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)
HDAC4 [1]
(Cell-free assay)
0.15 μM 0.29 μM 0.59 μM 1.66 μM >10 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 NFvMPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DXb|Q5KGh? NF\QeFRKSzVyPUOuNFQh|ryP MmHwNlY{PzhyM{i=
BT549 Mo\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjJO5loPDhiaB?= MVnJR|UxRTRwM{ig{txO M3S5WVI3Ozd6MEO4
MCF7 M4ezbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e3blQ5KGh? MkDxTWM2OD1yLk[3JO69VQ>? NHjP[okzPjN5OECzPC=>
T47D M3jOT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlH3OFghcA>? NGjXbItKSzVyPUGuNVch|ryP MYeyOlM4QDB|OB?=
MOLP8 NIfROWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF65OZA1QCCq NVTVTo5NUUN3ME2wMlbDuSByLkC0{txO NHHVSW0zPjB7MUWxPC=>
Panc1 NXH1VXMxTnWwY4Tpc44hSXO|YYm= NXq4ZVR5OC53L{GvNk42KM7:TR?= Mlm2OFghcA>? NHP1boJFVVOR MmnmeZBz\We3bHH0[ZMhdWmULUKwNy=> Mn;PNlU5PzJ7NEG=
Panc1 MWTGeY5kfGmxbjDBd5NigQ>? MX2wMlUwOS9{LkWg{txO NWn1UZlDPDhiaB?= NHr1PGNFVVOR NH7wXG9z\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiWlXCNUBwdiCkb4ToJI1TVkFiYX7kJJBzd3SnaX6gcIV3\W{EoB?= M{\KelI2QDd{OUSx
Panc1 Mn7kRZBweHSxc3nzJGF{e2G7 Mlu5NeKh|ryP NGHY[Vg4OsLiaB?= NXK2bpZQTE2VTx?= M3TrNpNmdnOrdHn6[ZMhWGGwY{GgZ4VtdHNiZn;yJIdmdWOrdHHibY5mNWmwZIXj[YQh[XCxcITvd4l{ NFnZSmYzPTh5Mkm0NS=>
Panc1 MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWmxxsDPxE1? NH;JbJo4OsLiaB?= NUnsfFNtTE2VTx?= NYfONVBD\W6qYX7j[ZMh\2WvY3n0ZYJqdmVvaX7keYNmeyClZXzsJJZq[WKrbHn0fUBl\WO{ZXHz[S=> NFPoZpgzPTh5Mkm0NS=>
MMCs NFjoSmxHfW6ldHnvckBCe3OjeR?= NFrxSWsyKM7:bR?= NF3uTVgxNTR6IHi= M{\4VYlv[3KnYYPld{BPWFKDIIDyc5RmcW5iZYjwdoV{e2mxbtMgNk446oDVMz61JIZwdGR? MW[yOFQ2OTN5OB?=
MMCs Mmr3SpVv[3Srb36gRZN{[Xl? MoLSNE42NzFizszN M3\sR|I1KGh? NHO2T29{cG:5czC0OU1nd2ymIIP0bY12dGG2aX;uJIlvKGOJTWCgcIV3\Wy| Mn:0NlQ1PTF|N{i=
MMCs NITCWItHfW6ldHnvckBCe3OjeR?= NWLNRo1VOcLizszN MUSyOEBp MYDpcoNz\WG|ZYOgTGFVKGGldHn2bZR6 NUn5[npNOjR2NUGzO|g>
MMCs M3frZWZ2dmO2aX;uJGF{e2G7 MojoNeKh|ryP MVWyOEBp MYfheYdu\W62czDncI9j[WxiYXPleJlt[XSrb36gcIV3\Wy|IH;mJIhqe3SxbnWgTFMuUzlxMUSgLGg{NUt7L{G0ZYMqKGGwZDDIOE1MOTJiKFi0MWsyOmGlKR?= Mle3NlQ1PTF|N{i=
MMCs NHHTOIFHfW6ldHnvckBCe3OjeR?= MUOxxsDPxE1? MoDQOk0zPCCq NHPkXmpld3OnLXTldIVv\GWwdHz5JIlvcGmkaYTzJJRp\SC2cnnt[ZRpgWyjdHnvckBt\X[nbDDv[kBJOy2NOTCoTFMuUzmvZUOp MVeyOFQ2OTN5OB?=
BxPC-3 M1LWbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\Ze|dGSzVyPUGuNUDPxE1? M{G5VFIyOzd3Nke5
AsPC-1 NFrUS2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfFR|UxRTNwOTFOwG0> MmXLNlE{PzV4N{m=
MiaPaca-2 M{Gx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnpXXhrTUN3ME2wMlYh|ryP M4HOTFIyOzd3Nke5
Panc-1 MmLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF32bnFGSzVyPUGuPEDPxE1? MXWyNVM4PTZ5OR?=
PAXF 546L† NWnF[|lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nCdmVEPTB;MT61JO69VQ>? MojiNlE{PzV4N{m=
PAXF 1657L† M1PGcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\XbGVEPTB;MD6zJO69VQ>? NF7XbFczOTN5NU[3PS=>
HCT15 MmfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwNzFOwG0> NXHCN5MzOjF|MUe0OVU>
HT-29 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVOzfpZ[UUN3ME2wMlch|ryP MnrwNlE{OTd2NUW=
SW48 MoPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\oTWM2OD1yLkig{txO NFTzN5IzOTNzN{S1OS=>
SW620 NV7zfHRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDLT3dKSzVyPUGg{txO M1HKcVIyOzF5NEW1
HMEC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTF7IN88US=> NWXJ[JpIOjF|MUe0OVU>
ANBL6  NWnr[XJyTnWwY4Tpc44hSXO|YYm= MkjrNeKh|ryP MUWyOEBp NVq5WVBX\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v NYLKZmx2OjFzN{G4NlE>
LP1 MUnGeY5kfGmxbjDBd5NigQ>? NX3O[4lGOcLizszN NVW2TWJnOjRiaB?= NEG5T4NmdmijbnPld{A2NUGFLXnu[JVk\WRiTVHHSU1COyCpZX7lJIV5eHKnc4Ppc44> MnXwNlEyPzF6MkG=
HD-LM2 NVfhR2hnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFm1e284OsLiaB?= NYfBdJR7TE2VTx?= M3XOfWlEPTB;MT64PEDPxE1? NGC1V2YzODh6MEGwOy=>
L428 MlWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVi3NuKhcA>? MXzEUXNQ M2LhNGlEPTB;MT65OkDPxE1? MW[yNFg5ODFyNx?=
KM-H2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvHTGg4OsLiaB?= NWHu[ppITE2VTx?= NHXtUJlKSzVyPUKuPFYh|ryP MoXONlA5QDBzMEe=
HD-LM2 MnfPSpVv[3Srb36gRZN{[Xl? NIO1bFUxNjFvMjFOwG0> MX2yOEBpyqB? NFfXfHZFVVOR MUHzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz MX2yNFg5ODFyNx?=
L428 MlP3SpVv[3Srb36gRZN{[Xl? NYj0Z|ZLOC5zLUKg{txO M1nJXlI1KGkEoB?= MY\EUXNQ NH31WXd{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx Mm\kNlA5QDBzMEe=
KM-H2 M1XMdmZ2dmO2aX;uJGF{e2G7 NXf0SZVbOC5zLUKg{txO MWGyOEBpyqB? NF7OO5lFVVOR NHS0WY5{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx Mlf4NlA5QDBzMEe=
HD-LM2 Mn\aRZBweHSxc3nzJGF{e2G7 MWmwMlEwOC53L{Gg{txO NYfjXodGPDhiaB?= MkP1SG1UVw>? NYXPSFc2cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MlH1NlA5QDBzMEe=
L428 NGjJRlBCeG:ydH;zbZMhSXO|YYm= NInPZoYxNjFxMD61M|Eh|ryP MoXqOFghcA>? M1zSWWROW09? NXTW[Ih7cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NH[0bY4zODh6MEGwOy=>
KM-H2 M1vqRmFxd3C2b4Ppd{BCe3OjeR?= M1zGeFAvOS9yLkWvNUDPxE1? MWO0PEBp NH:zSo9FVVOR M2PycYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M3TRVFIxQDhyMUC3
HD-LM2 MUDGeY5kfGmxbjDBd5NigQ>? MYWxxsDPxE1? NHfpdm0zPC92ODDo M1[wb2ROW09? M1HOVYRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> MWeyNFg5ODFyNx?=
L428 NGnkR5VHfW6ldHnvckBCe3OjeR?= MYCxxsDPxE1? NIXlOWQzPC92ODDo MV3EUXNQ NF7nOZNld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ NXPlUpFGOjB6OECxNFc>
KM-H2 NEL6WGlHfW6ldHnvckBCe3OjeR?= MoP4NeKh|ryP M1\iTlI1NzR6IHi= MkCwSG1UVw>? NIe4NZFld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ NHS0PWgzODh6MEGwOy=>
HD-LM2 MkLLSpVv[3Srb36gRZN{[Xl? NUe1XJNDOC53L{Gg{txO MX:yOE81QCCq MojzSG1UVw>? NGHzVZV2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M1XacVIxQDhyMUC3
L428 NFPubZJHfW6ldHnvckBCe3OjeR?= MoS2NE42NzFizszN MWeyOE81QCCq NF60bHFFVVOR NHvIZlZ2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NWfmb3l5OjB6OECxNFc>
KM-H2 MlvHSpVv[3Srb36gRZN{[Xl? M1\pV|AvPS9zIN88US=> NIrLU|UzPC92ODDo Mn24SG1UVw>? NIrRepd2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M4HwSFIxQDhyMUC3
HD-LM2 NFTFRnBHfW6ldHnvckBCe3OjeR?= MVSxxsDPxE1? MWewMlI2NTR6IHi= NYXVXFRmTE2VTx?= MULhZ5RqfmG2ZYOgUmYuc0J? NYq5NIxJOjB6OECxNFc>
L428 M{LrcGZ2dmO2aX;uJGF{e2G7 MVOxxsDPxE1? NIDTO28xNjJ3LUS4JIg> MX;EUXNQ MoKwZYN1cX[jdHXzJG5HNWuE MlPFNlA5QDBzMEe=
KM-H2 Mor2SpVv[3Srb36gRZN{[Xl? MmDJNeKh|ryP MkSyNE4zPS12ODDo Mn\1SG1UVw>? M1LhTIFkfGm4YYTld{BPTi2tQh?= MmHKNlA5QDBzMEe=
H526 NXW2W5IzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPYTWM2OD12OECgcm0> NInTPVgzODZ6Mk[0Ny=>
H146 NECwNGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPrTWM2OD1|NTDuUS=> NXn0b3ZTOjB4OEK2OFM>
H82 M4PmOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXYTWM2OD1{NUCgcm0> MlW2NlA3QDJ4NEO=
DMS114 Mof4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDRR4tKSzVyPU[0NEBvVQ>? NYfsbFlSOjB4OEK2OFM>
HeLa Mn;iSpVv[3Srb36gRZN{[Xl? M1jne|AvOy1zMDFOwG0> MWO4JIg> M17JOmROW09? NYHHR3c2cW6lcnXhd4V{KGGlZYT5cIF1\WRiSEOgT|khMEh|S{nBZ{kh[XRiMUCg{txO M3\t[FIxPTN6OESw
HeLa MXnGeY5kfGmxbjDBd5NigQ>? M2LYWFAvOy1zMDFOwG0> M1LPTVghcA>? MVrEUXNQ MWnpcoNz\WG|ZYOgZ4F{eGG|ZTCzJIFv\CB5IHHjeIl3[XSrb36g[I9{\SCmZYDlcoRmdnSueR?= Mke0NlA2Ozh6NEC=
HeLa NV7aVGdSTnWwY4Tpc44hSXO|YYm= NUDUUFEyOTBizszNxsA> NFTRdZA3NzF{L{K0JIg> NUW0bZByTE2VTx?= Mn;sbY5lfWOnczDtbZRwfGmlIHHjZ5VufWyjdHnvckBidmRiZHXsZZlm\CCyMkGg[ZhxemW|c3nvci=> NF:3eY0zODV|OEi0NC=>
HeLa  NYjNU4l2TnWwY4Tpc44hSXO|YYm= NWHsR2FXOTBizszNxsA> NEewUZQ4KGh? MoPnSG1UVw>? MkLm[Il{enWydIOgco9zdWGuIIPwbY5ldGViY3jlZ4txd2mwdDDmeY5kfGmxbh?= NYLnXXFnOjB3M{i4OFA>
PBMC  MkfFRZBweHSxc3nzJGF{e2G7 NXO4NGlIOC53L{KvN{DPxE1? MV:yOE81QCCq M3XZSolv\HWlZYOgZZBweHSxc3nzJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NY\2fpF6OjB2ME[5OFc>

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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* 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
NCT02993991 Not yet recruiting 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 January 2017 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 Active, not recruiting Metastatic Leiomyosarcoma Sarcoma Alliance for Research through Collaboration September 2015 Phase 2
NCT02429375 Recruiting Hodgkin Lymphoma Memorial Sloan Kettering Cancer Center|MethylGene Inc. April 2015 Phase 1|Phase 2
NCT02236195 Completed Urothelial Carcinoma Mirati Therapeutics Inc. October 2014 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID