-
HeLa  NX20d|Y2TnWwY4Tpc44hSXO|YYm= MkjXNVAh|ryPwrC= NG\rW3A4KGh? MoXwSG1UVw>? NYiyUXVz\Gm|coXweJMhdm:{bXHsJJNxcW6mbHWgZ4hm[2uyb3nueEBnfW6ldHnvci=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa NFvJT5lHfW6ldHnvckBCe3OjeR?= NWTrXo5COTBizszNxsA> NIrYUWI3NzF{L{K0JIg> MV\EUXNQ NGTudJJqdmS3Y3XzJI1qfG:2aXOgZYNkfW23bHH0bY9vKGGwZDDk[YxigWWmIICyNUBmgHC{ZYPzbY9v NHfkTFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWzPFg1OCd-MkC1N|g5PDB:L3G+
HeLa M1P3bWZ2dmO2aX;uJGF{e2G7 NUfXeGRYOC5|LUGwJO69VQ>? MYq4JIg> NFnhRlBFVVOR NGri[5BqdmO{ZXHz[ZMh[2G|cHHz[UA{KGGwZDC3JIFkfGm4YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa NUDPcplkTnWwY4Tpc44hSXO|YYm= MX[wMlMuOTBizszN MX24JIg> M2jCTGROW09? NVvxcWU6cW6lcnXhd4V{KGGlZYT5cIF1\WRiSEOgT|khMEh|S{nBZ{kh[XRiMUCg{txO MkLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3M{i4OFAoRjJyNUO4PFQxRC:jPh?=
DMS114 MoG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknKTWM2OD14NECgcm0> MmO0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEK2OFMoRjJyNkiyOlQ{RC:jPh?=
H82 NELESWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ3MDDuUS=> NVLMS4hIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFI3PDNpPkKwOlgzPjR|PD;hQi=>
H146 NGKxd5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXTTWM2OD1|NTDuUS=> M2f3PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H526 NUPKc|dWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PFZWlEPTB;NEiwJI5O Mlu5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEK2OFMoRjJyNkiyOlQ{RC:jPh?=
KM-H2 M3zLO2Z2dmO2aX;uJGF{e2G7 Mk\CNeKh|ryP MXqwMlI2NTR6IHi= M{\RR2ROW09? MWrhZ5RqfmG2ZYOgUmYuc0J? NEWyTmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
L428 M2n3WmZ2dmO2aX;uJGF{e2G7 MmDyNeKh|ryP M{\XS|AvOjVvNEigbC=> MnzPSG1UVw>? MVvhZ5RqfmG2ZYOgUmYuc0J? Mn3nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2 M{LjSGZ2dmO2aX;uJGF{e2G7 MXixxsDPxE1? MVewMlI2NTR6IHi= NXHIVlN4TE2VTx?= MYfhZ5RqfmG2ZYOgUmYuc0J? NGHhXoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
KM-H2 M4PRW2Z2dmO2aX;uJGF{e2G7 MmPKNE42NzFizszN MkXDNlQwPDhiaB?= NWDFS|Z[TE2VTx?= NEL6XVh2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NXLWb45qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 MXHGeY5kfGmxbjDBd5NigQ>? NH\tUZoxNjVxMTFOwG0> NGT2O4czPC92ODDo M{XJZmROW09? M1qyOZVxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 M2HrelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
HD-LM2 MXHGeY5kfGmxbjDBd5NigQ>? M{KyVFAvPS9zIN88US=> MWiyOE81QCCq NWj1TIJoTE2VTx?= NH[zdm92eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2 M{[1WWZ2dmO2aX;uJGF{e2G7 MUSxxsDPxE1? NVf4Oo9IOjRxNEigbC=> MkLESG1UVw>? NUT4Z5ZM\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? NGfqc|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
L428 M1vaZmZ2dmO2aX;uJGF{e2G7 NITuWVgyyqEQvF2= NUfae3VHOjRxNEigbC=> MVrEUXNQ MWfkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz NE\ySHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
HD-LM2 NVTvTYUxTnWwY4Tpc44hSXO|YYm= NG[0c3cyyqEQvF2= Ml\6NlQwPDhiaB?= NV25W2ZCTE2VTx?= MUXkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz M2PSdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 MVHBdI9xfG:|aYOgRZN{[Xl? NWnQV41EOC5zL{CuOU8yKM7:TR?= MVm0PEBp Moq3SG1UVw>? MVTpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 Mo\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 NFH4WZNCeG:ydH;zbZMhSXO|YYm= NFTmUm4xNjFxMD61M|Eh|ryP MWi0PEBp NEDxO|hFVVOR NWjPbGszcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M{XBcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
HD-LM2 MnfuRZBweHSxc3nzJGF{e2G7 MXywMlEwOC53L{Gg{txO M{n4elQ5KGh? NX\1dVczTE2VTx?= NVjYSoUzcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M4q0SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 M2fue2Z2dmO2aX;uJGF{e2G7 M1raXVAvOS1{IN88US=> NFPuVHQzPCCqwrC= M2TremROW09? NYHhUXdwe2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=> NHy4W3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
L428 MX;GeY5kfGmxbjDBd5NigQ>? NU[0fZZjOC5zLUKg{txO NUL1emdvOjRiaNMg MXPEUXNQ M{PRNZNpd3e|IHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhOyCjbnSgeZBz\We3bHH0bY9vKG:oIITo[UBk\WyuIHP5Z4xmKHKnZ4XsZZRwenlicILveIVqdiCyMkG= NV\DdYhJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 NVnTVZJxTnWwY4Tpc44hSXO|YYm= MYOwMlEuOiEQvF2= MWKyOEBpyqB? NH\PXllFVVOR NGfLN5N{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2 NIjtcoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[3NuKhcA>? NF;wVYxFVVOR MlHZTWM2OD1{Lki2JO69VQ>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
L428 NHjGS5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX4O|LDqGh? NIPERWpFVVOR NE[3c3BKSzVyPUGuPVYh|ryP MmX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2 NV\rSIo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLVO|LDqGh? M4f0bmROW09? NGHDW45KSzVyPUGuPFgh|ryP MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
LP1 M362OmZ2dmO2aX;uJGF{e2G7 NGfKepIyyqEQvF2= M1zQ[VI1KGh? MVnlcohidmOnczC1MWFENWmwZIXj[YQhVUGJRT3BN{Bo\W6nIHX4dJJme3Orb36= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF5MUiyNUc,OjFzN{G4NlE9N2F-
ANBL6  M2T3SWZ2dmO2aX;uJGF{e2G7 NFjzWYwyyqEQvF2= NVG4PIl[OjRiaB?= MY\lcohidmOnczC1MWFENWmwZIXj[YQhVUGJRT3BN{Bo\W6nIHX4dJJme3Orb36= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF5MUiyNUc,OjFzN{G4NlE9N2F-
HMEC M3zCdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2D2bmlEPTB;MUmg{txO Mn7sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MUe0OVUoRjJzM{G3OFU2RC:jPh?=
SW620 NIjNWFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFizszN MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF|MUe0OVU9N2F-
SW48 NIDlTYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFqzUJBKSzVyPUCuPEDPxE1? MlrZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MUe0OVUoRjJzM{G3OFU2RC:jPh?=
HT-29 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorMTWM2OD1yLkeg{txO NX\0O5lbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNVc1PTVpPkKxN|E4PDV3PD;hQi=>
HCT15 M1G2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHuTWM2OD1yLkeg{txO MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF|MUe0OVU9N2F-
PAXF 1657L† NGjYRm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnXSWM2OD1yLkOg{txO NYizcmIyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|U3PzlpPkKxN|c2Pjd7PD;hQi=>
PAXF 546L† MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTiSWM2OD1zLkWg{txO M{fqSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
Panc-1 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;hXFRGSzVyPUGuPEDPxE1? M{jGeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
MiaPaca-2 M{HJSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn1[WhqTUN3ME2wMlYh|ryP MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
AsPC-1 NWTWWlUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHLSWM2OD1|Lkmg{txO MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
BxPC-3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;ONWVEPTB;MT6xJO69VQ>? MlnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{W2O|koRjJzM{e1Olc6RC:jPh?=
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HepG2 NUHhXm9xSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M37PZlczKGi{cx?= NUPTXpZNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01NjJ3zszN NHHifW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK|5EcEWPQly8M4E,
HepG2 NX7Xd5lQSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MnLJNlQhcHK| MkPrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME21Mlc6|ryP Mn6yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
A549 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NYLjOWF{PzJiaILz M4S2b2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNU45P87:TR?= NVjac243RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
A549 M4K2VWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mk\2OFghcHK| MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUSuOVfPxE1? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|I6QDBxJ{7DbGVOSkx:L3G+
HCT116 M4LTV2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NWHxZ|NUOjRiaILz M4D1OmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI6NjZ7zszN M3;BSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4Ojl6MD:nQmNpTU2ETEyvZV4>
HeLa NFvXTnpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFPkPYUzPCCqcoO= NH[5[mJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFMvQM7:TR?= NUjHcZNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Bad / Bid / Bak / Puma / Bax / Cleaved caspase-9 / Cleaved caspase-3 / Cleaved PARP; 

PubMed: 27551526     


(a and b) DU-145 cells were treated with various doses of mocetinostat for 24 h. Western blotting was performed using the indicated antibodies. 

Ac-H3 / Ac-H4 / Ac-tubulin ; 

PubMed: 29186204     


Mocetinostat increased acetylated histone 3 and 4 in a time- and dose-dependent manner in LMS cells. Mocetinostat did not increase acetylated tubulin expression.

27551526 29186204
Immunofluorescence
E-cadherin / ZEB1 ; 

PubMed: 25872941     


Immunoblot and immunofluorescence showing that mocetinostat treatment (1 μM, 48 h) reduced ZEB1 expression and induced E-cadherin in Panc1. Expression of histone deacetylases was not altered by mocetinostat, but histone acetylation was induced. Scale bar 10 μm.

Nanog / MHC ; 

PubMed: 26240433     


c-Kit+ cells were treated with 2 µM MOCE for 2 or 7 days, as indicated. The cells were double-labeled with anti-Nanog (green) and anti-αMHC (red) antibodies. Nuclei were stained with DAPI (blue). The upper right section of each panel shows the enlargement of the box-selected area. Scale bars = 20 µm.

25872941 26240433
Growth inhibition assay
Cell viability; 

PubMed: 26378038     


B. Cells were treated with increasing concentrations of mocetinostat for 48 hours and assayed by the WST-1 cell viability assay. C. IC50 values were calculated by the GraphPad Prism software. 

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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 携带H1437肿瘤的雌性CD-1裸鼠
  • Dosages: 80 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 13 mg/mL (32.79 mM)
Water Insoluble
Ethanol Insoluble
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 粉状
溶于溶剂
别名 MG0103

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 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID