Mocetinostat (MGCD0103)

For research use only. Not for use in humans.

Catalog No.S1122 Synonyms: MG0103

57 publications

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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Selleck's Mocetinostat (MGCD0103) has been cited by 57 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 NVP4fYlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XFVVQ5KGh? NFG2RoRKSzVyPUOuNFQh|ryP NXrQWYtTOjZ|N{iwN|g>
BT549 NXv3OIpUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnGVJFTPDhiaB?= M{LMZWlEPTB;ND6zPEDPxE1? NVj0TWNmOjZ|N{iwN|g>
MCF7 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXy0PEBp NHu4ZnZKSzVyPUCuOlch|ryP NITIUFczPjN5OECzPC=>
T47D MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPVOXM1QCCq NV7CNGgyUUN3ME2xMlE4KM7:TR?= M1z2[|I3Ozd6MEO4
MOLP8 NX32RoZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUS0PEBp MnjFTWM2OD1yLkdCtUAxNjB2zszN NXuzbGFlOjZyOUG1NVg>
Panc1 Ml7mSpVv[3Srb36gRZN{[Xl? MWOwMlUwOS9{LkWg{txO M2q4[FQ5KGh? MXLEUXNQ NXr5[|B7fXC{ZXf1cIF1\XNibXnSMVIxOw>? MVmyOVg4Ojl2MR?=
Panc1 NHL3b25HfW6ldHnvckBCe3OjeR?= Mk\BNE42NzFxMj61JO69VQ>? MnjoOFghcA>? NIXKTpdFVVOR MYjy[YR2[2W|IHX4dJJme3Orb36gc4YhYkWEMTDvckBjd3SqIH3SUmEh[W6mIIDyc5RmcW5ibHX2[YzDqA>? NHfW[FAzPTh5Mkm0NS=>
Panc1 M4fTOmFxd3C2b4Ppd{BCe3OjeR?= MmW5NeKh|ryP MmHrO|LDqGh? NV7CN3JVTE2VTx?= MVfz[Y5{cXSrenXzJHBidmNzIHPlcIx{KG[xcjDn[Y1kcXSjYnnu[U1qdmS3Y3XkJIFxd3C2b4Ppdy=> NI[3Oo4zPTh5Mkm0NS=>
Panc1 NX\uSW92S2WubDDWbYFjcWyrdImgRZN{[Xl? M1HvWFHDqM7:TR?= MnXrO|LDqGh? NX;tSlVTTE2VTx?= Mnix[Y5p[W6lZYOg[4Vu[2m2YXLpcoUucW6mdXPld{Bk\WyuII\pZYJqdGm2eTDk[YNz\WG|ZR?= NGe2cGUzPTh5Mkm0NS=>
MMCs MWjGeY5kfGmxbjDBd5NigQ>? NEjZVnYyKM7:bR?= NWLLWW4zOC12ODDo M1W3Volv[3KnYYPld{BPWFKDIIDyc5RmcW5iZYjwdoV{e2mxbtMgNk446oDVMz61JIZwdGR? NIXQWlMzPDR3MUO3PC=>
MMCs NHrWfFVHfW6ldHnvckBCe3OjeR?= NV;hTml4OC53L{Gg{txO M3HITlI1KGh? MU\zbI94eyB2NT3mc4xlKHO2aX31cIF1cW:wIHnuJINIVVBibHX2[Yx{ MXKyOFQ2OTN5OB?=
MMCs NWWydlA1TnWwY4Tpc44hSXO|YYm= NFnxcnIyyqEQvF2= NFHOOowzPCCq MlXObY5kemWjc3XzJGhCXCCjY4Tpeol1gQ>? Mn;ZNlQ1PTF|N{i=
MMCs NHztOZFHfW6ldHnvckBCe3OjeR?= NUXWbJlFOcLizszN M{LwS|I1KGh? NHTmO5JifWevZX70d{BodG:kYXygZYNmfHmuYYTpc44hdGW4ZXzzJI9nKGirc4TvcoUhUDNvS{mvNVQhMEh|LVu5M|E1[WNrIHHu[EBJPC2NMUKgLGg1NUtzMnHjLS=> NXm4UoRLOjR2NUGzO|g>
MMCs MV;GeY5kfGmxbjDBd5NigQ>? MWexxsDPxE1? MYS2MVI1KGh? Ml\K[I9{\S2mZYDlcoRmdnSueTDpcohq[mm2czD0bIUhfHKrbXX0bJlt[XSrb36gcIV3\Wxib3[gTFMuUzliKFizMWs6dWV|KR?= NWDpfG9uOjR2NUGzO|g>
BxPC-3 NXrOd5dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr5XJZoTUN3ME2xMlEh|ryP Mon5NlE{PzV4N{m=
AsPC-1 MnLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\SZmVEPTB;Mz65JO69VQ>? NUfpd4hlOjF|N{W2O|k>
MiaPaca-2 M4L3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LDTWVEPTB;MD62JO69VQ>? NVm3eo9EOjF|N{W2O|k>
Panc-1 Ml71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDvUJl6TUN3ME2xMlgh|ryP M1fZR|IyOzd3Nke5
PAXF 546L† MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjRSWM2OD1zLkWg{txO MmrMNlE{PzV4N{m=
PAXF 1657L† NFzBV4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETZdYFGSzVyPUCuN{DPxE1? M{TKfFIyOzd3Nke5
HCT15 MmLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwNzFOwG0> MY[yNVMyPzR3NR?=
HT-29 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojuTWM2OD1yLkeg{txO MXGyNVMyPzR3NR?=
SW48 M3\nbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTBwODFOwG0> MUiyNVMyPzR3NR?=
SW620 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr3VI1KSzVyPUGg{txO NYHCUW1MOjF|MUe0OVU>
HMEC NXnx[m52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrlTWM2OD1zOTFOwG0> M1n2NFIyOzF5NEW1
ANBL6  NYm1RlVKTnWwY4Tpc44hSXO|YYm= MXWxxsDPxE1? MljMNlQhcA>? MUjlcohidmOnczC1MWFENWmwZIXj[YQhVUGJRT3BN{Bo\W6nIHX4dJJme3Orb36= NGPocIQzOTF5MUiyNS=>
LP1 NWHLcYJxTnWwY4Tpc44hSXO|YYm= M{\rOlHDqM7:TR?= M3fnWVI1KGh? NYrpdGtt\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v M2rVdVIyOTdzOEKx
HD-LM2 NXLnOWtTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUi3NuKhcA>? NYniR|NqTE2VTx?= MYLJR|UxRTFwOEig{txO Mn\PNlA5QDBzMEe=
L428 MnvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHHc5VWPzMEoHi= NHi0OJNFVVOR NFK2NpFKSzVyPUGuPVYh|ryP NVXsV5dQOjB6OECxNFc>
KM-H2 M{e4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoqyO|LDqGh? MXTEUXNQ NWjmNmlSUUN3ME2yMlg3KM7:TR?= NWXrT|lUOjB6OECxNFc>
HD-LM2 MVTGeY5kfGmxbjDBd5NigQ>? M4PGelAvOS1{IN88US=> MnPSNlQhcMLi MUPEUXNQ Ml\Hd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= NYrXbm5yOjB6OECxNFc>
L428 M3P6UGZ2dmO2aX;uJGF{e2G7 MWqwMlEuOiEQvF2= NVnSPY5oOjRiaNMg MXzEUXNQ NULkXm1Fe2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=> M3jFfVIxQDhyMUC3
KM-H2 MXfGeY5kfGmxbjDBd5NigQ>? M4DIW|AvOS1{IN88US=> NXruS|czOjRiaNMg M1TnRmROW09? MkTJd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= MoHTNlA5QDBzMEe=
HD-LM2 M1HjZ2Fxd3C2b4Ppd{BCe3OjeR?= NIfxSXkxNjFxMD61M|Eh|ryP NHKzRoI1QCCq M3fzTmROW09? NIfpSnBqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NVfud4RvOjB6OECxNFc>
L428 MoTHRZBweHSxc3nzJGF{e2G7 M{fDZlAvOS9yLkWvNUDPxE1? MWq0PEBp NE\DTm9FVVOR NHPqRVdqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MnXyNlA5QDBzMEe=
KM-H2 M4fjeGFxd3C2b4Ppd{BCe3OjeR?= M1nkOFAvOS9yLkWvNUDPxE1? NWLOO5piPDhiaB?= MoPTSG1UVw>? MX;pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M1PY[|IxQDhyMUC3
HD-LM2 M{Ta[mZ2dmO2aX;uJGF{e2G7 M2X0clHDqM7:TR?= Ml3INlQwPDhiaB?= M4TI[mROW09? MWHkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz NIDNUoYzODh6MEGwOy=>
L428 NUnkZ2hWTnWwY4Tpc44hSXO|YYm= MYGxxsDPxE1? MXKyOE81QCCq M{DjVGROW09? NYLsdItz\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? M3Pa[lIxQDhyMUC3
KM-H2 M3rsVGZ2dmO2aX;uJGF{e2G7 M1fL[VHDqM7:TR?= MmLRNlQwPDhiaB?= MX;EUXNQ NVfHR5JD\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? MoDHNlA5QDBzMEe=
HD-LM2 NYfwR2hYTnWwY4Tpc44hSXO|YYm= M2S3O|AvPS9zIN88US=> MYeyOE81QCCq MY\EUXNQ NUnwSVVyfXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> M1;oN|IxQDhyMUC3
L428 M13ENGZ2dmO2aX;uJGF{e2G7 NUHpcodiOC53L{Gg{txO NVTadpdIOjRxNEigbC=> NXjvN5VvTE2VTx?= NXfnNJpLfXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NXzrS|BWOjB6OECxNFc>
KM-H2 MX\GeY5kfGmxbjDBd5NigQ>? NXPSNpJWOC53L{Gg{txO NY[3dJRJOjRxNEigbC=> MVPEUXNQ NHO3SYZ2eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NEm0fmQzODh6MEGwOy=>
HD-LM2 NVnSU|E1TnWwY4Tpc44hSXO|YYm= M{LM[|HDqM7:TR?= NITYT2UxNjJ3LUS4JIg> M1qxRWROW09? MnPuZYN1cX[jdHXzJG5HNWuE NWTOdY1VOjB6OECxNFc>
L428 NFLXZ4lHfW6ldHnvckBCe3OjeR?= MlXuNeKh|ryP NELFW4sxNjJ3LUS4JIg> NYfROnE{TE2VTx?= M33qT4FkfGm4YYTld{BPTi2tQh?= Mk\HNlA5QDBzMEe=
KM-H2 MWTGeY5kfGmxbjDBd5NigQ>? M3rCdlHDqM7:TR?= NIC2[I8xNjJ3LUS4JIg> MnS5SG1UVw>? MWnhZ5RqfmG2ZYOgUmYuc0J? NV3YS4JjOjB6OECxNFc>
H526 NETscYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmn2TWM2OD12OECgcm0> NX3sN3drOjB4OEK2OFM>
H146 M1f1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fSNmlEPTB;M{Wgcm0> M3zlOVIxPjh{NkSz
H82 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TmNmlEPTB;MkWwJI5O NUPJTYdsOjB4OEK2OFM>
DMS114 MkLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\rPXNKSzVyPU[0NEBvVQ>? M3OycVIxPjh{NkSz
HeLa MnqxSpVv[3Srb36gRZN{[Xl? NEXqVnQxNjNvMUCg{txO MmDWPEBp NVm3OWVHTE2VTx?= NF;mXWFqdmO{ZXHz[ZMh[WOndInsZZRm\CCKMzDLPUApUDONOVHjLUBifCBzMDFOwG0> NG\UfVIzODV|OEi0NC=>
HeLa MkTTSpVv[3Srb36gRZN{[Xl? NELOPI0xNjNvMUCg{txO NEXpWog5KGh? NIXRbmFFVVOR NGPpWGpqdmO{ZXHz[ZMh[2G|cHHz[UA{KGGwZDC3JIFkfGm4YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> NGrRSZAzODV|OEi0NC=>
HeLa M4XnR2Z2dmO2aX;uJGF{e2G7 MlTaNVAh|ryPwrC= MXe2M|EzNzJ2IHi= MWPEUXNQ NI\Vd49qdmS3Y3XzJI1qfG:2aXOgZYNkfW23bHH0bY9vKGGwZDDk[YxigWWmIICyNUBmgHC{ZYPzbY9v NIrN[ZAzODV|OEi0NC=>
HeLa  MnXoSpVv[3Srb36gRZN{[Xl? NFXQ[20yOCEQvF5CpC=> NH\sdJU4KGh? NIP0dVlFVVOR NIT6VWdlcXO{dYD0d{Bvd3KvYXygd5BqdmSuZTDjbIVkc3CxaX70JIZ2dmO2aX;u M4jyd|IxPTN6OESw
PBMC  MUXBdI9xfG:|aYOgRZN{[Xl? NWrpRnZ{OC53L{KvN{DPxE1? NWjndZZFOjRxNEigbC=> NHPy[YNqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MVKyNFQxPjl2Nx?=

... 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]
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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]
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  • 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]
- Collapse
  • 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
Smiles NC1=CC=CC=C1NC(=O)C2=CC=C(CNC3=NC=CC(=N3)C4=CC=CN=C4)C=C2

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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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID