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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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 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[0PEBp NEXGRnFKSzVyPUOuNFQh|ryP NHjJRowzPjN5OECzPC=>
BT549 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmr3OFghcA>? NWLLcZhvUUN3ME20MlM5KM7:TR?= NGLxS4ozPjN5OECzPC=>
MCF7 M2[yNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LpOFQ5KGh? NEiyVGtKSzVyPUCuOlch|ryP MWSyOlM4QDB|OB?=
T47D M323Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUi0PEBp M4j0WWlEPTB;MT6xO{DPxE1? NEXpZWYzPjN5OECzPC=>
MOLP8 M3raVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFf2OnY1QCCq NXvK[2NzUUN3ME2wMlbDuSByLkC0{txO NUX0fJZbOjZyOUG1NVg>
Panc1 M3O0TGZ2dmO2aX;uJGF{e2G7 NV3zOIZ1OC53L{GvNk42KM7:TR?= MnvGOFghcA>? M{TzbGROW09? NH2wZVF2eHKnZ4XsZZRmeyCvaWKtNlA{ MVGyOVg4Ojl2MR?=
Panc1 NXrtUIp[TnWwY4Tpc44hSXO|YYm= NF36[WQxNjVxMT:yMlUh|ryP NFfRN3A1QCCq NYSyVIE5TE2VTx?= NWXST4E6emWmdXPld{BmgHC{ZYPzbY9vKG:oIGrFRlEhd25iYn;0bEBuWk6DIHHu[EBxem:2ZXnuJIxmfmWuwrC= NEXiN2szPTh5Mkm0NS=>
Panc1 NVvFVIpGSXCxcITvd4l{KEG|c3H5 NIPU[HAyyqEQvF2= M{T6TFczyqCq NIjjc5FFVVOR NWLvXJFwe2Wwc3n0bZpmeyCSYX7jNUBk\WyuczDmc5Ih\2WvY3n0ZYJqdmVvaX7keYNm\CCjcH;weI9{cXN? MYGyOVg4Ojl2MR?=
Panc1 NFTXRXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{PHWVHDqM7:TR?= Mn;jO|LDqGh? M{SybWROW09? NF3rVYpmdmijbnPld{Bo\W2laYThZolv\S2rbnT1Z4V{KGOnbHygeoli[mmuaYT5JIRm[3KnYYPl Mnq1NlU5PzJ7NEG=
MMCs M3v4N2Z2dmO2aX;uJGF{e2G7 NIC3[W0yKM7:bR?= MlXCNE01QCCq MYHpcoNz\WG|ZYOgUnBTSSCycn;0[YlvKGW6cILld5Nqd28EoEKuO-KBmzNwNTDmc4xl NX7qZ5pMOjR2NUGzO|g>
MMCs Mnq5SpVv[3Srb36gRZN{[Xl? M33UNVAvPS9zIN88US=> M3rFXFI1KGh? M3TtUpNpd3e|IES1MYZwdGRic4TpcZVt[XSrb36gbY4h[0ePUDDs[ZZmdHN? MWiyOFQ2OTN5OB?=
MMCs MoHzSpVv[3Srb36gRZN{[Xl? Ml\uNeKh|ryP MYWyOEBp NI\E[ldqdmO{ZXHz[ZMhUEGWIHHjeIl3cXS7 NXzlbINmOjR2NUGzO|g>
MMCs M{HEO2Z2dmO2aX;uJGF{e2G7 M1TFOFHDqM7:TR?= MUGyOEBp NIDlW5BifWevZX70d{BodG:kYXygZYNmfHmuYYTpc44hdGW4ZXzzJI9nKGirc4TvcoUhUDNvS{mvNVQhMEh|LVu5M|E1[WNrIHHu[EBJPC2NMUKgLGg1NUtzMnHjLS=> NHLwfYkzPDR3MUO3PC=>
MMCs MX;GeY5kfGmxbjDBd5NigQ>? M1P4[lHDqM7:TR?= M2H3eFYuOjRiaB?= NGDZ[ZNld3OnLXTldIVv\GWwdHz5JIlvcGmkaYTzJJRp\SC2cnnt[ZRpgWyjdHnvckBt\X[nbDDv[kBJOy2NOTCoTFMuUzmvZUOp MkXTNlQ1PTF|N{i=
BxPC-3 NEnhXmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zHcGVEPTB;MT6xJO69VQ>? NITTdnMzOTN5NU[3PS=>
AsPC-1 Mlv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3GwO2VEPTB;Mz65JO69VQ>? Mn;qNlE{PzV4N{m=
MiaPaca-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LDdmVEPTB;MD62JO69VQ>? NWjDXVdHOjF|N{W2O|k>
Panc-1 NI\yO2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXwV4NGSzVyPUGuPEDPxE1? NX;ROVd3OjF|N{W2O|k>
PAXF 546L† M3PM[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\ZPGVEPTB;MT61JO69VQ>? MoD5NlE{PzV4N{m=
PAXF 1657L† NXy3SXNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLFR|UxRTBwMzFOwG0> NVnkXpdoOjF|N{W2O|k>
HCT15 NIrZNG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfKcXJKSzVyPUCuO{DPxE1? MnXSNlE{OTd2NUW=
HT-29 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfBOmFLUUN3ME2wMlch|ryP NEnpW28zOTNzN{S1OS=>
SW48 Ml;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwODFOwG0> NFO1N5AzOTNzN{S1OS=>
SW620 NVvuOYNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHEblU6UUN3ME2xJO69VQ>? M2DSblIyOzF5NEW1
HMEC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTjOZZ6UUN3ME2xPUDPxE1? M3XMSFIyOzF5NEW1
ANBL6  NIjscmNHfW6ldHnvckBCe3OjeR?= NIHhbVAyyqEQvF2= NHn5UnEzPCCq NGq3cJhmdmijbnPld{A2NUGFLXnu[JVk\WRiTVHHSU1COyCpZX7lJIV5eHKnc4Ppc44> M3rYZ|IyOTdzOEKx
LP1 NV;pXIY5TnWwY4Tpc44hSXO|YYm= NFnEe4QyyqEQvF2= NHr2PJczPCCq M3fGboVvcGGwY3XzJFUuSUNvaX7keYNm\CCPQVfFMWE{KGenbnWg[ZhxemW|c3nvci=> MlTSNlEyPzF6MkG=
HD-LM2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fO[lczyqCq MojISG1UVw>? NIfRbG5KSzVyPUGuPFgh|ryP MUiyNFg5ODFyNx?=
L428 MnfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1S5dlczyqCq MUjEUXNQ MWHJR|UxRTFwOU[g{txO MVmyNFg5ODFyNx?=
KM-H2 M3;6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlH5O|LDqGh? MVHEUXNQ MXvJR|UxRTJwOE[g{txO NX;ic5lWOjB6OECxNFc>
HD-LM2 M4X5bGZ2dmO2aX;uJGF{e2G7 NW[3fXR7OC5zLUKg{txO M3HpdVI1KGkEoB?= NFXESZNFVVOR NGLMeJp{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx M4f6OVIxQDhyMUC3
L428 MYnGeY5kfGmxbjDBd5NigQ>? NYfnWINHOC5zLUKg{txO MXiyOEBpyqB? NF[0RphFVVOR MnXXd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= M{jifVIxQDhyMUC3
KM-H2 MVfGeY5kfGmxbjDBd5NigQ>? M1:4XFAvOS1{IN88US=> MV6yOEBpyqB? NXf0UFd4TE2VTx?= NVvrOVh5e2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=> NWriVHpDOjB6OECxNFc>
HD-LM2 MXfBdI9xfG:|aYOgRZN{[Xl? Mn25NE4yNzBwNT:xJO69VQ>? MYq0PEBp MV7EUXNQ NHTOOYlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NILweI8zODh6MEGwOy=>
L428 M4HZZWFxd3C2b4Ppd{BCe3OjeR?= NEKzepIxNjFxMD61M|Eh|ryP NGj3R5I1QCCq MUnEUXNQ NHHTNWlqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NXntNW1[OjB6OECxNFc>
KM-H2 NF3KdHlCeG:ydH;zbZMhSXO|YYm= Mkn5NE4yNzBwNT:xJO69VQ>? NFnEbWQ1QCCq MYTEUXNQ MXfpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 NVvCXFRyOjB6OECxNFc>
HD-LM2 NVu5PZY5TnWwY4Tpc44hSXO|YYm= NUHTToZ6OcLizszN M2fXZ|I1NzR6IHi= MVnEUXNQ M4\EbIRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> NXfkW2VLOjB6OECxNFc>
L428 NV;QdphHTnWwY4Tpc44hSXO|YYm= M2XKZ|HDqM7:TR?= NWize3pzOjRxNEigbC=> NYLadFhKTE2VTx?= MX3kc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz MkLGNlA5QDBzMEe=
KM-H2 M3zhdmZ2dmO2aX;uJGF{e2G7 MmexNeKh|ryP MmT3NlQwPDhiaB?= MV7EUXNQ M{DufIRwf26{ZXf1cIF1\XNiWFnBVEwh[WO2aY\heIVlKGOjc4Dhd4V{KDliYX7kJFM> MlH3NlA5QDBzMEe=
HD-LM2 Mn75SpVv[3Srb36gRZN{[Xl? NF[5eJkxNjVxMTFOwG0> NUL2fGVGOjRxNEigbC=> MVHEUXNQ NWezfog4fXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NF74UoUzODh6MEGwOy=>
L428 M3zN[2Z2dmO2aX;uJGF{e2G7 MnqwNE42NzFizszN M3;rRlI1NzR6IHi= MnvjSG1UVw>? Mm\SeZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= Mn73NlA5QDBzMEe=
KM-H2 NEjaUmJHfW6ldHnvckBCe3OjeR?= MkDTNE42NzFizszN MnjGNlQwPDhiaB?= NEX4[JNFVVOR Ml;seZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MmjiNlA5QDBzMEe=
HD-LM2 Ml;wSpVv[3Srb36gRZN{[Xl? MV6xxsDPxE1? NFPMXZQxNjJ3LUS4JIg> NFfPSIVFVVOR NV;Q[4ps[WO2aY\heIV{KE6ILXvC M{fYb|IxQDhyMUC3
L428 NIHOXWxHfW6ldHnvckBCe3OjeR?= Mlf5NeKh|ryP NVT4[WdlOC5{NT20PEBp NXvKUHhGTE2VTx?= MV3hZ5RqfmG2ZYOgUmYuc0J? NVrTPHpJOjB6OECxNFc>
KM-H2 MnLSSpVv[3Srb36gRZN{[Xl? MUGxxsDPxE1? NUjpUFNkOC5{NT20PEBp NF60WWpFVVOR NFLi[m9i[3SrdnH0[ZMhVkZva1K= MX6yNFg5ODFyNx?=
H526 NHXIcmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkf5TWM2OD12OECgcm0> M3;EZVIxPjh{NkSz
H146 NXuwXVM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn2zTWM2OD1|NTDuUS=> MXyyNFY5OjZ2Mx?=
H82 NFmyZYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzufI5KSzVyPUK1NEBvVQ>? MXSyNFY5OjZ2Mx?=
DMS114 NFTnZnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnOSnJEUUN3ME22OFAhdk1? NVzrS45ZOjB4OEK2OFM>
HeLa MYfGeY5kfGmxbjDBd5NigQ>? MlK1NE4{NTFyIN88US=> MUO4JIg> NYqy[5kyTE2VTx?= MV;pcoNz\WG|ZYOgZYNmfHmuYYTl[EBJOyCNOTCoTFNMQUGlKTDheEAyOCEQvF2= NGCwbZQzODV|OEi0NC=>
HeLa MnPtSpVv[3Srb36gRZN{[Xl? NGfTSXAxNjNvMUCg{txO MY[4JIg> NIqzZXhFVVOR NIThbWNqdmO{ZXHz[ZMh[2G|cHHz[UA{KGGwZDC3JIFkfGm4YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> MX2yNFU{QDh2MB?=
HeLa M4jmXWZ2dmO2aX;uJGF{e2G7 MVSxNEDPxE4EoB?= Mn[1Ok8yOi9{NDDo NETq[4pFVVOR MYXpcoR2[2W|IH3peI91cWNiYXPjeY12dGG2aX;uJIFv\CCmZXzhfYVlKHB{MTDlfJBz\XO|aX;u M3r4XFIxPTN6OESw
HeLa  NVT5SZc3TnWwY4Tpc44hSXO|YYm= MX[xNEDPxE4EoB?= NWTJd|lTPyCq MkHjSG1UVw>? NH\PdHZlcXO{dYD0d{Bvd3KvYXygd5BqdmSuZTDjbIVkc3CxaX70JIZ2dmO2aX;u NV[wNY9iOjB3M{i4OFA>
PBMC  MX;BdI9xfG:|aYOgRZN{[Xl? M3;wd|AvPS9{L{Og{txO MnT0NlQwPDhiaB?= NGnIOmJqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MYiyNFQxPjl2Nx?=

... 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID