Mocetinostat (MGCD0103)

製品コードS1122 別名:MG0103

Mocetinostat (MGCD0103)化学構造

分子量(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.

サイズ 価格(税別)  
JPY 31540.00
JPY 28220.00
JPY 44820.00
JPY 78020.00
JPY 127820.00

カスタマーフィードバック(6)

  •  

    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.

  • 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.

  •  

    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.

    Western blot analysis of Acetyl-H3 and H3. 0-20μM MGCD0103 was added.

     

     

    Dr. Zhang of Tianjin Medical University. Mocetinostat (MGCD0103) purchased from Selleck.

製品安全説明書

HDAC阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 NVT0fINJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3qxTVQ5KGh? MljZTWM2OD1|LkC0JO69VQ>? M1;qNVI3Ozd6MEO4
BT549 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPsXG01QCCq M2PKdGlEPTB;ND6zPEDPxE1? MX6yOlM4QDB|OB?=
MCF7 Ml;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HpU|Q5KGh? MkHKTWM2OD1yLk[3JO69VQ>? M{LmOFI3Ozd6MEO4
T47D NUXjTpVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVv5VnM4PDhiaB?= MXnJR|UxRTFwMUeg{txO NV7rPFhpOjZ|N{iwN|g>
MOLP8 M{DBUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojUOFghcA>? NGHO[lVKSzVyPUCuOuKyKDBwMEVOwG0> NHjWXXEzPjB7MUWxPC=>
Panc1 Mn;YSpVv[3Srb36gRZN{[Xl? MnzENE42NzFxMj61JO69VQ>? NUfuW3huPDhiaB?= MXPEUXNQ M2DHW5VxemWpdXzheIV{KG2rUj2yNFM> NIXad|czPTh5Mkm0NS=>
Panc1 NE\4WYdHfW6ldHnvckBCe3OjeR?= MoPXNE42NzFxMj61JO69VQ>? NW\aXFh5PDhiaB?= M3LZRWROW09? NVe5WYszemWmdXPld{BmgHC{ZYPzbY9vKG:oIGrFRlEhd25iYn;0bEBuWk6DIHHu[EBxem:2ZXnuJIxmfmWuwrC= NF\6OVUzPTh5Mkm0NS=>
Panc1 NV\aN5NXSXCxcITvd4l{KEG|c3H5 M3yyNFHDqM7:TR?= M2PTblczyqCq NVH1dHJPTE2VTx?= MUTz[Y5{cXSrenXzJHBidmNzIHPlcIx{KG[xcjDn[Y1kcXSjYnnu[U1qdmS3Y3XkJIFxd3C2b4Ppdy=> NIL5b2kzPTh5Mkm0NS=>
Panc1 NFq4WIpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYKxxsDPxE1? M1LsVFczyqCq M2jTeGROW09? NF7UWohmdmijbnPld{Bo\W2laYThZolv\S2rbnT1Z4V{KGOnbHygeoli[mmuaYT5JIRm[3KnYYPl M1LH[FI2QDd{OUSx
MMCs Ml71SpVv[3Srb36gRZN{[Xl? NGi2dYkyKM7:bR?= M{XZSFAuPDhiaB?= MnnNbY5kemWjc3XzJG5RWkFicILveIVqdiCneIDy[ZN{cW:wwrCyMlfjiJN|LkWg[o9t\A>? MmjINlQ1PTF|N{i=
MMCs M{f5PWZ2dmO2aX;uJGF{e2G7 NXvrRmhtOC53L{Gg{txO MUSyOEBp Ml\vd4hwf3NiNEWt[o9t\CC|dHnteYxifGmxbjDpckBkT02SIHzleoVtew>? NFPjTnczPDR3MUO3PC=>
MMCs NVXiVHd{TnWwY4Tpc44hSXO|YYm= NHLTVooyyqEQvF2= M1jNSFI1KGh? MX3pcoNz\WG|ZYOgTGFVKGGldHn2bZR6 MkL4NlQ1PTF|N{i=
MMCs NUTtb|AyTnWwY4Tpc44hSXO|YYm= M1rnb|HDqM7:TR?= M33QcVI1KGh? M4KydoF2\22nboTzJIdtd2KjbDDhZ4V1gWyjdHnvckBt\X[nbIOgc4YhcGm|dH;u[UBJOy2NOT:xOEApUDNvS{mvNVRi[yliYX7kJGg1NUtzMjCoTFQuUzF{YXOp MnnrNlQ1PTF|N{i=
MMCs NHLWSFVHfW6ldHnvckBCe3OjeR?= NXG0RYZrOcLizszN NHz5OZc3NTJ2IHi= MnHV[I9{\S2mZYDlcoRmdnSueTDpcohq[mm2czD0bIUhfHKrbXX0bJlt[XSrb36gcIV3\Wxib3[gTFMuUzliKFizMWs6dWV|KR?= M3nPUlI1PDVzM{e4
BxPC-3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvsU2lRTUN3ME2xMlEh|ryP MnjKNlE{PzV4N{m=
AsPC-1 MnfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnFR|UxRTNwOTFOwG0> NX3yOIlzOjF|N{W2O|k>
MiaPaca-2 M2fuN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnvW|JGSzVyPUCuOkDPxE1? NVLrfIVYOjF|N{W2O|k>
Panc-1 NInwUFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\tT2NGSzVyPUGuPEDPxE1? MVyyNVM4PTZ5OR?=
PAXF 546L† NHPY[oFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;nSWM2OD1zLkWg{txO MXOyNVM4PTZ5OR?=
PAXF 1657L† NEK2[ZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NET6VWdGSzVyPUCuN{DPxE1? M2fKTVIyOzd3Nke5
HCT15 NHvjbWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwNzFOwG0> NV;wdlhEOjF|MUe0OVU>
HT-29 NFfQbZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfHfllKSzVyPUCuO{DPxE1? MnTTNlE{OTd2NUW=
SW48 NEjtVFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLJTWM2OD1yLkig{txO NUTNdGJNOjF|MUe0OVU>
SW620 NEDWUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TF[GlEPTB;MTFOwG0> NW\sU3piOjF|MUe0OVU>
HMEC NGXEcIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLwXJdQUUN3ME2xPUDPxE1? NGnmWJYzOTNzN{S1OS=>
ANBL6  MnvrSpVv[3Srb36gRZN{[Xl? M1zFWFHDqM7:TR?= MWiyOEBp NGC5T4JmdmijbnPld{A2NUGFLXnu[JVk\WRiTVHHSU1COyCpZX7lJIV5eHKnc4Ppc44> M3fleFIyOTdzOEKx
LP1 MkTOSpVv[3Srb36gRZN{[Xl? NWLjeIhiOcLizszN M2e2Z|I1KGh? NGixUJVmdmijbnPld{A2NUGFLXnu[JVk\WRiTVHHSU1COyCpZX7lJIV5eHKnc4Ppc44> NYq2NJFZOjFzN{G4NlE>
HD-LM2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHhTnlZPzMEoHi= NVPxWFh4TE2VTx?= M{mwVGlEPTB;MT64PEDPxE1? M2TYNVIxQDhyMUC3
L428 NVzONVM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:3NuKhcA>? M{XrSWROW09? NV7ZNoREUUN3ME2xMlk3KM7:TR?= MXWyNFg5ODFyNx?=
KM-H2 NVO5e5FqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXO3NuKhcA>? NYDWcWFSTE2VTx?= MX3JR|UxRTJwOE[g{txO NU\QTIpkOjB6OECxNFc>
HD-LM2 M4jUc2Z2dmO2aX;uJGF{e2G7 Mk[wNE4yNTJizszN NXn2ZYxvOjRiaNMg M2\lZmROW09? MnPMd4hwf3NiYXPleJlt[XSrb36gc4YhcGm|dH;u[UA{KGGwZDD1dJJm\3WuYYTpc44hd2ZidHjlJINmdGxiY4njcIUhemWpdXzheI9zgSCycn;0[YlvKHB{MR?= M4\W[lIxQDhyMUC3
L428 NE\vNHFHfW6ldHnvckBCe3OjeR?= M4LpSlAvOS1{IN88US=> NFr1WJYzPCCqwrC= M{LjcGROW09? NGSwfJZ{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx NWj4SmtiOjB6OECxNFc>
KM-H2 M{\l[2Z2dmO2aX;uJGF{e2G7 MXywMlEuOiEQvF2= MkC4NlQhcMLi MmjlSG1UVw>? MVfzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz NYLRSGxmOjB6OECxNFc>
HD-LM2 M3HFV2Fxd3C2b4Ppd{BCe3OjeR?= NUXIRZp6OC5zL{CuOU8yKM7:TR?= MYe0PEBp MlTwSG1UVw>? MVnpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M1TJZVIxQDhyMUC3
L428 MYXBdI9xfG:|aYOgRZN{[Xl? M17hVFAvOS9yLkWvNUDPxE1? MVe0PEBp M3PXcWROW09? M1rHRolv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= NEnGeoczODh6MEGwOy=>
KM-H2 MkDSRZBweHSxc3nzJGF{e2G7 MkL5NE4yNzBwNT:xJO69VQ>? Mnv3OFghcA>? M{[2dGROW09? MV7pcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MYeyNFg5ODFyNx?=
HD-LM2 M1HSZmZ2dmO2aX;uJGF{e2G7 Mly2NeKh|ryP NXfsfGE5OjRxNEigbC=> M3WwcWROW09? NIqyNGtld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ MUmyNFg5ODFyNx?=
L428 M1nYOWZ2dmO2aX;uJGF{e2G7 M2W2cFHDqM7:TR?= M4\PbVI1NzR6IHi= Ml3HSG1UVw>? MUjkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz M1nQUFIxQDhyMUC3
KM-H2 M2XPcGZ2dmO2aX;uJGF{e2G7 NWLl[YxnOcLizszN M{DiT|I1NzR6IHi= MYnEUXNQ MkGw[I94dnKnZ4XsZZRmeyC[SVHQMEBi[3SrdnH0[YQh[2G|cHHz[ZMhQSCjbnSgNy=> NF7XU5AzODh6MEGwOy=>
HD-LM2 MlzkSpVv[3Srb36gRZN{[Xl? NITtdmgxNjVxMTFOwG0> NEftZlMzPC92ODDo NYXNXHE4TE2VTx?= MXr1dJJm\3WuYYTld{BVVkZvzsGg[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MU[yNFg5ODFyNx?=
L428 M{npWmZ2dmO2aX;uJGF{e2G7 NYDySGxyOC53L{Gg{txO NELaSpMzPC92ODDo NXLhemlHTE2VTx?= MoW5eZBz\We3bHH0[ZMhXE6ILd8xJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MlrWNlA5QDBzMEe=
KM-H2 MmXOSpVv[3Srb36gRZN{[Xl? MWKwMlUwOSEQvF2= NFX5cmwzPC92ODDo MkjMSG1UVw>? M4G4S5VxemWpdXzheIV{KFSQRj5OtUBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MkD3NlA5QDBzMEe=
HD-LM2 NIGzRoNHfW6ldHnvckBCe3OjeR?= MV2xxsDPxE1? NH;tbWMxNjJ3LUS4JIg> MXjEUXNQ MWfhZ5RqfmG2ZYOgUmYuc0J? MV[yNFg5ODFyNx?=
L428 MU\GeY5kfGmxbjDBd5NigQ>? NFPCc24yyqEQvF2= NEGzXoIxNjJ3LUS4JIg> NUTIOWlYTE2VTx?= MX3hZ5RqfmG2ZYOgUmYuc0J? MlX5NlA5QDBzMEe=
KM-H2 MVPGeY5kfGmxbjDBd5NigQ>? MkXCNeKh|ryP MVewMlI2NTR6IHi= MX3EUXNQ NGe5eY1i[3SrdnH0[ZMhVkZva1K= M1nwclIxQDhyMUC3
H526 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:4WW9wUUN3ME20PFAhdk1? M2DGeFIxPjh{NkSz
H146 NX6yOFJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHlVI1KSzVyPUO1JI5O M2Ltc|IxPjh{NkSz
H82 NGr4Z5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzXTWM2OD1{NUCgcm0> MVmyNFY5OjZ2Mx?=
DMS114 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTZ2MDDuUS=> MUmyNFY5OjZ2Mx?=
HeLa M4TIR2Z2dmO2aX;uJGF{e2G7 M3:2bFAvOy1zMDFOwG0> NUXCcXNFQCCq MmjNSG1UVw>? NVeyUIZUcW6lcnXhd4V{KGGlZYT5cIF1\WRiSEOgT|khMEh|S{nBZ{kh[XRiMUCg{txO NYnweWw6OjB3M{i4OFA>
HeLa NYjZ[XdnTnWwY4Tpc44hSXO|YYm= NHfP[VMxNjNvMUCg{txO MW[4JIg> MkPsSG1UVw>? NWTibZBVcW6lcnXhd4V{KGOjc4Dhd4UhOyCjbnSgO{Bi[3SrdnH0bY9vKGSxc3Wg[IVx\W6mZX70cJk> MnvrNlA2Ozh6NEC=
HeLa MVHGeY5kfGmxbjDBd5NigQ>? NUXxWYZGOTBizszNxsA> NVHFc3lDPi9zMj:yOEBp NXjHO|k5TE2VTx?= M2TpN4lv\HWlZYOgcYl1d3SrYzDhZ4N2dXWuYYTpc44h[W6mIHTlcIF6\WRicEKxJIV5eHKnc4Ppc44> MWqyNFU{QDh2MB?=
HeLa  MmqzSpVv[3Srb36gRZN{[Xl? M1TGVVExKM7:TdMg MWO3JIg> MVLEUXNQ NXrZZ3BW\Gm|coXweJMhdm:{bXHsJJNxcW6mbHWgZ4hm[2uyb3nueEBnfW6ldHnvci=> MYSyNFU{QDh2MB?=
PBMC  MlrMRZBweHSxc3nzJGF{e2G7 NXzsO2E1OC53L{KvN{DPxE1? MVOyOE81QCCq M3e0T4lv\HWlZYOgZZBweHSxc3nzJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MYGyNFQxPjl2Nx?=

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体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 細胞株: Human mammary epithelial cells (HMEC), human foreskin fibroblasts (MRHF) cells
  • 濃度: 0-60 μM
  • 反応時間: 72 hours
  • 実験の流れ: 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
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: Female CD-1 nude mice bearing H1437 tumors
  • 製剤: PBS acidified with 0.1 M HCl or PEG400/0.2 M HCl saline, 40:60
  • 投薬量: 80 mg/kg
  • 投与方法: Administered via p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 13 mg/mL (32.79 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% PEG400+0.5% Tween80+5% Propylene glycol
混合させたのち直ちに使用することを推奨します。
30mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 396.44
化学式

C23H20N6O

CAS No. 726169-73-9
保管
in solvent
別名 MG0103

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03565406 Recruiting Melanoma New York University School of Medicine April 25 2018 Phase 1
NCT02993991 Withdrawn 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
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
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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID