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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Cited by 41 Publications

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 NFfRfHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlf2OFghcA>? MYHJR|UxRTNwMESg{txO MkK0NlY{PzhyM{i=
BT549 M4fLb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUG0PEBp NEn4SVBKSzVyPUSuN|gh|ryP NVLqOVBGOjZ|N{iwN|g>
MCF7 MkHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzPeJY{PDhiaB?= NFXDPYxKSzVyPUCuOlch|ryP MX6yOlM4QDB|OB?=
T47D MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonCOFghcA>? MnjHTWM2OD1zLkG3JO69VQ>? M3jPUlI3Ozd6MEO4
MOLP8 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnmyOFghcA>? MV;JR|UxRTBwNtMxJFAvODUQvF2= NVjvUXd5OjZyOUG1NVg>
Panc1 NWTBeVI{TnWwY4Tpc44hSXO|YYm= MWewMlUwOS9{LkWg{txO MmO2OFghcA>? NYG2O4h1TE2VTx?= MU\1dJJm\3WuYYTld{BucVJvMkCz M4\MNVI2QDd{OUSx
Panc1 MWPGeY5kfGmxbjDBd5NigQ>? NHWxU|ExNjVxMT:yMlUh|ryP NULMcm9RPDhiaB?= NHnYXY9FVVOR MUTy[YR2[2W|IHX4dJJme3Orb36gc4YhYkWEMTDvckBjd3SqIH3SUmEh[W6mIIDyc5RmcW5ibHX2[YzDqA>? NWHZeIVVOjV6N{K5OFE>
Panc1 MYTBdI9xfG:|aYOgRZN{[Xl? NInm[FEyyqEQvF2= MYC3NuKhcA>? NITBbmpFVVOR NVL0Wm9[e2Wwc3n0bZpmeyCSYX7jNUBk\WyuczDmc5Ih\2WvY3n0ZYJqdmVvaX7keYNm\CCjcH;weI9{cXN? NUnke2NpOjV6N{K5OFE>
Panc1 NUPZTmlGS2WubDDWbYFjcWyrdImgRZN{[Xl? NYHIdJNqOcLizszN NX3XTYdyPzMEoHi= MnL4SG1UVw>? M1zDW4VvcGGwY3XzJIdmdWOrdHHibY5mNWmwZIXj[ZMh[2WubDD2bYFjcWyrdImg[IVkemWjc3W= NWfFOXdWOjV6N{K5OFE>
MMCs MXzGeY5kfGmxbjDBd5NigQ>? MWGxJO69dQ>? Mkf0NE01QCCq NFHyN|BqdmO{ZXHz[ZMhVlCUQTDwdo91\WmwIHX4dJJme3Orb39CpFIvP+LCk{OuOUBnd2ym NH\T[IszPDR3MUO3PC=>
MMCs NFO3S5pHfW6ldHnvckBCe3OjeR?= MU[wMlUwOSEQvF2= MVGyOEBp MmLWd4hwf3NiNEWt[o9t\CC|dHnteYxifGmxbjDpckBkT02SIHzleoVtew>? NH\xUZQzPDR3MUO3PC=>
MMCs MWrGeY5kfGmxbjDBd5NigQ>? M1ziVFHDqM7:TR?= M{XWUlI1KGh? MmHUbY5kemWjc3XzJGhCXCCjY4Tpeol1gQ>? NVHMbIZJOjR2NUGzO|g>
MMCs MXLGeY5kfGmxbjDBd5NigQ>? M2e2R|HDqM7:TR?= M1LGdlI1KGh? MlPPZZVodWWwdIOg[4xw[mGuIHHj[ZR6dGG2aX;uJIxmfmWuczDv[kBpcXO2b37lJGg{NUt7L{G0JEhJOy2NOT:xOIFkMSCjbnSgTFQuUzF{IDjIOE1MOTKjYzm= NYPxeVdtOjR2NUGzO|g>
MMCs NUHreW1ZTnWwY4Tpc44hSXO|YYm= MWSxxsDPxE1? NGHGWVQ3NTJ2IHi= MX\kc5NmNWSncHXu[IVvfGy7IHnubIljcXS|IITo[UB1emmvZYTofYxifGmxbjDs[ZZmdCCxZjDIN{1MQSBqSEOtT|lu\TNr NUjUTVU3OjR2NUGzO|g>
BxPC-3 MkjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TNXWVEPTB;MT6xJO69VQ>? NHnkOIozOTN5NU[3PS=>
AsPC-1 NGn3e4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTFR|UxRTNwOTFOwG0> NHnVXHEzOTN5NU[3PS=>
MiaPaca-2 M3;G[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLzRZlGSzVyPUCuOkDPxE1? M{PTflIyOzd3Nke5
Panc-1 M2\ySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjFR|UxRTFwODFOwG0> M1zWdFIyOzd3Nke5
PAXF 546L† MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;oOm5GSzVyPUGuOUDPxE1? MUOyNVM4PTZ5OR?=
PAXF 1657L† NHPNbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXienZGSzVyPUCuN{DPxE1? M{nYelIyOzd3Nke5
HCT15 NXzmV5ZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfKTWM2OD1yLkeg{txO NV3TVnRYOjF|MUe0OVU>
HT-29 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmK4TWM2OD1yLkeg{txO NF20XmUzOTNzN{S1OS=>
SW48 NF;6RppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTBwODFOwG0> Mn7RNlE{OTd2NUW=
SW620 NFTuVWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NES4Z5JKSzVyPUGg{txO NIT4R3UzOTNzN{S1OS=>
HMEC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlG2TWM2OD1zOTFOwG0> M2HwTFIyOzF5NEW1
ANBL6  MmLOSpVv[3Srb36gRZN{[Xl? MkPGNeKh|ryP NXH2T4lDOjRiaB?= NF3rNoJmdmijbnPld{A2NUGFLXnu[JVk\WRiTVHHSU1COyCpZX7lJIV5eHKnc4Ppc44> MXOyNVE4OTh{MR?=
LP1 MWPGeY5kfGmxbjDBd5NigQ>? MYOxxsDPxE1? MWKyOEBp MXnlcohidmOnczC1MWFENWmwZIXj[YQhVUGJRT3BN{Bo\W6nIHX4dJJme3Orb36= NV7lfWlFOjFzN{G4NlE>
HD-LM2 NXfhc2FTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\ZU|I4OsLiaB?= M1PxO2ROW09? NYPnSXpsUUN3ME2xMlg5KM7:TR?= M3XzVFIxQDhyMUC3
L428 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfOUodOPzMEoHi= MXrEUXNQ NUToe3g2UUN3ME2xMlk3KM7:TR?= M130W|IxQDhyMUC3
KM-H2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLzO|LDqGh? M{DQO2ROW09? NHn6V5FKSzVyPUKuPFYh|ryP NWrJbZUxOjB6OECxNFc>
HD-LM2 M{SxZWZ2dmO2aX;uJGF{e2G7 MWGwMlEuOiEQvF2= MnvuNlQhcMLi MWTEUXNQ NVHMTohve2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=> MV2yNFg5ODFyNx?=
L428 NGXyfFlHfW6ldHnvckBCe3OjeR?= M1LST|AvOS1{IN88US=> NXzTUpc5OjRiaNMg MkDXSG1UVw>? MnWxd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= M{G4WVIxQDhyMUC3
KM-H2 MlzpSpVv[3Srb36gRZN{[Xl? MUiwMlEuOiEQvF2= NHfKZZUzPCCqwrC= NIriR5dFVVOR MkTod4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= MnHuNlA5QDBzMEe=
HD-LM2 MVrBdI9xfG:|aYOgRZN{[Xl? NWC0SZFEOC5zL{CuOU8yKM7:TR?= MljwOFghcA>? Mn\jSG1UVw>? M3PH[olv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MVSyNFg5ODFyNx?=
L428 NUeybVNmSXCxcITvd4l{KEG|c3H5 M2G2TVAvOS9yLkWvNUDPxE1? MXS0PEBp NU\YflRZTE2VTx?= NXLOXnpYcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NYrCOYFHOjB6OECxNFc>
KM-H2 M3HOXmFxd3C2b4Ppd{BCe3OjeR?= NXK5U3B6OC5zL{CuOU8yKM7:TR?= NVexbXQ{PDhiaB?= NIS1PXBFVVOR M1GyZ4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= MWCyNFg5ODFyNx?=
HD-LM2 NYf0WZk1TnWwY4Tpc44hSXO|YYm= MkHrNeKh|ryP MoHJNlQwPDhiaB?= NET5WnBFVVOR MXzkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz NH;CeXMzODh6MEGwOy=>
L428 MljPSpVv[3Srb36gRZN{[Xl? M3\oSlHDqM7:TR?= M37TdVI1NzR6IHi= NV\2NFhiTE2VTx?= MYjkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz NF;2VZMzODh6MEGwOy=>
KM-H2 M33pNmZ2dmO2aX;uJGF{e2G7 M4\aZVHDqM7:TR?= MnT0NlQwPDhiaB?= NG\H[lZFVVOR M1jBRoRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> MYqyNFg5ODFyNx?=
HD-LM2 M1zxXmZ2dmO2aX;uJGF{e2G7 NVTiVW1JOC53L{Gg{txO NIjkV|YzPC92ODDo NULwcI1kTE2VTx?= NXfGUZczfXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MXOyNFg5ODFyNx?=
L428 MkLmSpVv[3Srb36gRZN{[Xl? MoH6NE42NzFizszN MWmyOE81QCCq M2i5XGROW09? MkKxeZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MnnhNlA5QDBzMEe=
KM-H2 MXzGeY5kfGmxbjDBd5NigQ>? MkeyNE42NzFizszN NFfUT3EzPC92ODDo NHH5bXJFVVOR MX;1dJJm\3WuYYTld{BVVkZvzsGg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MojkNlA5QDBzMEe=
HD-LM2 M{\U[GZ2dmO2aX;uJGF{e2G7 MYqxxsDPxE1? MVmwMlI2NTR6IHi= MWHEUXNQ M4DIWYFkfGm4YYTld{BPTi2tQh?= NF;xXYQzODh6MEGwOy=>
L428 MX7GeY5kfGmxbjDBd5NigQ>? MkGzNeKh|ryP NXvHcJJDOC5{NT20PEBp Mmj1SG1UVw>? NVLLRYRz[WO2aY\heIV{KE6ILXvC NV\SWHBKOjB6OECxNFc>
KM-H2 M{PhPGZ2dmO2aX;uJGF{e2G7 MoDtNeKh|ryP NUjMVZpDOC5{NT20PEBp NWHCPJgyTE2VTx?= MonnZYN1cX[jdHXzJG5HNWuE NUi0Wm82OjB6OECxNFc>
H526 Ml[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjXXHllUUN3ME20PFAhdk1? Mn:0NlA3QDJ4NEO=
H146 M3yx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTN3IH7N MnjPNlA3QDJ4NEO=
H82 NWPj[2NIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHYTWM2OD1{NUCgcm0> MkjUNlA3QDJ4NEO=
DMS114 NEDYWo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTZ2MDDuUS=> M4PhdlIxPjh{NkSz
HeLa MlzVSpVv[3Srb36gRZN{[Xl? NEnBe4YxNjNvMUCg{txO M1XFU|ghcA>? NUm4XGVkTE2VTx?= NFzZcGxqdmO{ZXHz[ZMh[WOndInsZZRm\CCKMzDLPUApUDONOVHjLUBifCBzMDFOwG0> NYjJR5NIOjB3M{i4OFA>
HeLa MV7GeY5kfGmxbjDBd5NigQ>? NXHQeoRYOC5|LUGwJO69VQ>? NFPKN4Y5KGh? MlLFSG1UVw>? NH3iS2lqdmO{ZXHz[ZMh[2G|cHHz[UA{KGGwZDC3JIFkfGm4YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NXS0RYdEOjB3M{i4OFA>
HeLa M2rYO2Z2dmO2aX;uJGF{e2G7 NHK2ZVcyOCEQvF5CpC=> Ml[xOk8yOi9{NDDo M2PxZmROW09? NV;K[pVvcW6mdXPld{BucXSxdHnjJIFk[3WvdXzheIlwdiCjbnSg[IVt[XmnZDDwNlEh\XiycnXzd4lwdg>? NULtSotjOjB3M{i4OFA>
HeLa  NH24[GNHfW6ldHnvckBCe3OjeR?= MWmxNEDPxE4EoB?= NVyxUFBDPyCq Mnq5SG1UVw>? M{\zVoRqe3K3cITzJI5wem2jbDDzdIlv\GynIHPo[YNseG:rboSg[pVv[3Srb36= NGXVcHIzODV|OEi0NC=>
PBMC  MlrHRZBweHSxc3nzJGF{e2G7 M3vvblAvPS9{L{Og{txO M1HlZ|I1NzR6IHi= MnT5bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MXmyNFQxPjl2Nx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Ac-H3 / Ac-H4 / Ac-tubulin ; 

PubMed: 29186204     


Mocetinostat increased acetylated histone 3 and 4 in a time- and dose-dependent manner in LMS cells. Mocetinostat did not increase acetylated tubulin expression.

Bad / Bid / Bak / Puma / Bax / Cleaved caspase-9 / Cleaved caspase-3 / Cleaved PARP; 

PubMed: 27551526     


(a and b) DU-145 cells were treated with various doses of mocetinostat for 24 h. Western blotting was performed using the indicated antibodies. 

29186204 27551526
Immunofluorescence
Nanog / MHC ; 

PubMed: 26240433     


c-Kit+ cells were treated with 2 µM MOCE for 2 or 7 days, as indicated. The cells were double-labeled with anti-Nanog (green) and anti-αMHC (red) antibodies. Nuclei were stained with DAPI (blue). The upper right section of each panel shows the enlargement of the box-selected area. Scale bars = 20 µm.

E-cadherin / ZEB1 ; 

PubMed: 25872941     


Immunoblot and immunofluorescence showing that mocetinostat treatment (1 μM, 48 h) reduced ZEB1 expression and induced E-cadherin in Panc1. Expression of histone deacetylases was not altered by mocetinostat, but histone acetylation was induced. Scale bar 10 μm.

26240433 25872941
Growth inhibition assay
Cell viability; 

PubMed: 26378038     


B. Cells were treated with increasing concentrations of mocetinostat for 48 hours and assayed by the WST-1 cell viability assay. C. IC50 values were calculated by the GraphPad Prism software. 

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

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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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT02805660 Active not recruiting Drug: mocetinostat|Drug: durvalumab Advanced Cancer Mirati Therapeutics Inc. May 2016 Phase 1|Phase 2
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID