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 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFf4PJU1QCCq MorYTWM2OD1|LkC0JO69VQ>? NGLo[VEzPjN5OECzPC=>
BT549 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV2wW5I6PDhiaB?= NGXNOWRKSzVyPUSuN|gh|ryP MYqyOlM4QDB|OB?=
MCF7 NXm1fmpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLHOFghcA>? M1\pU2lEPTB;MD62O{DPxE1? M17TT|I3Ozd6MEO4
T47D M2\kPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2K5R|Q5KGh? MlHkTWM2OD1zLkG3JO69VQ>? Mk[3NlY{PzhyM{i=
MOLP8 M3P1PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoL6OFghcA>? NHq5RXJKSzVyPUCuOuKyKDBwMEVOwG0> MmLuNlYxQTF3MUi=
Panc1 M4X0[2Z2dmO2aX;uJGF{e2G7 NXnRfnNFOC53L{GvNk42KM7:TR?= MoLuOFghcA>? M4r3XGROW09? M4i3XpVxemWpdXzheIV{KG2rUj2yNFM> MmfDNlU5PzJ7NEG=
Panc1 MYnGeY5kfGmxbjDBd5NigQ>? MYqwMlUwOS9{LkWg{txO NEDrfmg1QCCq MWTEUXNQ MlHYdoVlfWOnczDlfJBz\XO|aX;uJI9nKFqHQkGgc44h[m:2aDDtVm5CKGGwZDDwdo91\WmwIHzleoVtyqB? NFWxXo0zPTh5Mkm0NS=>
Panc1 MoLqRZBweHSxc3nzJGF{e2G7 MmLpNeKh|ryP MlW2O|LDqGh? NUHhcGxLTE2VTx?= M3zYeZNmdnOrdHn6[ZMhWGGwY{GgZ4VtdHNiZn;yJIdmdWOrdHHibY5mNWmwZIXj[YQh[XCxcITvd4l{ NIfvZ24zPTh5Mkm0NS=>
Panc1 M4K4OWNmdGxiVnnhZoltcXS7IFHzd4F6 MVexxsDPxE1? NHTRS|k4OsLiaB?= MlvmSG1UVw>? M{XoT4VvcGGwY3XzJIdmdWOrdHHibY5mNWmwZIXj[ZMh[2WubDD2bYFjcWyrdImg[IVkemWjc3W= NV3QVFFIOjV6N{K5OFE>
MMCs NWHLdWF2TnWwY4Tpc44hSXO|YYm= M2\Lb|Eh|ryv NW\3bXd7OC12ODDo NF3UfpFqdmO{ZXHz[ZMhVlCUQTDwdo91\WmwIHX4dJJme3Orb39CpFIvP+LCk{OuOUBnd2ym M4LFdlI1PDVzM{e4
MMCs MnG1SpVv[3Srb36gRZN{[Xl? M2G4T|AvPS9zIN88US=> MlHaNlQhcA>? NHjSPYV{cG:5czC0OU1nd2ymIIP0bY12dGG2aX;uJIlvKGOJTWCgcIV3\Wy| NXHHUWV7OjR2NUGzO|g>
MMCs NYTJR486TnWwY4Tpc44hSXO|YYm= M1\PZVHDqM7:TR?= NHnMSXAzPCCq NHfuXFdqdmO{ZXHz[ZMhUEGWIHHjeIl3cXS7 MljtNlQ1PTF|N{i=
MMCs MnPkSpVv[3Srb36gRZN{[Xl? MYCxxsDPxE1? MUKyOEBp NXvvRZB1[XWpbXXueJMh\2yxYnHsJIFk\XS7bHH0bY9vKGyndnXsd{Bw\iCqaYP0c45mKEh|LVu5M|E1KCiKMz3LPU8yPGGlKTDhcoQhUDRvS{GyJEhJPC2NMULhZ{k> MlTNNlQ1PTF|N{i=
MMCs MY\GeY5kfGmxbjDBd5NigQ>? Mn7XNeKh|ryP NXPLfHd[Pi1{NDDo NWHId2Rq\G:|ZT3k[ZBmdmSnboTsfUBqdmirYnn0d{B1cGVidILpcYV1cHmuYYTpc44hdGW4ZXygc4YhUDNvS{mgLGg{NUt7bXWzLS=> NU\UXI85OjR2NUGzO|g>
BxPC-3 NHrDNnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\nfZNGSzVyPUGuNUDPxE1? M2fTRlIyOzd3Nke5
AsPC-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLWSWM2OD1|Lkmg{txO MXmyNVM4PTZ5OR?=
MiaPaca-2 MkHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnFR|UxRTBwNjFOwG0> M33CNVIyOzd3Nke5
Panc-1 NXSzR5ljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWW0UFkxTUN3ME2xMlgh|ryP NUXYeINnOjF|N{W2O|k>
PAXF 546L† MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LsbWVEPTB;MT61JO69VQ>? M173NlIyOzd3Nke5
PAXF 1657L† M1TjRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\lS2VEPTB;MD6zJO69VQ>? MY[yNVM4PTZ5OR?=
HCT15 NH6xR4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjC[WlNUUN3ME2wMlch|ryP MnzENlE{OTd2NUW=
HT-29 NFTMSppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTBwNzFOwG0> NGH5RYwzOTNzN{S1OS=>
SW48 NYfSSJI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwODFOwG0> MYKyNVMyPzR3NR?=
SW620 MoPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\IbIlYUUN3ME2xJO69VQ>? MYOyNVMyPzR3NR?=
HMEC MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTF7IN88US=> M1PiZVIyOzF5NEW1
ANBL6  M2e2XGZ2dmO2aX;uJGF{e2G7 NVHDPXprOcLizszN M{WyVVI1KGh? MXvlcohidmOnczC1MWFENWmwZIXj[YQhVUGJRT3BN{Bo\W6nIHX4dJJme3Orb36= M4DUNVIyOTdzOEKx
LP1 NXjZ[XpVTnWwY4Tpc44hSXO|YYm= M2m1VlHDqM7:TR?= NXrx[3M6OjRiaB?= M3XsboVvcGGwY3XzJFUuSUNvaX7keYNm\CCPQVfFMWE{KGenbnWg[ZhxemW|c3nvci=> MV[yNVE4OTh{MR?=
HD-LM2 NVjaU5Z5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\me5RRPzMEoHi= NYLSfI82TE2VTx?= MVXJR|UxRTFwOEig{txO MX6yNFg5ODFyNx?=
L428 M2PBV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjlO|LDqGh? M{K0bGROW09? MXnJR|UxRTFwOU[g{txO NIT2e|YzODh6MEGwOy=>
KM-H2 M2HvXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\lW|czyqCq M{LiWGROW09? M1[zcmlEPTB;Mj64OkDPxE1? Mn;aNlA5QDBzMEe=
HD-LM2 M3ribWZ2dmO2aX;uJGF{e2G7 MVywMlEuOiEQvF2= NIfpfWozPCCqwrC= NYjnR|B3TE2VTx?= MXPzbI94eyCjY3X0fYxifGmxbjDv[kBpcXO2b37lJFMh[W6mIIXwdoVofWyjdHnvckBw\iC2aHWgZ4VtdCCleXPs[UBz\We3bHH0c5J6KHC{b4TlbY4heDJz M4S0ZlIxQDhyMUC3
L428 Ml;rSpVv[3Srb36gRZN{[Xl? NGO0XVYxNjFvMjFOwG0> MX2yOEBpyqB? NX3GdY84TE2VTx?= NYXvNZg3e2ixd4OgZYNmfHmuYYTpc44hd2ZiaHnzeI9v\SB|IHHu[EB2eHKnZ4XsZZRqd25ib3[geIhmKGOnbHygZ5lkdGVicnXneYxifG:{eTDwdo91\WmwIICyNS=> MmLlNlA5QDBzMEe=
KM-H2 MlHySpVv[3Srb36gRZN{[Xl? Mk\PNE4yNTJizszN M4P1d|I1KGkEoB?= MYnEUXNQ NIe2UJN{cG:5czDhZ4V1gWyjdHnvckBw\iCqaYP0c45mKDNiYX7kJJVxemWpdXzheIlwdiCxZjD0bIUh[2WubDDjfYNt\SC{ZXf1cIF1d3K7IIDyc5RmcW5icEKx MnfVNlA5QDBzMEe=
HD-LM2 NYTBTWpmSXCxcITvd4l{KEG|c3H5 MVywMlEwOC53L{Gg{txO MlHlOFghcA>? M13MNmROW09? MmfGbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MlTxNlA5QDBzMEe=
L428 MnfFRZBweHSxc3nzJGF{e2G7 M3fwW|AvOS9yLkWvNUDPxE1? M1PWfFQ5KGh? NWDFRXZMTE2VTx?= MVjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M2\KUlIxQDhyMUC3
KM-H2 MUnBdI9xfG:|aYOgRZN{[Xl? Mn\uNE4yNzBwNT:xJO69VQ>? NV;QbZBDPDhiaB?= NX;xWJhITE2VTx?= NGnHO3NqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M{LxU|IxQDhyMUC3
HD-LM2 MljSSpVv[3Srb36gRZN{[Xl? NULkcXNIOcLizszN NFqyWHAzPC92ODDo NI\QVpRFVVOR NHPEOJNld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ NFXNO4szODh6MEGwOy=>
L428 NYnsNWpRTnWwY4Tpc44hSXO|YYm= M{f1c|HDqM7:TR?= M1\VOVI1NzR6IHi= NFmyO4dFVVOR MVXkc5dvemWpdXzheIV{KFiLQWCsJIFkfGm4YYTl[EBk[XOyYYPld{A6KGGwZDCz M2TQXlIxQDhyMUC3
KM-H2 NEnRRlNHfW6ldHnvckBCe3OjeR?= M1W2TlHDqM7:TR?= MWSyOE81QCCq NH34SW1FVVOR NF\JepJld3ewcnXneYxifGW|IGjJRXAtKGGldHn2ZZRm\CClYYPwZZNmeyB7IHHu[EA{ NIC2eXQzODh6MEGwOy=>
HD-LM2 NF:zZVRHfW6ldHnvckBCe3OjeR?= NX2z[ZZ6OC53L{Gg{txO MlK3NlQwPDhiaB?= NH3KXZVFVVOR NUTVUmJifXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MkXLNlA5QDBzMEe=
L428 M{TGNmZ2dmO2aX;uJGF{e2G7 MYCwMlUwOSEQvF2= M4TGOVI1NzR6IHi= M2S4dGROW09? NYPQZppsfXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NWHWUol3OjB6OECxNFc>
KM-H2 MX;GeY5kfGmxbjDBd5NigQ>? NGPYTmIxNjVxMTFOwG0> NUPhfo05OjRxNEigbC=> NVm0dZZMTE2VTx?= NVnKUpJHfXC{ZXf1cIF1\XNiVF7GMe6yKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MVyyNFg5ODFyNx?=
HD-LM2 NWfMb3hqTnWwY4Tpc44hSXO|YYm= NUf0PGJ2OcLizszN M3XhPFAvOjVvNEigbC=> M2rQSmROW09? Mnj4ZYN1cX[jdHXzJG5HNWuE MXKyNFg5ODFyNx?=
L428 M1PVbWZ2dmO2aX;uJGF{e2G7 MVKxxsDPxE1? NELyOJAxNjJ3LUS4JIg> NGfTbXZFVVOR NXft[Y9q[WO2aY\heIV{KE6ILXvC M{nmSVIxQDhyMUC3
KM-H2 NGXK[45HfW6ldHnvckBCe3OjeR?= Ml[yNeKh|ryP NH\KVYExNjJ3LUS4JIg> MVXEUXNQ NXqwdmFS[WO2aY\heIV{KE6ILXvC NULXfVF1OjB6OECxNFc>
H526 NYDCZZB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vsR2lEPTB;NEiwJI5O MVmyNFY5OjZ2Mx?=
H146 NFSwd3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jub2lEPTB;M{Wgcm0> NXXIVWhiOjB4OEK2OFM>
H82 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorwTWM2OD1{NUCgcm0> NIDrU24zODZ6Mk[0Ny=>
DMS114 MnHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\zTWM2OD14NECgcm0> NWHSXnFiOjB4OEK2OFM>
HeLa MYfGeY5kfGmxbjDBd5NigQ>? NX7zWYVrOC5|LUGwJO69VQ>? NIPXcYs5KGh? M1KzTmROW09? NV\jdVlqcW6lcnXhd4V{KGGlZYT5cIF1\WRiSEOgT|khMEh|S{nBZ{kh[XRiMUCg{txO Mki0NlA2Ozh6NEC=
HeLa NXXUXGw6TnWwY4Tpc44hSXO|YYm= Mm\KNE4{NTFyIN88US=> MmLzPEBp MXrEUXNQ NIP0dI9qdmO{ZXHz[ZMh[2G|cHHz[UA{KGGwZDC3JIFkfGm4YYTpc44h\G:|ZTDk[ZBmdmSnboTsfS=> M3P1SlIxPTN6OESw
HeLa MX3GeY5kfGmxbjDBd5NigQ>? M3vtUFExKM7:TdMg M{S1elYwOTJxMkSgbC=> M3;kc2ROW09? M3zRd4lv\HWlZYOgcYl1d3SrYzDhZ4N2dXWuYYTpc44h[W6mIHTlcIF6\WRicEKxJIV5eHKnc4Ppc44> NVfUU29zOjB3M{i4OFA>
HeLa  NX3kU5ZlTnWwY4Tpc44hSXO|YYm= NIiyOo8yOCEQvF5CpC=> MX63JIg> M4\kZ2ROW09? M2r5[YRqe3K3cITzJI5wem2jbDDzdIlv\GynIHPo[YNseG:rboSg[pVv[3Srb36= NXn6ZYh2OjB3M{i4OFA>
PBMC  NGLZXWRCeG:ydH;zbZMhSXO|YYm= NVPiSI9MOC53L{KvN{DPxE1? NFvSO5MzPC92ODDo NVjYeJFFcW6mdXPld{BieG:ydH;zbZMh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MYWyNFQxPjl2Nx?=

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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
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
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
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

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