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 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 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TwfVQ5KGh? MX\JR|UxRTNwMESg{txO MV[yOlM4QDB|OB?=
BT549 NYnRR2lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\NVVQ5KGh? NIHaXlNKSzVyPUSuN|gh|ryP NUTwOJlCOjZ|N{iwN|g>
MCF7 M4LEVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUS0PEBp MkPsTWM2OD1yLk[3JO69VQ>? NVLYRpBnOjZ|N{iwN|g>
T47D NWfoRmVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVi0PEBp NFvJ[5RKSzVyPUGuNVch|ryP MXqyOlM4QDB|OB?=
MOLP8 M1PDS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF25Uo41QCCq MlzvTWM2OD1yLkdCtUAxNjB2zszN M3uwR|I3ODlzNUG4
Panc1 NHHZTYtHfW6ldHnvckBCe3OjeR?= Mn\HNE42NzFxMj61JO69VQ>? Mo[0OFghcA>? NILWXXZFVVOR M3jjfZVxemWpdXzheIV{KG2rUj2yNFM> M{iwOVI2QDd{OUSx
Panc1 NXnlZpY2TnWwY4Tpc44hSXO|YYm= NFLIR28xNjVxMT:yMlUh|ryP M{XuN|Q5KGh? MoPQSG1UVw>? MVfy[YR2[2W|IHX4dJJme3Orb36gc4YhYkWEMTDvckBjd3SqIH3SUmEh[W6mIIDyc5RmcW5ibHX2[YzDqA>? NYXnSG9MOjV6N{K5OFE>
Panc1 MnfRRZBweHSxc3nzJGF{e2G7 MWSxxsDPxE1? NVWyTotjPzMEoHi= MnfjSG1UVw>? M3nobZNmdnOrdHn6[ZMhWGGwY{GgZ4VtdHNiZn;yJIdmdWOrdHHibY5mNWmwZIXj[YQh[XCxcITvd4l{ NIPUNIIzPTh5Mkm0NS=>
Panc1 MlTPR4VtdCCYaXHibYxqfHliQYPzZZk> M2S5V|HDqM7:TR?= M1XI[FczyqCq M2nQSWROW09? M3y1d4VvcGGwY3XzJIdmdWOrdHHibY5mNWmwZIXj[ZMh[2WubDD2bYFjcWyrdImg[IVkemWjc3W= MmO0NlU5PzJ7NEG=
MMCs MXvGeY5kfGmxbjDBd5NigQ>? MkTiNUDPxG1? MVKwMVQ5KGh? MYfpcoNz\WG|ZYOgUnBTSSCycn;0[YlvKGW6cILld5Nqd28EoEKuO-KBmzNwNTDmc4xl M4q5dFI1PDVzM{e4
MMCs M1LOdGZ2dmO2aX;uJGF{e2G7 MkDhNE42NzFizszN MXiyOEBp NEe1eXh{cG:5czC0OU1nd2ymIIP0bY12dGG2aX;uJIlvKGOJTWCgcIV3\Wy| NHLM[JIzPDR3MUO3PC=>
MMCs MUjGeY5kfGmxbjDBd5NigQ>? MVSxxsDPxE1? MnXBNlQhcA>? M3v6PIlv[3KnYYPld{BJSVRiYXP0bZZqfHl? NIrqZW0zPDR3MUO3PC=>
MMCs Ml7QSpVv[3Srb36gRZN{[Xl? NHPKTWgyyqEQvF2= MknzNlQhcA>? NFP4[ZZifWevZX70d{BodG:kYXygZYNmfHmuYYTpc44hdGW4ZXzzJI9nKGirc4TvcoUhUDNvS{mvNVQhMEh|LVu5M|E1[WNrIHHu[EBJPC2NMUKgLGg1NUtzMnHjLS=> NFXmTlMzPDR3MUO3PC=>
MMCs NFnYe3JHfW6ldHnvckBCe3OjeR?= M3rIUFHDqM7:TR?= MVq2MVI1KGh? M1TQSIRwe2VvZHXw[Y5l\W62bImgbY5pcWKrdIOgeIhmKHS{aX3leIh6dGG2aX;uJIxmfmWuIH;mJGg{NUt7IDjIN{1MQW2nMzm= MYGyOFQ2OTN5OB?=
BxPC-3 MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;KSWM2OD1zLkGg{txO MW[yNVM4PTZ5OR?=
AsPC-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXWV2lGSzVyPUOuPUDPxE1? NETqWHMzOTN5NU[3PS=>
MiaPaca-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;xRmVEPTB;MD62JO69VQ>? NXTjfZZbOjF|N{W2O|k>
Panc-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjLSWM2OD1zLkig{txO NH\KcWIzOTN5NU[3PS=>
PAXF 546L† MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjRb5kyTUN3ME2xMlUh|ryP NHrDVIczOTN5NU[3PS=>
PAXF 1657L† M1PjNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LYeWVEPTB;MD6zJO69VQ>? NHjNNYEzOTN5NU[3PS=>
HCT15 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwNzFOwG0> NW\S[I5jOjF|MUe0OVU>
HT-29 NGS4WItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkToTWM2OD1yLkeg{txO NYns[m1TOjF|MUe0OVU>
SW48 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3TWIhKSzVyPUCuPEDPxE1? MXqyNVMyPzR3NR?=
SW620 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnqwTWM2OD1zIN88US=> MoixNlE{OTd2NUW=
HMEC NXrM[FdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrXRllOUUN3ME2xPUDPxE1? MVqyNVMyPzR3NR?=
ANBL6  M1rYXWZ2dmO2aX;uJGF{e2G7 MWmxxsDPxE1? NWjHUldOOjRiaB?= NYDLVIRQ\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v NF\kVIQzOTF5MUiyNS=>
LP1 MlPhSpVv[3Srb36gRZN{[Xl? MWWxxsDPxE1? MYOyOEBp NX7NR3Jn\W6qYX7j[ZMhPS2DQz3pcoR2[2WmIF3BS2UuSTNiZ3Xu[UBmgHC{ZYPzbY9v M2jINVIyOTdzOEKx
HD-LM2 M3zmVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDkZWx7PzMEoHi= MnfOSG1UVw>? NEXxW5dKSzVyPUGuPFgh|ryP NVTheWVuOjB6OECxNFc>
L428 M{XyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XQflczyqCq NH;rTJdFVVOR Mmn3TWM2OD1zLkm2JO69VQ>? NHjVTmgzODh6MEGwOy=>
KM-H2 M1f3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUC3NuKhcA>? NHnXbpZFVVOR Ml3ZTWM2OD1{Lki2JO69VQ>? MVGyNFg5ODFyNx?=
HD-LM2 M2fqV2Z2dmO2aX;uJGF{e2G7 M{HzZVAvOS1{IN88US=> M4HGS|I1KGkEoB?= M2rF[2ROW09? NH3BUmx{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx NEX4bpMzODh6MEGwOy=>
L428 MonjSpVv[3Srb36gRZN{[Xl? M2WzNVAvOS1{IN88US=> M1H3Z|I1KGkEoB?= M2n3bmROW09? NFy1cZR{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx NEfTR5kzODh6MEGwOy=>
KM-H2 NXWzeYk2TnWwY4Tpc44hSXO|YYm= MmGwNE4yNTJizszN MXeyOEBpyqB? Mmf4SG1UVw>? NG\STZV{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx NU\KO4VkOjB6OECxNFc>
HD-LM2 M{e1T2Fxd3C2b4Ppd{BCe3OjeR?= MXGwMlEwOC53L{Gg{txO MXS0PEBp Mo[4SG1UVw>? NEC4fXVqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M4XPTFIxQDhyMUC3
L428 NGj6XphCeG:ydH;zbZMhSXO|YYm= MUOwMlEwOC53L{Gg{txO MXy0PEBp M3TZO2ROW09? NVzxR3JucW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> MlPPNlA5QDBzMEe=
KM-H2 MYPBdI9xfG:|aYOgRZN{[Xl? M1\zelAvOS9yLkWvNUDPxE1? MlPOOFghcA>? NWX3VoxyTE2VTx?= MkTwbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MUCyNFg5ODFyNx?=
HD-LM2 NV;VfYlwTnWwY4Tpc44hSXO|YYm= MlXtNeKh|ryP NG\GUY8zPC92ODDo M3n6[WROW09? Mo\S[I94dnKnZ4XsZZRmeyC[SVHQMEBi[3SrdnH0[YQh[2G|cHHz[ZMhQSCjbnSgNy=> M1\LVFIxQDhyMUC3
L428 MYrGeY5kfGmxbjDBd5NigQ>? NV:xO3Y2OcLizszN MVOyOE81QCCq M2fnU2ROW09? NVLmS2Vo\G:5boLl[5Vt[XSnczDYTWFRNCCjY4TpeoF1\WRiY3HzdIF{\XNiOTDhcoQhOw>? NGrY[JgzODh6MEGwOy=>
KM-H2 MlfoSpVv[3Srb36gRZN{[Xl? MVOxxsDPxE1? M3;tR|I1NzR6IHi= NUXmeYlmTE2VTx?= MU\kc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz Ml\ZNlA5QDBzMEe=
HD-LM2 NWHENHFSTnWwY4Tpc44hSXO|YYm= NFPyNJAxNjVxMTFOwG0> MYOyOE81QCCq M{LWPWROW09? NWjGfnE1fXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MkO5NlA5QDBzMEe=
L428 NWDhNlRNTnWwY4Tpc44hSXO|YYm= NIfNT5ExNjVxMTFOwG0> NGXTSVMzPC92ODDo M4\Te2ROW09? NH:1cY92eHKnZ4XsZZRmeyCWTl[t{tEh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M{DYNVIxQDhyMUC3
KM-H2 M1PibGZ2dmO2aX;uJGF{e2G7 MUOwMlUwOSEQvF2= MX2yOE81QCCq NEW4VmFFVVOR MWH1dJJm\3WuYYTld{BVVkZvzsGg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M4O4N|IxQDhyMUC3
HD-LM2 MVXGeY5kfGmxbjDBd5NigQ>? NWnR[VdyOcLizszN MlnwNE4zPS12ODDo M1;lWWROW09? NFzheZNi[3SrdnH0[ZMhVkZva1K= NHTPS3QzODh6MEGwOy=>
L428 M2PCeWZ2dmO2aX;uJGF{e2G7 MWexxsDPxE1? NXLxN21QOC5{NT20PEBp MU\EUXNQ NGHyNJZi[3SrdnH0[ZMhVkZva1K= M3LHZlIxQDhyMUC3
KM-H2 Mo\1SpVv[3Srb36gRZN{[Xl? MnvONeKh|ryP MWqwMlI2NTR6IHi= MWLEUXNQ NGrjc4Vi[3SrdnH0[ZMhVkZva1K= MV2yNFg5ODFyNx?=
H526 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFz4XmpKSzVyPUS4NEBvVQ>? MXuyNFY5OjZ2Mx?=
H146 NY\tbFU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jNUWlEPTB;M{Wgcm0> NV\iOZVPOjB4OEK2OFM>
H82 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PwU2lEPTB;MkWwJI5O MWKyNFY5OjZ2Mx?=
DMS114 MoSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHITWM2OD14NECgcm0> M1PtfFIxPjh{NkSz
HeLa NGT4OnNHfW6ldHnvckBCe3OjeR?= NFPNPXgxNjNvMUCg{txO MUK4JIg> M3zSWGROW09? M1XZVolv[3KnYYPld{Bi[2W2eXzheIVlKEh|IFu5JEhJO0t7QXOpJIF1KDFyIN88US=> MW[yNFU{QDh2MB?=
HeLa MU\GeY5kfGmxbjDBd5NigQ>? MnzzNE4{NTFyIN88US=> M1XQNVghcA>? MYnEUXNQ NXjrWm9RcW6lcnXhd4V{KGOjc4Dhd4UhOyCjbnSgO{Bi[3SrdnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> M3\0UVIxPTN6OESw
HeLa MWLGeY5kfGmxbjDBd5NigQ>? NInKdYMyOCEQvF5CpC=> M1v5dVYwOTJxMkSgbC=> MlqwSG1UVw>? M4W5bYlv\HWlZYOgcYl1d3SrYzDhZ4N2dXWuYYTpc44h[W6mIHTlcIF6\WRicEKxJIV5eHKnc4Ppc44> NEDVRZEzODV|OEi0NC=>
HeLa  M1L2c2Z2dmO2aX;uJGF{e2G7 M2WybVExKM7:TdMg MXS3JIg> M2HF[2ROW09? Ml\4[Il{enWydIOgco9zdWGuIIPwbY5ldGViY3jlZ4txd2mwdDDmeY5kfGmxbh?= M1fuNVIxPTN6OESw
PBMC  NUDlc5pqSXCxcITvd4l{KEG|c3H5 MXuwMlUwOi9|IN88US=> MlG0NlQwPDhiaB?= MWHpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGGwZDD0bY1mKGSncHXu[IVvfGy7 NIrWbXYzODRyNkm0Oy=>

... 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]
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  • 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