Mocetinostat (MGCD0103)

Catalog No.S1122 Synonyms: MG0103

For research use only.

Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.

Mocetinostat (MGCD0103) Chemical Structure

CAS No. 726169-73-9

Selleck's Mocetinostat (MGCD0103) has been cited by 97 publications

Purity & Quality Control

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Biological Activity

Description Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
Targets
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
In vitro

MGCD0103 inhibits only a subset of the nine human recombinant HDACs, including HDAC1, HDAC2, HDAC3, and HDAC11 at nanomolar or low micromolar concentrations, in a dose-dependent manner. MGCD0103 reveals most potent inhibitory activity against human HDAC1 and HDAC2 enzymes in vitro, and it does not inhibit class II HDACs. The exocyclic amino group in MGCD0103 is necessary for enzyme inhibitory activity because HDAC-inhibitory activity against HDAC1 and HDAC2 is completely abolished with the desamino analogue. The inhibitory activity of MGCD0103 reaches the maximum plateau at 6 μM, and the maximal inhibitable enzyme pool affected by MGCD0103 is 75% of the total enzyme activity in HCT116 cells whereas NVP-LAQ824 inhibits almost 100% of that in these cells. In A549 cells, MGCD0103 also exhibits dose-dependent inhibition of HDAC activity in whole cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PBMC  MliyRZBweHSxc3nzJGF{e2G7 NYHWO2NPOC53L{KvN{DPxE1? NVO3[G1bOjRxNEigbC=> NIniNHlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 Ml3OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB2ME[5OFcoRjJyNEC2PVQ4RC:jPh?=
HeLa  M3HrWWZ2dmO2aX;uJGF{e2G7 M{ezdVExKM7:TdMg NEC3cJM4KGh? NH:yOHZFVVOR M4XKd4Rqe3K3cITzJI5wem2jbDDzdIlv\GynIHPo[YNseG:rboSg[pVv[3Srb36= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa MnjFSpVv[3Srb36gRZN{[Xl? M3XwU|ExKM7:TdMg MVG2M|EzNzJ2IHi= M4PQVGROW09? M1Xvd4lv\HWlZYOgcYl1d3SrYzDhZ4N2dXWuYYTpc44h[W6mIHTlcIF6\WRicEKxJIV5eHKnc4Ppc44> NYDLepBLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N|g5PDBpPkKwOVM5QDRyPD;hQi=>
HeLa MVfGeY5kfGmxbjDBd5NigQ>? M3PjUVAvOy1zMDFOwG0> M4i4dFghcA>? NV3VSZhkTE2VTx?= MnrTbY5kemWjc3XzJINie3Cjc3WgN{BidmRiNzDhZ5RqfmG2aX;uJIRwe2ViZHXw[Y5l\W62bIm= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV|OEi0NEc,OjB3M{i4OFA9N2F-
HeLa MlvMSpVv[3Srb36gRZN{[Xl? M3jkblAvOy1zMDFOwG0> NVi5cHlbQCCq M{PuNWROW09? NWPrfIpXcW6lcnXhd4V{KGGlZYT5cIF1\WRiSEOgT|khMEh|S{nBZ{kh[XRiMUCg{txO NF25PIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWzPFg1OCd-MkC1N|g5PDB:L3G+
DMS114 Mnz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nScmlEPTB;NkSwJI5O M1;OblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H82 Mn7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYi0PW1zUUN3ME2yOVAhdk1? Mn7sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEK2OFMoRjJyNkiyOlQ{RC:jPh?=
H146 NFTtcnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfkeFdKSzVyPUO1JI5O M{n0SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H526 NHfDTGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDSeVdKSzVyPUS4NEBvVQ>? M1jBZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
KM-H2 M{PQTWZ2dmO2aX;uJGF{e2G7 M2XWUFHDqM7:TR?= M{\3cVAvOjVvNEigbC=> MV;EUXNQ NXn4UGU6[WO2aY\heIV{KE6ILXvC NYHPOoRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 MVPGeY5kfGmxbjDBd5NigQ>? NIK1V40yyqEQvF2= NGC0WVMxNjJ3LUS4JIg> NEmwTFhFVVOR NInQcJRi[3SrdnH0[ZMhVkZva1K= NEH6dXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
HD-LM2 NVnFeoR[TnWwY4Tpc44hSXO|YYm= MVyxxsDPxE1? Mne1NE4zPS12ODDo M2Gxc2ROW09? NHTyOXdi[3SrdnH0[ZMhVkZva1K= M3;MTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 Ml;JSpVv[3Srb36gRZN{[Xl? NYmxV2kyOC53L{Gg{txO NEDUSoYzPC92ODDo MVfEUXNQ MnPteZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= Ml61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 Mk\RSpVv[3Srb36gRZN{[Xl? M{XuPFAvPS9zIN88US=> MXKyOE81QCCq MW\EUXNQ M2LQZZVxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MlTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2 MVrGeY5kfGmxbjDBd5NigQ>? NFfJfpYxNjVxMTFOwG0> MmTFNlQwPDhiaB?= MY\EUXNQ MlS3eZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2 MX\GeY5kfGmxbjDBd5NigQ>? NFuxbHQyyqEQvF2= NVfwW2xPOjRxNEigbC=> MV3EUXNQ NV2xTHNo\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? Mmq5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 NEDKSmVHfW6ldHnvckBCe3OjeR?= M3v0flHDqM7:TR?= M2TLZ|I1NzR6IHi= M4iz[GROW09? NYDzT2Jw\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2 MnToSpVv[3Srb36gRZN{[Xl? NXTDVmRMOcLizszN NXzGcng3OjRxNEigbC=> NI\Bd2VFVVOR NXHRVXdC\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
KM-H2 NELVOm1CeG:ydH;zbZMhSXO|YYm= M3LxWFAvOS9yLkWvNUDPxE1? MlPlOFghcA>? M3;OWGROW09? NWjQZZpMcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NEnK[5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
L428 NFXXbINCeG:ydH;zbZMhSXO|YYm= M37WS|AvOS9yLkWvNUDPxE1? MYW0PEBp M2frfGROW09? NX7CcGxncW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2 NWTYe|BsSXCxcITvd4l{KEG|c3H5 MoLzNE4yNzBwNT:xJO69VQ>? MX[0PEBp NHLZRmhFVVOR NUjjZ2lPcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NVf0Z2lrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2 NVTVbmxUTnWwY4Tpc44hSXO|YYm= NXjuSmtTOC5zLUKg{txO MYiyOEBpyqB? NGjZc5lFVVOR M1THS5Npd3e|IHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhOyCjbnSgeZBz\We3bHH0bY9vKG:oIITo[UBk\WyuIHP5Z4xmKHKnZ4XsZZRwenlicILveIVqdiCyMkG= M4DD[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428 NXfuNHNRTnWwY4Tpc44hSXO|YYm= NYPySWVqOC5zLUKg{txO M4LwNFI1KGkEoB?= NImwUmVFVVOR MUfzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz NXPyboJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 M1S2UmZ2dmO2aX;uJGF{e2G7 MkfPNE4yNTJizszN M2nTTFI1KGkEoB?= MonRSG1UVw>? MnSxd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= M2G1[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37BcVczyqCq M1r6W2ROW09? NFHLbW1KSzVyPUKuPFYh|ryP MojRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 M3zrdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXW3NuKhcA>? NEXiS3FFVVOR Mmr4TWM2OD1zLkm2JO69VQ>? NX3tcHFIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUC3NuKhcA>? M1PSW2ROW09? NWT1TFFtUUN3ME2xMlg5KM7:TR?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
LP1 NWe2[JdwTnWwY4Tpc44hSXO|YYm= NV7t[WEyOcLizszN M1y0T|I1KGh? M2fDXoVvcGGwY3XzJFUuSUNvaX7keYNm\CCPQVfFMWE{KGenbnWg[ZhxemW|c3nvci=> NX\sS484RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGxO|E5OjFpPkKxNVcyQDJzPD;hQi=>
ANBL6  NUL4OlhETnWwY4Tpc44hSXO|YYm= Ml7SNeKh|ryP NVf4RWVOOjRiaB?= NVfXRoFb\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF5MUiyNUc,OjFzN{G4NlE9N2F-
HMEC M{nkeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTmVGRKSzVyPUG5JO69VQ>? M1\wSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{G3OFU2Lz5{MUOxO|Q2PTxxYU6=
SW620 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTFizszN NELkWZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO|Q2PSd-MkGzNVc1PTV:L3G+
SW48 M2K0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nPTWlEPTB;MD64JO69VQ>? M{XwfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{G3OFU2Lz5{MUOxO|Q2PTxxYU6=
HT-29 M3W5Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzmdJpHUUN3ME2wMlch|ryP M1TLUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{G3OFU2Lz5{MUOxO|Q2PTxxYU6=
HCT15 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fnSmlEPTB;MD63JO69VQ>? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF|MUe0OVU9N2F-
PAXF 1657L† NVfCNHFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3z[pVGSzVyPUCuN{DPxE1? MkjkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{W2O|koRjJzM{e1Olc6RC:jPh?=
PAXF 546L† M1nSXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHKeYJGSzVyPUGuOUDPxE1? NYXWcI4yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|U3PzlpPkKxN|c2Pjd7PD;hQi=>
Panc-1 NXG0R5ZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLMSWM2OD1zLkig{txO MnHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{W2O|koRjJzM{e1Olc6RC:jPh?=
MiaPaca-2 NH\6NnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoD1SWM2OD1yLk[g{txO NVj3XIxXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|U3PzlpPkKxN|c2Pjd7PD;hQi=>
AsPC-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLwSWM2OD1|Lkmg{txO MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
BxPC-3 NGG4[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnpPVBGSzVyPUGuNUDPxE1? NIX5emU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3OVY4QSd-MkGzO|U3Pzl:L3G+
MMCs NVrlTWdTTnWwY4Tpc44hSXO|YYm= NHXzVmIyyqEQvF2= Mk\wOk0zPCCq Mnzj[I9{\S2mZYDlcoRmdnSueTDpcohq[mm2czD0bIUhfHKrbXX0bJlt[XSrb36gcIV3\Wxib3[gTFMuUzliKFizMWs6dWV|KR?= NFTlVJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES1NVM4QCd-MkS0OVE{Pzh:L3G+
MMCs NF\ydI9HfW6ldHnvckBCe3OjeR?= M4fVcVHDqM7:TR?= NGGzTYIzPCCq MVLheYdu\W62czDncI9j[WxiYXPleJlt[XSrb36gcIV3\Wy|IH;mJIhqe3SxbnWgTFMuUzlxMUSgLGg{NUt7L{G0ZYMqKGGwZDDIOE1MOTJiKFi0MWsyOmGlKR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR3MUO3PEc,OjR2NUGzO|g9N2F-
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A549 NXL4NXdnSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M{XwRlczKGi{cx?= M{XGdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNU45P87:TR?= MnHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
A549 MlHJRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MY[0PEBpenN? M{PRUGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xOE42P87:TR?= MlfIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HCT116 NVTuWmJYSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MYOyOEBpenN? M2fDfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI6NjZ7zszN MnXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlczQThyLze+R4hGVUKOPD;hQi=>
HeLa M33VfmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MkfjNlQhcHK| MlrQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSzMljPxE1? NUnodHlqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
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
In vivo MGCD0103 significantly inhibites growth of human tumor xenografts in nude mice and the antitumor activity correlated with induction of histone acetylation in tumors. P.O. administration of MGCD0103 (2HBr salt) significantly decreases growth of implanted advanced A549 tumors in nude mice in a dose-dependent manner after 13 days of daily administration. MGCD0103 (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blockes growth of tumors compared with vehicle treatment alone with no change in body weight. In addition, MGCD0103 does not reduce WBC counts and is well tolerated. MGCD0103 is also orally active in many other human tumor xenograft models including NSCLC H1437. MGCD0103 at 80 mg/kg (free base) almost completely blocks the growth of H1437 tumors after 13 days of daily p.o. administration with no reduction of body weight in animals. [1] MGCD0103 reduces pulmonary arterial pressure more dramatically than tadalafil, a standard-of-care therapy for human pulmonary hypertension that functions as a vasodilator. Moreover, MGCD0103 improves pulmonary artery acceleration time and reduced systolic notching of the pulmonary artery flow envelope, which suggests a positive impact of the HDAC inhibitor on pulmonary vascular remodeling and stiffening. [2]

Protocol (from reference)

Kinase Assay:[1]
  • HDAC enzyme assay in vitro:

    The deacetylase enzyme assay is based on a homogeneous fluorescence release assay. Purified recombinant HDAC enzymes are incubated with MGCD0103 diluted in various concentrations for 10 minutes in assay buffer [25 mM HEPES (pH 8.0), 137 mM NaCl, 1 mM MgCl2, 2.7 mM KCl] at room temperature. The substrate Boc-Lys(ε-Ac)-AMC is added to the reaction for further incubation at 37 °C. The concentration of the substrate and the incubation time varies for different isotypes of HDAC enzymes. A 20-min trypsin incubation at room temperature allows the release of the fluorophore from the deacetylated substrate. The fluorescent signal is detected by fluorometer at excitation of 360 nm, emission of 470 nm, and cutoff at 435 nm.

Cell Research:[1]
  • Cell lines: Human mammary epithelial cells (HMEC), human foreskin fibroblasts (MRHF) cells
  • Concentrations: 0-60 μM
  • Incubation Time: 72 hours
  • Method: Human mammary epithelial cells (HMEC) and human foreskin fibroblasts (MRHF) cells in 96-well plates are incubated with MGCD0103 at various concentrations for 72 hours at 37 °C in 5% CO2. MTT is added at a final concentration of 0.5 mg/ml and incubated with the cells for 4 hours before an equal volume of solubilization buffer [50% N,N-dimethylformamide, 20% SDS (pH 4.7)] is added. After overnight incubation, solubilized dye is quantified by reading at 570 nm using a reference at 630 nm. Absorbance values are converted to cell numbers according to a standard growth curve of the relevant cell line. The concentration which reduces cell numbers to 50% relative to DMSO-treated cells is determined as MTT IC5
Animal Research:[1]
  • Animal Models: Female CD-1 nude mice bearing H1437 tumors
  • Dosages: 80 mg/kg
  • Administration: Administered via p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% Propylene glycol
For best results, use promptly after mixing.

30mg/mL

Chemical Information

Molecular Weight 396.44
Formula

C23H20N6O

CAS No. 726169-73-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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