Mocetinostat (MGCD0103)

Catalog No.S1122 Synonyms: MG0103

Mocetinostat (MGCD0103) Chemical Structure

Molecular Weight(MW): 396.44

Mocetinostat (MGCD0103) 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. Phase 2.

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In DMSO USD 190 In stock
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6 Customer Reviews

  •  

    Comparison of MCAS ovarian cancer cells harboring control and CtBP2 knockdown shRNAs for sensitivity to chemotherapeutic agents. For each cell line, the MTT reading of the untreated cells was assigned as 100%. HDAC inhibitors: (a) Trichostatin A; (b) Vorinostat; (c) Belinostat; (d) MGCD0103; (e) valproic acid; and (f ) carboplatin, a non-HDAC inhibitor.

    Oncogene 2012 32, 3896-903. Mocetinostat (MGCD0103) purchased from Selleck.

    Class-specific histone deacetylase inhibition ameliorates cholesterol accumulation. Mutant fibroblasts (NPC-26) were incubated for 18 h in the presence of the HDAC class-specific inhibitors MC1568 and MGCD0103 (5 μM) and assessed for cholesterol accumulation by filipin fluorescence. Quantification of filipin fluorescence is expressed as arbitrary units. *, p<0.05, treated versus untreated cells by two-tailed Student,s t test.

    J Biol Chem 2011 286, 23842–23851. Mocetinostat (MGCD0103) purchased from Selleck.

  •  

    HDACI sensitivities in pancreatic cancer cell lines and the HPDE cells. Panels A–C: PANC-1 cells were harvested and lysed after incubation with a range of concentrations of MGCD0103 (0–1.0 uM), MC1568 (0–10 uM), or Tubastatin A (0–4 uM) for 96 h. Soluble proteins were analyzed on Western blots probed by anti-acetylated (ac)-H4, -H4, -ac-tubulin, or –b-actin antibody. Panel D: AsPC-1, BxPC-3, PANC-1, or the HPDE cells were cultured at 37’C for 96 h in complete medium in 96-well plates, with a range of concentrations of MGCD0103, MC1568, or Tubastatin A, and cell viabilities were determined using the MTT reagent.

    PLoS One 2012 7, e52095. Mocetinostat (MGCD0103) purchased from Selleck.

    HDACIs That Simultaneously Inhibit HDACs 1 and 6 Showed Greater Antileukemic Activities than HDACIs that Don,t at Cmax Concentrations. THP-1 cells were treated with LBH-589, PXD101, SAHA, VPA, MS-275 and MGCD0103 at Cmax concentrations for 3 h and 24 h, respectively. The cells post 3 h treatments were washed three times with complete medium and divided into two halves. One half of the cells was resuspended in complete media and cultured for up to 24 h to determine the effects of the 3 h treatments on cell proliferation and apoptosis. The other half of the cells was used to prepare whole cell lysates. Whole cell lysates from the 3 h and 24 h treatments were extracted and subjected to Western blots probed by anti-ac-tubulin or-β-actin antibody (panels A&B), or subjected to HDAC1 enzymatic assays post IP as described in the Materials and Methods (Panels C&D). The effects of the 3 h and 24 h HDACI treatments on cell proliferation, as reflected by percent decrease of live cells relative to untreated cells (panel E), and apoptosis (panel F) were determined by flow cytometry analysis as described in the Materials and Methods.

     

     

    PLoS One 2011 6, e17138. Mocetinostat (MGCD0103) purchased from Selleck.

  • Induction of DNA Damage and Bim Is Critical for HDACI-Induced Apoptosis in Pediatric AML Cells. THP-1 cells were treated with the HDACIs at Cmax concentrations for 3 (panel A) and 24 h (panel B), respectively. Whole cell lysates were extracted and subjected to Western blots probed by anti-p21, -c-Myc, -cH2AX, -Bim, or -b-actin antibody.

     

     

    PLoS One 2011 6, e17138. Mocetinostat (MGCD0103) purchased from Selleck.

    Western blot analysis of Acetyl-H3 and H3. 0-20μM MGCD0103 was added.

     

     

    Dr. Zhang of Tianjin Medical University. Mocetinostat (MGCD0103) purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Mocetinostat (MGCD0103) 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. 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
MDA-MB-231 M2PVV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljOOFghcA>? NI\ueZBKSzVyPUOuNFQh|ryP NWizSIoyOjZ|N{iwN|g>
BT549 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXq0PEBp NXzLeop[UUN3ME20MlM5KM7:TR?= MY[yOlM4QDB|OB?=
MCF7 M4TQVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVq0PEBp NWTYXHp4UUN3ME2wMlY4KM7:TR?= NYPjO3l1OjZ|N{iwN|g>
T47D MoXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF[5[3U1QCCq NHjqWJlKSzVyPUGuNVch|ryP Mk\rNlY{PzhyM{i=
MOLP8 NUKwXHBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvxXGxXPDhiaB?= MYnJR|UxRTBwNtMxJFAvODUQvF2= Mon6NlYxQTF3MUi=
Panc1 MV3GeY5kfGmxbjDBd5NigQ>? Ml\aNE42NzFxMj61JO69VQ>? MYi0PEBp MWTEUXNQ MXz1dJJm\3WuYYTld{BucVJvMkCz NIjGXpUzPTh5Mkm0NS=>
Panc1 NGXkU45HfW6ldHnvckBCe3OjeR?= MormNE42NzFxMj61JO69VQ>? NIK5W3k1QCCq MXzEUXNQ NX\RbFFzemWmdXPld{BmgHC{ZYPzbY9vKG:oIGrFRlEhd25iYn;0bEBuWk6DIHHu[EBxem:2ZXnuJIxmfmWuwrC= M2Dj[|I2QDd{OUSx
Panc1 MlnaRZBweHSxc3nzJGF{e2G7 MnX0NeKh|ryP NU\le3prPzMEoHi= MorySG1UVw>? NH\DWWx{\W6|aYTpfoV{KFCjbnOxJINmdGy|IH\vdkBo\W2laYThZolv\S2rbnT1Z4VlKGGyb4D0c5Nqew>? NGrNR2QzPTh5Mkm0NS=>
Panc1 M3LOSmNmdGxiVnnhZoltcXS7IFHzd4F6 NVzXcW5UOcLizszN NHj6NXo4OsLiaB?= MY\EUXNQ MlzJ[Y5p[W6lZYOg[4Vu[2m2YXLpcoUucW6mdXPld{Bk\WyuII\pZYJqdGm2eTDk[YNz\WG|ZR?= NI[4R3UzPTh5Mkm0NS=>
MMCs MofzSpVv[3Srb36gRZN{[Xl? Mn\oNUDPxG1? NYP0TZpWOC12ODDo Mo\QbY5kemWjc3XzJG5RWkFicILveIVqdiCneIDy[ZN{cW:wwrCyMlfjiJN|LkWg[o9t\A>? MX:yOFQ2OTN5OB?=
MMCs MYXGeY5kfGmxbjDBd5NigQ>? MlvBNE42NzFizszN M2P0VVI1KGh? Mom0d4hwf3NiNEWt[o9t\CC|dHnteYxifGmxbjDpckBkT02SIHzleoVtew>? MkH2NlQ1PTF|N{i=
MMCs NXj2VmFlTnWwY4Tpc44hSXO|YYm= MX[xxsDPxE1? NHXqbHozPCCq NWL4UVFocW6lcnXhd4V{KEiDVDDhZ5Rqfmm2eR?= NHvNSm0zPDR3MUO3PC=>
MMCs Mm\xSpVv[3Srb36gRZN{[Xl? M1XOXlHDqM7:TR?= NV\xUYo2OjRiaB?= NF[yUZlifWevZX70d{BodG:kYXygZYNmfHmuYYTpc44hdGW4ZXzzJI9nKGirc4TvcoUhUDNvS{mvNVQhMEh|LVu5M|E1[WNrIHHu[EBJPC2NMUKgLGg1NUtzMnHjLS=> MXKyOFQ2OTN5OB?=
MMCs NGPBeYZHfW6ldHnvckBCe3OjeR?= MnjJNeKh|ryP Mnv2Ok0zPCCq M3\jWIRwe2VvZHXw[Y5l\W62bImgbY5pcWKrdIOgeIhmKHS{aX3leIh6dGG2aX;uJIxmfmWuIH;mJGg{NUt7IDjIN{1MQW2nMzm= M4Ox[|I1PDVzM{e4
BxPC-3 NVLYZoJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLFR|UxRTFwMTFOwG0> M1vjcVIyOzd3Nke5
AsPC-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPjSWM2OD1|Lkmg{txO NUmyfoNVOjF|N{W2O|k>
MiaPaca-2 NWrZd2ZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvFR|UxRTBwNjFOwG0> MVWyNVM4PTZ5OR?=
Panc-1 M3LXO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fQRWVEPTB;MT64JO69VQ>? M{HsPVIyOzd3Nke5
PAXF 546L† NEnHe4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDlOJZGSzVyPUGuOUDPxE1? Mk[4NlE{PzV4N{m=
PAXF 1657L† MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXFR|UxRTBwMzFOwG0> M1PwVFIyOzd3Nke5
HCT15 M37Wemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjsc|huUUN3ME2wMlch|ryP NXS4bnZoOjF|MUe0OVU>
HT-29 M1PzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHFUJVKUUN3ME2wMlch|ryP MVqyNVMyPzR3NR?=
SW48 M3i2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\GN4t3UUN3ME2wMlgh|ryP MmHBNlE{OTd2NUW=
SW620 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTwVItHUUN3ME2xJO69VQ>? M2\ZUlIyOzF5NEW1
HMEC MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTF7IN88US=> Mn;MNlE{OTd2NUW=
ANBL6  MoTQSpVv[3Srb36gRZN{[Xl? M4\z[FHDqM7:TR?= MljUNlQhcA>? NUOyZopS\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v NXLKPZJqOjFzN{G4NlE>
LP1 MnTxSpVv[3Srb36gRZN{[Xl? NGnXeIwyyqEQvF2= M3rwblI1KGh? NVmwVXBz\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v MU[yNVE4OTh{MR?=
HD-LM2 M1PsfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWi3NuKhcA>? M4L3fWROW09? M3rLR2lEPTB;MT64PEDPxE1? M3vCWFIxQDhyMUC3
L428 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfwO|LDqGh? MVrEUXNQ NWnDVGtmUUN3ME2xMlk3KM7:TR?= M{TmVVIxQDhyMUC3
KM-H2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjCO|LDqGh? NUTDU5hnTE2VTx?= MXHJR|UxRTJwOE[g{txO MnL0NlA5QDBzMEe=
HD-LM2 NH36U4JHfW6ldHnvckBCe3OjeR?= NHr2dXcxNjFvMjFOwG0> MV6yOEBpyqB? NEXPfINFVVOR MXzzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz M{fNT|IxQDhyMUC3
L428 MX\GeY5kfGmxbjDBd5NigQ>? NWGxb5lyOC5zLUKg{txO MXSyOEBpyqB? NHzE[WZFVVOR MYHzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz MnHhNlA5QDBzMEe=
KM-H2 NWrCS24zTnWwY4Tpc44hSXO|YYm= NXTTdlBpOC5zLUKg{txO MXmyOEBpyqB? NV;xPJFxTE2VTx?= MlzVd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= Mn75NlA5QDBzMEe=
HD-LM2 M{TNbWFxd3C2b4Ppd{BCe3OjeR?= MmLkNE4yNzBwNT:xJO69VQ>? NUTWVGJpPDhiaB?= MVPEUXNQ NXHnfGFScW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MUGyNFg5ODFyNx?=
L428 MnjtRZBweHSxc3nzJGF{e2G7 NGPOZ|AxNjFxMD61M|Eh|ryP MV20PEBp MmjMSG1UVw>? MmrtbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MoDkNlA5QDBzMEe=
KM-H2 MUHBdI9xfG:|aYOgRZN{[Xl? MmrzNE4yNzBwNT:xJO69VQ>? NW\1UWh{PDhiaB?= NYTFSGRxTE2VTx?= NFPoNoVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M{m2eVIxQDhyMUC3
HD-LM2 NVjsTIxITnWwY4Tpc44hSXO|YYm= MlzNNeKh|ryP NEnHU5IzPC92ODDo M2W0SGROW09? MVnkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz MorENlA5QDBzMEe=
L428 MYXGeY5kfGmxbjDBd5NigQ>? Ml\FNeKh|ryP MlLUNlQwPDhiaB?= Mn7pSG1UVw>? NI\Z[Fhld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ MnzyNlA5QDBzMEe=
KM-H2 NFTEOGFHfW6ldHnvckBCe3OjeR?= MUCxxsDPxE1? M{DjdFI1NzR6IHi= NGTqUI1FVVOR M{i3bIRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> M4LTPVIxQDhyMUC3
HD-LM2 NGTPPJpHfW6ldHnvckBCe3OjeR?= NVHtTJBnOC53L{Gg{txO M2G4R|I1NzR6IHi= NHnnUpFFVVOR MmrleZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NETrTJYzODh6MEGwOy=>
L428 MXnGeY5kfGmxbjDBd5NigQ>? MnXFNE42NzFizszN MX[yOE81QCCq NGfDT21FVVOR NI[zZnR2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> Mm\UNlA5QDBzMEe=
KM-H2 NH7FbZBHfW6ldHnvckBCe3OjeR?= Mlq1NE42NzFizszN MVeyOE81QCCq M{e5VWROW09? M{jtT5VxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NFLtU3YzODh6MEGwOy=>
HD-LM2 NXzCSZI{TnWwY4Tpc44hSXO|YYm= NVLHR5JyOcLizszN NIXFN5ExNjJ3LUS4JIg> M{XhdWROW09? M4LhO4FkfGm4YYTld{BPTi2tQh?= M1zqZVIxQDhyMUC3
L428 MoHVSpVv[3Srb36gRZN{[Xl? MWKxxsDPxE1? NHfxflExNjJ3LUS4JIg> MoTtSG1UVw>? MmDOZYN1cX[jdHXzJG5HNWuE NXzLd|dPOjB6OECxNFc>
KM-H2 MnfxSpVv[3Srb36gRZN{[Xl? MX[xxsDPxE1? NXfJSYllOC5{NT20PEBp NEDWWnBFVVOR M3O0XoFkfGm4YYTld{BPTi2tQh?= M2\TbFIxQDhyMUC3
H526 NGPyXmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{foV2lEPTB;NEiwJI5O NHy2dlUzODZ6Mk[0Ny=>
H146 NVnsW3BIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Tve2lEPTB;M{Wgcm0> NHjo[5gzODZ6Mk[0Ny=>
H82 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJ3MDDuUS=> MWeyNFY5OjZ2Mx?=
DMS114 NGntdotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[yemlEPTB;NkSwJI5O M3rvTFIxPjh{NkSz
HeLa MmG3SpVv[3Srb36gRZN{[Xl? MlOwNE4{NTFyIN88US=> NG\acXU5KGh? NYf1NnJDTE2VTx?= MkjwbY5kemWjc3XzJIFk\XS7bHH0[YQhUDNiS{mgLGg{UzmDYzmgZZQhOTBizszN NXewc456OjB3M{i4OFA>
HeLa NEi0[IRHfW6ldHnvckBCe3OjeR?= NXu1SXVFOC5|LUGwJO69VQ>? MlnEPEBp NFjRUXBFVVOR NWDWV5hzcW6lcnXhd4V{KGOjc4Dhd4UhOyCjbnSgO{Bi[3SrdnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> NGXTXXIzODV|OEi0NC=>
HeLa NH;EeJlHfW6ldHnvckBCe3OjeR?= MX6xNEDPxE4EoB?= MUe2M|EzNzJ2IHi= NF\LeZJFVVOR NUjFS2R7cW6mdXPld{BucXSxdHnjJIFk[3WvdXzheIlwdiCjbnSg[IVt[XmnZDDwNlEh\XiycnXzd4lwdg>? NGTRN2gzODV|OEi0NC=>
HeLa  NIHuUFVHfW6ldHnvckBCe3OjeR?= NYrYV5RJOTBizszNxsA> M1nmZ|chcA>? MXjEUXNQ NF3sRlBlcXO{dYD0d{Bvd3KvYXygd5BqdmSuZTDjbIVkc3CxaX70JIZ2dmO2aX;u MkeyNlA2Ozh6NEC=
PBMC  NFvRepdCeG:ydH;zbZMhSXO|YYm= NFSzbmYxNjVxMj:zJO69VQ>? NVfTbW8zOjRxNEigbC=> NF7KVpVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MXmyNFQxPjl2Nx?=

... Click to View More Cell Line Experimental Data

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

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Female CD-1 nude mice bearing H1437 tumors
  • Formulation: PBS acidified with 0.1 M HCl or PEG400/0.2 M HCl saline, 40:60
  • 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 powder
in solvent
Synonyms MG0103

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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03220477 Recruiting Lung Cancer Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme Corp.|Astex Pharmaceuticals|Mirati Therapeutics Inc.|Stand Up To Cancer|Van Andel Research Institute August 4 2017 Phase 1
NCT03565406 Recruiting Melanoma New York University School of Medicine April 25 2018 Phase 1
NCT02954991 Recruiting Carcinoma Non-Small-Cell Lung Mirati Therapeutics Inc. November 2016 Phase 2
NCT02805660 Recruiting Advanced Cancer Mirati Therapeutics Inc. May 2016 Phase 1|Phase 2
NCT02303262 Completed Metastatic Leiomyosarcoma Sarcoma Alliance for Research through Collaboration September 2015 Phase 2
NCT02429375 Active not recruiting Hodgkin Lymphoma Memorial Sloan Kettering Cancer Center|MethylGene Inc. April 2015 Phase 1|Phase 2

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID