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 3862.98 现货
RMB 6314.53 现货
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客户使用Selleck生产的Mocetinostat (MGCD0103)发表文献85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  MXfBdI9xfG:|aYOgRZN{[Xl? M3LGOFAvPS9{L{Og{txO MmrvNlQwPDhiaB?= MVvpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODRyNkm0O{c,OjB2ME[5OFc9N2F-
HeLa  MVHGeY5kfGmxbjDBd5NigQ>? MlzqNVAh|ryPwrC= NHXBTI04KGh? NGDKTZpFVVOR MWTkbZNzfXC2czDuc5Ju[Wxic4DpcoRt\SClaHXjb5BwcW62IH\1coN1cW:w NF[ye|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWzPFg1OCd-MkC1N|g5PDB:L3G+
HeLa MmC4SpVv[3Srb36gRZN{[Xl? M4f3UFExKM7:TdMg M3:ydVYwOTJxMkSgbC=> NXnXSZFPTE2VTx?= NWTrU41ZcW6mdXPld{BucXSxdHnjJIFk[3WvdXzheIlwdiCjbnSg[IVt[XmnZDDwNlEh\XiycnXzd4lwdg>? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa M2PzXGZ2dmO2aX;uJGF{e2G7 M{TzNlAvOy1zMDFOwG0> M3L2SFghcA>? MVTEUXNQ MWXpcoNz\WG|ZYOgZ4F{eGG|ZTCzJIFv\CB5IHHjeIl3[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= NX3PeY9nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N|g5PDBpPkKwOVM5QDRyPD;hQi=>
HeLa Ml74SpVv[3Srb36gRZN{[Xl? MkjhNE4{NTFyIN88US=> NFfzZZU5KGh? MUfEUXNQ MkjSbY5kemWjc3XzJIFk\XS7bHH0[YQhUDNiS{mgLGg{UzmDYzmgZZQhOTBizszN NUD2TnpzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N|g5PDBpPkKwOVM5QDRyPD;hQi=>
DMS114 NFLjdXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTZ2MDDuUS=> M2DJc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H82 M134SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETxTG9KSzVyPUK1NEBvVQ>? NX\i[FZkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFI3PDNpPkKwOlgzPjR|PD;hQi=>
H146 M3[4cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jUcWlEPTB;M{Wgcm0> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ6Mk[0N{c,OjB4OEK2OFM9N2F-
H526 NInicGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTR6MDDuUS=> NYT1[YlZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFI3PDNpPkKwOlgzPjR|PD;hQi=>
KM-H2 M4TzdGZ2dmO2aX;uJGF{e2G7 MV6xxsDPxE1? MmizNE4zPS12ODDo MorsSG1UVw>? NXTKTmk3[WO2aY\heIV{KE6ILXvC NU\NS5d7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 NWXpPGd4TnWwY4Tpc44hSXO|YYm= MmSwNeKh|ryP MUSwMlI2NTR6IHi= M4L5TWROW09? MkK0ZYN1cX[jdHXzJG5HNWuE NEixRpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
HD-LM2 MYPGeY5kfGmxbjDBd5NigQ>? NY\vbI5nOcLizszN NYjVWoppOC5{NT20PEBp M1\BVmROW09? NEPv[I9i[3SrdnH0[ZMhVkZva1K= Mnf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
KM-H2 NF23WYpHfW6ldHnvckBCe3OjeR?= NEf4NG4xNjVxMTFOwG0> NYfPO4xnOjRxNEigbC=> NHm1VHdFVVOR NHP6d5B2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NX\FZXV5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 MWnGeY5kfGmxbjDBd5NigQ>? NHfCelcxNjVxMTFOwG0> M3KzW|I1NzR6IHi= NYLlXY9ITE2VTx?= NWTpZXVnfXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2 MYPGeY5kfGmxbjDBd5NigQ>? MVSwMlUwOSEQvF2= MonKNlQwPDhiaB?= NHG0Xo5FVVOR M2TERpVxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NEP3VIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
KM-H2 MXXGeY5kfGmxbjDBd5NigQ>? MWKxxsDPxE1? NHLwc|kzPC92ODDo NEntXYVFVVOR M3XrZYRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> NXPzclVHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 Mn[3SpVv[3Srb36gRZN{[Xl? M4PWXVHDqM7:TR?= MWOyOE81QCCq NFzZNWRFVVOR NYPsfWh[\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2 MYjGeY5kfGmxbjDBd5NigQ>? MWCxxsDPxE1? NGnYO2IzPC92ODDo NX3GS5NlTE2VTx?= NU\sWIE{\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? NXmxZYtKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2 MX3BdI9xfG:|aYOgRZN{[Xl? MmntNE4yNzBwNT:xJO69VQ>? M{C1WlQ5KGh? NEm3fYpFVVOR Mnm1bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M3vkTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428 M3i3cWFxd3C2b4Ppd{BCe3OjeR?= M{DS[|AvOS9yLkWvNUDPxE1? M2S2dVQ5KGh? NFnuO2lFVVOR Mo\qbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NH\N[m89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
HD-LM2 MoTHRZBweHSxc3nzJGF{e2G7 M3jMelAvOS9yLkWvNUDPxE1? M1XyZ|Q5KGh? MUfEUXNQ NX:0PYxVcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> Ml3XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
KM-H2 NFfsW4FHfW6ldHnvckBCe3OjeR?= MlntNE4yNTJizszN NYXvW5RWOjRiaNMg NFzv[2VFVVOR NEHNeIx{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx M1K3OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428 M3XTU2Z2dmO2aX;uJGF{e2G7 MljENE4yNTJizszN MkjENlQhcMLi NVvpOog3TE2VTx?= M1WwcJNpd3e|IHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhOyCjbnSgeZBz\We3bHH0bY9vKG:oIITo[UBk\WyuIHP5Z4xmKHKnZ4XsZZRwenlicILveIVqdiCyMkG= NEn6cGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
HD-LM2 NUH5RY1rTnWwY4Tpc44hSXO|YYm= NIq5PIcxNjFvMjFOwG0> MlTvNlQhcMLi NUPiXlVMTE2VTx?= NYXaSXNqe2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=> NVL0UnQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2 NXL1fGEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zHXFczyqCq NXPuUG1tTE2VTx?= M1LjOmlEPTB;Mj64OkDPxE1? NYD4V4drRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 MnXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoW5O|LDqGh? NEXo[mlFVVOR M1nkNmlEPTB;MT65OkDPxE1? NUD6dIo5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 NEfqbZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUW3NuKhcA>? NUHqPIM1TE2VTx?= M4C2RWlEPTB;MT64PEDPxE1? MlvHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
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ANBL6  NXjENHBnTnWwY4Tpc44hSXO|YYm= M{PZOlHDqM7:TR?= M4PZW|I1KGh? Mkf3[Y5p[W6lZYOgOU1CSy2rbnT1Z4VlKE2DR1WtRVMh\2WwZTDlfJBz\XO|aX;u M13qOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMUexPFIyLz5{MUG3NVgzOTxxYU6=
HMEC NWPhUY5xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj5SHdKSzVyPUG5JO69VQ>? M2T5flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{G3OFU2Lz5{MUOxO|Q2PTxxYU6=
SW620 M17md2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nYeWlEPTB;MTFOwG0> NY\kUlVVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzNVc1PTVpPkKxN|E4PDV3PD;hQi=>
SW48 NV;EZ5ByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnJ[XpDUUN3ME2wMlgh|ryP MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF|MUe0OVU9N2F-
HT-29 NIDKW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTlTWM2OD1yLkeg{txO NGC2dFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO|Q2PSd-MkGzNVc1PTV:L3G+
HCT15 NWL4d5F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwNzFOwG0> M4TK[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{G3OFU2Lz5{MUOxO|Q2PTxxYU6=
PAXF 1657L† M2jCPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHHeXBOTUN3ME2wMlMh|ryP NXz0NoVGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|U3PzlpPkKxN|c2Pjd7PD;hQi=>
PAXF 546L† MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojrSWM2OD1zLkWg{txO M1fzc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
Panc-1 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoK4SWM2OD1zLkig{txO MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
MiaPaca-2 NVzzfmJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfFR|UxRTBwNjFOwG0> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
AsPC-1 NXfVUZpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWf3SJhyTUN3ME2zMlkh|ryP MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
BxPC-3 MlXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfndFUzTUN3ME2xMlEh|ryP M3WxRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
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HepG2 NVXIR|c3SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MoK3NlQhcHK| NXP4RYc{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02Njd7zszN MoK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
A549 NUKyTW5LSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1nB[|czKGi{cx?= MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUGuPFfPxE1? NX;zPXo4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
A549 NWe2WYlJSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NELVeYI1QCCqcoO= NV21THV{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE1NjV5zszN MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|I6QDBxJ{7DbGVOSkx:L3G+
HCT116 MoeyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3;rTFI1KGi{cx?= M{jPc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI6NjZ7zszN NEfndJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK|5EcEWPQly8M4E,
HeLa NXLqOFZlSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4\yRlI1KGi{cx?= Mny0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSzMljPxE1? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|I6QDBxJ{7DbGVOSkx:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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.

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. 

29186204 27551526
Immunofluorescence
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.

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.

26240433 25872941
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、MSDS / 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、MSDS / 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