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 93 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  MVLBdI9xfG:|aYOgRZN{[Xl? MoruNE42NzJxMzFOwG0> M1fwNlI1NzR6IHi= NX;hWoRncW6mdXPld{BieG:ydH;zbZMh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NUfC[FRGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0NFY6PDdpPkKwOFA3QTR5PD;hQi=>
HeLa  NXLQZpFtTnWwY4Tpc44hSXO|YYm= MWOxNEDPxE4EoB?= MlrDO{Bp NFv0U2pFVVOR Ml;V[Il{enWydIOgco9zdWGuIIPwbY5ldGViY3jlZ4txd2mwdDDmeY5kfGmxbh?= NITNUGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWzPFg1OCd-MkC1N|g5PDB:L3G+
HeLa NHr2NW1HfW6ldHnvckBCe3OjeR?= MV:xNEDPxE4EoB?= M3HVO|YwOTJxMkSgbC=> MonKSG1UVw>? MlK3bY5lfWOnczDtbZRwfGmlIHHjZ5VufWyjdHnvckBidmRiZHXsZZlm\CCyMkGg[ZhxemW|c3nvci=> M2fWZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUO4PFQxLz5{MEWzPFg1ODxxYU6=
HeLa MYnGeY5kfGmxbjDBd5NigQ>? MoXaNE4{NTFyIN88US=> M{H2bVghcA>? NEXEV3dFVVOR M2fZdIlv[3KnYYPld{Bk[XOyYYPlJFMh[W6mIEegZYN1cX[jdHnvckBld3OnIHTldIVv\GWwdHz5 NUXrWplGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N|g5PDBpPkKwOVM5QDRyPD;hQi=>
HeLa NGDoXlBHfW6ldHnvckBCe3OjeR?= NW\mWYNWOC5|LUGwJO69VQ>? NXTzNo9NQCCq NUPiXYhoTE2VTx?= NFzRfWRqdmO{ZXHz[ZMh[WOndInsZZRm\CCKMzDLPUApUDONOVHjLUBifCBzMDFOwG0> NV;TRmY3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1N|g5PDBpPkKwOVM5QDRyPD;hQi=>
DMS114 M3zXeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTZ2MDDuUS=> M4SyVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H82 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTDfYQ3UUN3ME2yOVAhdk1? M1XnTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkiyOlQ{Lz5{ME[4NlY1OzxxYU6=
H146 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLkU3BVUUN3ME2zOUBvVQ>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ6Mk[0N{c,OjB4OEK2OFM9N2F-
H526 M3fB[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XSZmlEPTB;NEiwJI5O NXnsO4x3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFI3PDNpPkKwOlgzPjR|PD;hQi=>
KM-H2 NVrzdWVSTnWwY4Tpc44hSXO|YYm= M2[5VlHDqM7:TR?= MU[wMlI2NTR6IHi= NYi5PXU5TE2VTx?= NX\5ephs[WO2aY\heIV{KE6ILXvC M{frO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
L428 MWrGeY5kfGmxbjDBd5NigQ>? NYjEWJQ4OcLizszN Mly4NE4zPS12ODDo NF64dVdFVVOR M{LhS4FkfGm4YYTld{BPTi2tQh?= Mmn0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2 NH7VVWdHfW6ldHnvckBCe3OjeR?= MlPrNeKh|ryP M3rWTFAvOjVvNEigbC=> NX62cZRLTE2VTx?= M1riSIFkfGm4YYTld{BPTi2tQh?= M3;SU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 NVntPWl{TnWwY4Tpc44hSXO|YYm= NEHqNWQxNjVxMTFOwG0> NV3XRpVWOjRxNEigbC=> NWTocpc3TE2VTx?= MV\1dJJm\3WuYYTld{BVVkZvzsGg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= Ml;QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 MWLGeY5kfGmxbjDBd5NigQ>? NEe3OXkxNjVxMTFOwG0> M2e1U|I1NzR6IHi= NELDfFlFVVOR M3jNNpVxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NVjkOYFrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 MoniSpVv[3Srb36gRZN{[Xl? NV;0c5REOC53L{Gg{txO NXnWd2xiOjRxNEigbC=> NGTNdJJFVVOR M3Xld5VxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NIC4cGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
KM-H2 NFj3[m1HfW6ldHnvckBCe3OjeR?= NIXTTIUyyqEQvF2= MVWyOE81QCCq MVzEUXNQ NYi4O4sx\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? MnroQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
L428 MorqSpVv[3Srb36gRZN{[Xl? M{foe|HDqM7:TR?= MnjZNlQwPDhiaB?= MmnnSG1UVw>? NVrGbnNb\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? NUL1OXpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
HD-LM2 M4HaWWZ2dmO2aX;uJGF{e2G7 Mlu1NeKh|ryP M{ThTlI1NzR6IHi= M1uybWROW09? NHLITnRld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ NYHT[o91RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2 MUHBdI9xfG:|aYOgRZN{[Xl? NFHOTm0xNjFxMD61M|Eh|ryP MoC2OFghcA>? NHW4bFNFVVOR M2Hjbolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NVXDbWZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 MlHoRZBweHSxc3nzJGF{e2G7 MmjnNE4yNzBwNT:xJO69VQ>? Mkf3OFghcA>? M2XZdGROW09? NYrxbXBkcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODh6MEGwO{c,OjB6OECxNFc9N2F-
HD-LM2 NIr3[45CeG:ydH;zbZMhSXO|YYm= NW\GSmFvOC5zL{CuOU8yKM7:TR?= MnrGOFghcA>? MWrEUXNQ MWHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NYjDdoJNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
KM-H2 MVPGeY5kfGmxbjDBd5NigQ>? NGSyN28xNjFvMjFOwG0> NV7JOZI3OjRiaNMg NIXBNVFFVVOR MoPhd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= NUDGfVc1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC4PFAyODdpPkKwPFgxOTB5PD;hQi=>
L428 MoKySpVv[3Srb36gRZN{[Xl? MWCwMlEuOiEQvF2= NU\CSVZlOjRiaNMg M2\pPWROW09? MV3zbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz MlfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2 M4XnRmZ2dmO2aX;uJGF{e2G7 M{\rRlAvOS1{IN88US=> NHTpOlgzPCCqwrC= NGi3W2hFVVOR NICxeod{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx M4q5WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEiwNVA4Lz5{MEi4NFExPzxxYU6=
KM-H2 NELSN49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTsUFkxPzMEoHi= NVrG[WIzTE2VTx?= MWLJR|UxRTJwOE[g{txO NIrwUlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
L428 M4LFVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPNTVU4PzMEoHi= NUPtVY81TE2VTx?= NVnZdHFKUUN3ME2xMlk3KM7:TR?= MoPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB6OECxNFcoRjJyOEiwNVA4RC:jPh?=
HD-LM2 MkHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIn0WHA4OsLiaB?= NUPFNW5lTE2VTx?= MUTJR|UxRTFwOEig{txO NEXhPZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEi4NFExPyd-MkC4PFAyODd:L3G+
LP1 M2mwfWZ2dmO2aX;uJGF{e2G7 MWOxxsDPxE1? M1e3UVI1KGh? NELXZZhmdmijbnPld{A2NUGFLXnu[JVk\WRiTVHHSU1COyCpZX7lJIV5eHKnc4Ppc44> MlzSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFzN{G4NlEoRjJzMUexPFIyRC:jPh?=
ANBL6  MlPCSpVv[3Srb36gRZN{[Xl? MUexxsDPxE1? M2XNXVI1KGh? NYTVbVRS\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v M4\HOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMUexPFIyLz5{MUG3NVgzOTxxYU6=
HMEC MlflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fPemlEPTB;MUmg{txO NET4UXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO|Q2PSd-MkGzNVc1PTV:L3G+
SW620 Mnq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTFizszN MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF|MUe0OVU9N2F-
SW48 NWXKTWM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LIXmlEPTB;MD64JO69VQ>? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzN{S1OUc,OjF|MUe0OVU9N2F-
HT-29 Mn\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PWTmlEPTB;MD63JO69VQ>? Mnq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MUe0OVUoRjJzM{G3OFU2RC:jPh?=
HCT15 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTrd|ZkUUN3ME2wMlch|ryP NIC5VWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUOxO|Q2PSd-MkGzNVc1PTV:L3G+
PAXF 1657L† MkCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj3e4pzTUN3ME2wMlMh|ryP M33DN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e1Olc6Lz5{MUO3OVY4QTxxYU6=
PAXF 546L† MnW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PiS2VEPTB;MT61JO69VQ>? NFjNfI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3OVY4QSd-MkGzO|U3Pzl:L3G+
Panc-1 MmfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3W5e2VEPTB;MT64JO69VQ>? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
MiaPaca-2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ezNGVEPTB;MD62JO69VQ>? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
AsPC-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7POYlrTUN3ME2zMlkh|ryP MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
BxPC-3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETMeoNGSzVyPUGuNUDPxE1? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5NU[3PUc,OjF|N{W2O|k9N2F-
MMCs NFXmR3RHfW6ldHnvckBCe3OjeR?= M1PoTFHDqM7:TR?= MWS2MVI1KGh? NWDSfHpT\G:|ZT3k[ZBmdmSnboTsfUBqdmirYnn0d{B1cGVidILpcYV1cHmuYYTpc44hdGW4ZXygc4YhUDNvS{mgLGg{NUt7bXWzLS=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR3MUO3PEc,OjR2NUGzO|g9N2F-
MMCs Mn3YSpVv[3Srb36gRZN{[Xl? MnSyNeKh|ryP NYfYXmV[OjRiaB?= NXvNcJRZ[XWpbXXueJMh\2yxYnHsJIFk\XS7bHH0bY9vKGyndnXsd{Bw\iCqaYP0c45mKEh|LVu5M|E1KCiKMz3LPU8yPGGlKTDhcoQhUDRvS{GyJEhJPC2NMULhZ{k> NVL3[W85RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OVE{PzhpPkK0OFUyOzd6PD;hQi=>
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A549 Mn\zRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MUW3NkBpenN? NH[zRYRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NVEvQDgQvF2= M1L0Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4Ojl6MD:nQmNpTU2ETEyvZV4>
A549 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoH5OFghcHK| Mm[3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUG0MlU4|ryP NXWwdZRqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
HCT116 M{i5WmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mn;sNlQhcHK| MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgNlQhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2yPU43Qc7:TR?= NYfsTmpTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd{OUiwM{c,S2iHTVLMQE9iRg>?
HeLa NULaNGpiSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NIjPU2ozPCCqcoO= MljQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSzMljPxE1? NI[5Z|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzJ7OECvK|5EcEWPQly8M4E,
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
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: Female CD-1 nude mice bearing H1437 tumors
  • Dosages: 80 mg/kg
  • Administration: Administered via p.o.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 13 mg/mL
(32.79 mM)
Water Insoluble
Ethanol Insoluble

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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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