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 M3;zeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PYdFQ5KGh? NXnLbG9qUUN3ME2zMlA1KM7:TR?= M{fBfVI3Ozd6MEO4
BT549 Mnz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HKd|Q5KGh? MmLBTWM2OD12LkO4JO69VQ>? MU[yOlM4QDB|OB?=
MCF7 M{TEUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;4bFQ5KGh? MkPUTWM2OD1yLk[3JO69VQ>? NGXZOZUzPjN5OECzPC=>
T47D M3rrcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrLXHA1QCCq NE\MWJFKSzVyPUGuNVch|ryP MmnXNlY{PzhyM{i=
MOLP8 M2HLc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUSyVo13PDhiaB?= MWDJR|UxRTBwNtMxJFAvODUQvF2= M13WT|I3ODlzNUG4
Panc1 NVLZdXJETnWwY4Tpc44hSXO|YYm= NWfH[JZDOC53L{GvNk42KM7:TR?= MoGwOFghcA>? NHvKVZJFVVOR NUPNfodDfXC{ZXf1cIF1\XNibXnSMVIxOw>? M1nCbFI2QDd{OUSx
Panc1 NXHUWm9vTnWwY4Tpc44hSXO|YYm= MVGwMlUwOS9{LkWg{txO MlzmOFghcA>? NGSxNnlFVVOR Mn\CdoVlfWOnczDlfJBz\XO|aX;uJI9nKFqHQkGgc44h[m:2aDDtVm5CKGGwZDDwdo91\WmwIHzleoVtyqB? MWiyOVg4Ojl2MR?=
Panc1 M2P0N2Fxd3C2b4Ppd{BCe3OjeR?= NInyNoUyyqEQvF2= M2m2[lczyqCq NYrKOZhZTE2VTx?= M1TnN5NmdnOrdHn6[ZMhWGGwY{GgZ4VtdHNiZn;yJIdmdWOrdHHibY5mNWmwZIXj[YQh[XCxcITvd4l{ M3nUO|I2QDd{OUSx
Panc1 M3\ZSmNmdGxiVnnhZoltcXS7IFHzd4F6 M1T2[|HDqM7:TR?= MW[3NuKhcA>? MULEUXNQ M2XSV4VvcGGwY3XzJIdmdWOrdHHibY5mNWmwZIXj[ZMh[2WubDD2bYFjcWyrdImg[IVkemWjc3W= NUC3SoZxOjV6N{K5OFE>
MMCs M4\5UmZ2dmO2aX;uJGF{e2G7 MUGxJO69dQ>? Mn3lNE01QCCq MWfpcoNz\WG|ZYOgUnBTSSCycn;0[YlvKGW6cILld5Nqd28EoEKuO-KBmzNwNTDmc4xl M{PwelI1PDVzM{e4
MMCs NHfoZ|dHfW6ldHnvckBCe3OjeR?= M4HWbVAvPS9zIN88US=> MnrTNlQhcA>? NV74PFU3e2ixd4OgOFUu\m:uZDDzeIlufWyjdHnvckBqdiClR13QJIxmfmWucx?= NXO4O5NxOjR2NUGzO|g>
MMCs M{TLOWZ2dmO2aX;uJGF{e2G7 MoDONeKh|ryP NH7ERW0zPCCq MkHvbY5kemWjc3XzJGhCXCCjY4Tpeol1gQ>? MnzrNlQ1PTF|N{i=
MMCs NIDVcHlHfW6ldHnvckBCe3OjeR?= MYmxxsDPxE1? NFnBR48zPCCq NVTHc5NC[XWpbXXueJMh\2yxYnHsJIFk\XS7bHH0bY9vKGyndnXsd{Bw\iCqaYP0c45mKEh|LVu5M|E1KCiKMz3LPU8yPGGlKTDhcoQhUDRvS{GyJEhJPC2NMULhZ{k> NVO3SHZqOjR2NUGzO|g>
MMCs M4fPZ2Z2dmO2aX;uJGF{e2G7 MXuxxsDPxE1? M2SxVlYuOjRiaB?= NVKwfnQ4\G:|ZT3k[ZBmdmSnboTsfUBqdmirYnn0d{B1cGVidILpcYV1cHmuYYTpc44hdGW4ZXygc4YhUDNvS{mgLGg{NUt7bXWzLS=> Mn7yNlQ1PTF|N{i=
BxPC-3 NHqxRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXXSWM2OD1zLkGg{txO NGDFVVIzOTN5NU[3PS=>
AsPC-1 M17GXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHFR|UxRTNwOTFOwG0> MUKyNVM4PTZ5OR?=
MiaPaca-2 M4LZSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHFR|UxRTBwNjFOwG0> MoPFNlE{PzV4N{m=
Panc-1 MkT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFO3PGtGSzVyPUGuPEDPxE1? M{XrNVIyOzd3Nke5
PAXF 546L† NYT2S|JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLwSWM2OD1zLkWg{txO NHXGPYEzOTN5NU[3PS=>
PAXF 1657L† Mk[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfIVW5CTUN3ME2wMlMh|ryP MmTFNlE{PzV4N{m=
HCT15 NFjVXXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGC4RoJKSzVyPUCuO{DPxE1? MYOyNVMyPzR3NR?=
HT-29 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwNzFOwG0> MonlNlE{OTd2NUW=
SW48 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDXTm9KSzVyPUCuPEDPxE1? NYrrVm1KOjF|MUe0OVU>
SW620 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjXWJNnUUN3ME2xJO69VQ>? NWf0[IY3OjF|MUe0OVU>
HMEC M{j0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF7IN88US=> M1u5W|IyOzF5NEW1
ANBL6  MWfGeY5kfGmxbjDBd5NigQ>? M1nmdFHDqM7:TR?= MWKyOEBp NWK2S|E1\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v M3vweFIyOTdzOEKx
LP1 NGLS[XBHfW6ldHnvckBCe3OjeR?= NVH2PFA3OcLizszN M4XlV|I1KGh? MYDlcohidmOnczC1MWFENWmwZIXj[YQhVUGJRT3BN{Bo\W6nIHX4dJJme3Orb36= NXTBcFZkOjFzN{G4NlE>
HD-LM2 NXvZdpVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYX3UVh2PzMEoHi= NILmNGZFVVOR NYjVXZdOUUN3ME2xMlg5KM7:TR?= NW\yblVxOjB6OECxNFc>
L428 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLv[Zg4PzMEoHi= NF7LVIdFVVOR Mo[yTWM2OD1zLkm2JO69VQ>? NYH1ZphJOjB6OECxNFc>
KM-H2 NIPYbpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUe3NuKhcA>? NV3oUJlKTE2VTx?= Mnr1TWM2OD1{Lki2JO69VQ>? MUSyNFg5ODFyNx?=
HD-LM2 Ml;4SpVv[3Srb36gRZN{[Xl? MoDaNE4yNTJizszN M1naeFI1KGkEoB?= M3HXVGROW09? MoPzd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= MWCyNFg5ODFyNx?=
L428 NXzxSXNyTnWwY4Tpc44hSXO|YYm= MnTTNE4yNTJizszN NVjifWdTOjRiaNMg MoDCSG1UVw>? NVL4TJBTe2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=> M{G0W|IxQDhyMUC3
KM-H2 NYTuVoxrTnWwY4Tpc44hSXO|YYm= NETCSGYxNjFvMjFOwG0> NVTVZnMyOjRiaNMg NGXt[ldFVVOR MYrzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz NGPBbJYzODh6MEGwOy=>
HD-LM2 MnjZRZBweHSxc3nzJGF{e2G7 M3PmcVAvOS9yLkWvNUDPxE1? NVf4dYdKPDhiaB?= NGrEd2FFVVOR NVXIUHFrcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> M1\uN|IxQDhyMUC3
L428 NV3y[2pCSXCxcITvd4l{KEG|c3H5 MoHENE4yNzBwNT:xJO69VQ>? M3W4WlQ5KGh? NG\FOXJFVVOR MlvCbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= M4DjRlIxQDhyMUC3
KM-H2 Mo[4RZBweHSxc3nzJGF{e2G7 Mn\HNE4yNzBwNT:xJO69VQ>? M3PycFQ5KGh? MnLESG1UVw>? MYLpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NY\TbFNYOjB6OECxNFc>
HD-LM2 MnzjSpVv[3Srb36gRZN{[Xl? MUCxxsDPxE1? MWGyOE81QCCq NY\UOpA2TE2VTx?= NHHrTW5ld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ NVz6ZYdmOjB6OECxNFc>
L428 MYfGeY5kfGmxbjDBd5NigQ>? MX:xxsDPxE1? NVzGT2tuOjRxNEigbC=> MnK2SG1UVw>? NG\lZpJld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ NETlVoUzODh6MEGwOy=>
KM-H2 MUnGeY5kfGmxbjDBd5NigQ>? Mom1NeKh|ryP M{fBTlI1NzR6IHi= MomwSG1UVw>? M2izNIRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> NWnUWmJYOjB6OECxNFc>
HD-LM2 NVPWUWpoTnWwY4Tpc44hSXO|YYm= M3HTU|AvPS9zIN88US=> Mn[zNlQwPDhiaB?= NXHrflVLTE2VTx?= NV64eVlFfXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NF;UT|EzODh6MEGwOy=>
L428 M2HZbmZ2dmO2aX;uJGF{e2G7 NFXtblkxNjVxMTFOwG0> NEXyOm0zPC92ODDo NH7ZPFhFVVOR MnTteZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NFHSe2MzODh6MEGwOy=>
KM-H2 NWDFSGRjTnWwY4Tpc44hSXO|YYm= MYiwMlUwOSEQvF2= NVSzSJZmOjRxNEigbC=> M4m1OWROW09? NHryXXh2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MX2yNFg5ODFyNx?=
HD-LM2 M3HtSmZ2dmO2aX;uJGF{e2G7 NHfnV4UyyqEQvF2= M3u3W|AvOjVvNEigbC=> NFOxSnhFVVOR NXHMe2M2[WO2aY\heIV{KE6ILXvC NXHNd4pXOjB6OECxNFc>
L428 MVLGeY5kfGmxbjDBd5NigQ>? MX6xxsDPxE1? MVmwMlI2NTR6IHi= M2ruTWROW09? NXjZSXF3[WO2aY\heIV{KE6ILXvC NYflVIhyOjB6OECxNFc>
KM-H2 M2nh[mZ2dmO2aX;uJGF{e2G7 MWqxxsDPxE1? NILWXJYxNjJ3LUS4JIg> M2DWXWROW09? M4TGb4FkfGm4YYTld{BPTi2tQh?= M1LHc|IxQDhyMUC3
H526 NGPPfXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnznTWM2OD12OECgcm0> NXTCbFdzOjB4OEK2OFM>
H146 Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTN3IH7N NYHsPFRGOjB4OEK2OFM>
H82 NXzJVGV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTyTWM2OD1{NUCgcm0> M4rPbVIxPjh{NkSz
DMS114 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfPNINWUUN3ME22OFAhdk1? M{jIWVIxPjh{NkSz
HeLa NGeyRY5HfW6ldHnvckBCe3OjeR?= NELTW|kxNjNvMUCg{txO Ml\tPEBp MmjjSG1UVw>? NFLaPVBqdmO{ZXHz[ZMh[WOndInsZZRm\CCKMzDLPUApUDONOVHjLUBifCBzMDFOwG0> M4TJVFIxPTN6OESw
HeLa MVPGeY5kfGmxbjDBd5NigQ>? Mnr3NE4{NTFyIN88US=> NHXEd2k5KGh? NXLaR2RwTE2VTx?= M1HGcIlv[3KnYYPld{Bk[XOyYYPlJFMh[W6mIEegZYN1cX[jdHnvckBld3OnIHTldIVv\GWwdHz5 NU\jWYtyOjB3M{i4OFA>
HeLa NGTodmFHfW6ldHnvckBCe3OjeR?= NEHOW|MyOCEQvF5CpC=> MnTLOk8yOi9{NDDo M{HrdGROW09? NVfpWZZOcW6mdXPld{BucXSxdHnjJIFk[3WvdXzheIlwdiCjbnSg[IVt[XmnZDDwNlEh\XiycnXzd4lwdg>? MXGyNFU{QDh2MB?=
HeLa  NF7mZVJHfW6ldHnvckBCe3OjeR?= M3T1ZVExKM7:TdMg NEPYdIY4KGh? MXrEUXNQ MYXkbZNzfXC2czDuc5Ju[Wxic4DpcoRt\SClaHXjb5BwcW62IH\1coN1cW:w NHn3UWIzODV|OEi0NC=>
PBMC  MVLBdI9xfG:|aYOgRZN{[Xl? MU[wMlUwOi9|IN88US=> MlTwNlQwPDhiaB?= NYDZOJIxcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NX\BfItmOjB2ME[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 Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% Propylene glycol
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
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
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