Decitabine 化学構造
分子量: 228.21

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Quality Control & MSDS

製品説明

  • Compare DNA Methyltransferase Inhibitors
    DNA Methyltransferase製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 デシタビンは、HL-60とKG1a細胞の438nMと4.38nMのIC50によるDNAメチル化の強力な阻害剤です。
ターゲット DNA methyltransferase (HL-60) DNA methyltransferase (KG1a)
IC50 100 ng/mL 1 ng/mL [1]
In vitro試験 Decitabine inhibits cell growth in a dose and time-dependent manner with IC50 of approximately 438 nM and 43.8 nM for 72 hours and 96 hours exposure in HL-60 and KG1a leukemic cells, respectively. [1] A recent study shows that Decitabine exhibits high anti-proliferative and pro-apoptotic activity against anaplastic large cell lymphoma (ALCL), and inhibits [3H]–thymidine uptake in KARPAS-299 cells with EC50 of 0.49 μM. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Eca109 NF62RYlHfW6ldHnvckBCe3OjeR?= MlrpNE42yqEQvF2= MYeyOEBp M3rWcpdifGW{ M2LBcI1w\HWuYYTld{B1cGViZ3Xu[UBmgHC{ZYPzbY9vKG:oIF3BS2UuSSCvZX3i[ZJ{ MWKyOVEzOzB6Mh?=
Eca109 M4XGPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjnNHo4OC53L{KuOU82KM7:TR?= M2j0NFI1NzR6L{eyJIg> MVP3ZZRmeg>? MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NYjzdpVOOjVzMkOwPFI>
Eca109 MUfGeY5kfGmxbjDBd5NigQ>? MVuwMlXDqM7:TR?= NIXVXmw3NzF{L{K0JIg> NF;MWW14[XSnch?= MmPFbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd28EoB?= NVq0SmM6OjVzMkOwPFI>
Eca109 M1fEWWZ2dmO2aX;uJGF{e2G7 NH62RXAxNjYEoN88US=> M{HZO|I1KGh? MV33ZZRmeg>? NHzR[INqdmirYnn0d{Bk\WyuIHnueoF{cW:w MWWyOVEzOzB6Mh?=
Eca109 NXjWcIVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWiwMlXDqM7:TR?= NV3mZVZwOjRiaB?= NETnbHN4[XSnch?= NHnQcHBqdmS3Y3XzJGczN01iYYLy[ZN1KGmwIITo[UBk\WyuIHP5Z4xm M3fye|I2OTJ|MEiy
Eca109 NGWwbmxHfW6ldHnvckBCe3OjeR?= MojaNE42NzFizszN MUiyOEBp MXn3ZZRmeg>? MnHo[IVkemWjc3XzJIV5eHKnc4Ppc44hd2ZiTl[t{tpDOiCjbnSgUW1ROg>? MVmyOVEzOzB6Mh?=
SW1116  M122WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnvNE42NzFxMj:1JO69VQ>? MXi0PEBp M4jTSmROW09? M3n0S4VvcGGwY3XzJJRp\SCJZX\peIlvcWJiaX7keYNm\CClZXzsJIlvcGmkaYTpc44> MVWyOFg4PDJ6Nh?=
LOVO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVqwMlUwOS9{L{Wg{txO MmPJOFghcA>? NVrIXlg5TE2VTx?= NFqzUm1mdmijbnPld{B1cGViR3XmbZRqdmmkIHnu[JVk\WRiY3XscEBqdmirYnn0bY9v NW\TWY9MOjR6N{SyPFY>
SW1116  M13UVWZ2dmO2aX;uJGF{e2G7 M{HURlExKM7:TR?= MXS0PEBp MXPEUXNQ MmjubY5kemWjc3XzJJRp\SCnZn\lZ5RqfmViYYSgbY5pcWKrdHnu[{BCU1RiYX7kJI1VV1Jic3nncoFtcW6pIIDheIh4[Xm|IHPvcYJqdmWmIIfpeIgh\2WoaYTpcolj Ml;MNlQ5PzR{OE[=
LOVO NVz1O3FkTnWwY4Tpc44hSXO|YYm= NUL1O41oOTBizszN MVW0PEBp MXPEUXNQ NHnZ[HBqdmO{ZXHz[ZMhfGinIHXm[oVkfGm4ZTDheEBqdmirYnn0bY5oKEGNVDDhcoQhdVSRUjDzbYdv[WyrbnegdIF1cHejeYOgZ49u[mmwZXSge4l1cCCpZX\peIlvcWJ? M2nXUlI1QDd2Mki2
SW1116  NVTzbHlUSXCxcITvd4l{KEG|c3H5 MWGxNEDPxE1? MlfiOFghcA>? MkXiSG1UVw>? MXzlcohidmOnczDH[YZqfGmwaXKtbY5lfWOnZDDhdI9xfG:|aYO= MXyyOFg4PDJ6Nh?=
LOVO MlPlRZBweHSxc3nzJGF{e2G7 MlLnNVAh|ryP NGDwVlA1QCCq NYnHVmdQTE2VTx?= M162TIVvcGGwY3XzJGdm\mm2aX7pZk1qdmS3Y3XkJIFxd3C2b4Ppdy=> M13FSlI1QDd2Mki2
RPMI-8226 M1XnWWFxd3C2b4Ppd{BCe3OjeR?= NWfRUJpzOS9{IN88US=> Mnr3OFgwPzJxOU[gbC=> M4XDT2ROW09? M2DMWIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NH;RdYYzPDh|M{GwPC=>
OPM-2  MWLBdI9xfG:|aYOgRZN{[Xl? NVT0[GxlOS9{IN88US=> MY[3Nk86Pi9zMkCgbC=> M330Z2ROW09? NXTOdGN[cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NX;ROppCOjR6M{OxNFg>
JJN3  M1vNUmFxd3C2b4Ppd{BCe3OjeR?= NX;uPWxxOC53L{Gg{txO NGPSToczPC92ODDo MoDMSG1UVw>? M2XnRYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NXHG[GM6OjR6M{OxNFg>
NCI-H929  MVPBdI9xfG:|aYOgRZN{[Xl? NUC5bmtEOS9{IN88US=> NEjhd4M4Oi97Nj:xNlAhcA>? M1K0R2ROW09? NWO4fnZncW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NGi4dJQzPDh|M{GwPC=>
RPMI-8226 M3[2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHhNU8zKM7:TR?= M2C4N|I1NzR6L{eyJIg> Mn[3SG1UVw>? NGjOTJFi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= NFnOR44zPDh|M{GwPC=>
OPM-2  MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TzVlEwOiEQvF2= NXTvU3I{OjRxNEivO|IhcA>? NIjvV2xFVVOR M{DRSIFn\mWldIOgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCwZXfheIl3\Wy7 Ml3wNlQ5OzNzMEi=
JJN3  NIXCfJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIX6bWoxNjVxMTFOwG0> MoXtNlQwPDhxN{KgbC=> NIH4VnBFVVOR NYXYXXd6[W[oZXP0d{Bk\WyuIHP5Z4xmKHC{b3fy[ZN{cW:wIH7l[4F1cX[nbIm= NHH4O20zPDh|M{GwPC=>
NCI-H929  NIT5[HpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETteY0yNzJizszN NEDTWVMzPC92OD:3NkBp MnGySG1UVw>? NFTWXoZi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= M1H3[FI1QDN|MUC4
HeLa NXfiNJpmU2mwYYPlJGF{e2G7 NXfXVpVPU2l;MUCwNQKBmzVyMECg{txOKG[xcjDoSW5VOQ>? MYGyOFc5ODB7OB?=
HeLa MoG3T4lv[XOnIFHzd4F6 M2fSOmtqRTVwNjFCtUAxNjVizszNJIZweiCqRV7UNi=> MkToNlQ4QDByOUi=
HeLa MmC1T4lv[XOnIFHzd4F6 M4nlXGtqRTJzLk[gxtEhOy5yIN88UUBnd3JiaFPOWFE> NIPvWVEzPDd6MEC5PC=>
HeLa NHXib29McW6jc3WgRZN{[Xl? NXHseWhbU2l;MUSuOEDDuSB2Lk[g{txOKG[xcjDoR25VOw>? M3zNUFI1PzhyMEm4
NB4 M2\lN2Z2dmO2aX;uJGF{e2G7 M2rWfFIvPS93L{euOU8yOCEQvF2= MWCyOEBp M2L3ZmROW09? Mn3nbY5kemWjc3XhJJRp\SCneIDy[ZN{cW:wIH;mJJBz\WO3coPvdkBucVJvMUK1ZS=> M2T2UVI1PDh2OEew
CD4+ CD25− T  MoTKSpVv[3Srb36gRZN{[Xl? MmPPNU82KM7:TR?= MV7y[YR2[2WVIHfsc4JidCCGTlGgcYV1cHmuYYTpc44> Mk\mNlQ1PzZ|NkC=
BV-173 NF\LWGRCeG:ydH;zbZMhSXO|YYm= NYrrUWZ5OC5{NT:wMlUwOC55NT:xJO69VQ>? NGiwR2Q1QC95Mj:5OkBp MXxCpHBDWw>? M1X2NYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> NFPqVVMzPDR{M{[xNy=>
ML-1 MWDBdI9xfG:|aYOgRZN{[Xl? MnL4NE4zPS9yLkWvNE44PS9zIN88US=> NHjJU3o1QC95Mj:5OkBp MkPaxsBRSlN? NFjrWVJqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIJwfGhiZH;z[U0h[W6mIITpcYUuKGSncHXu[IVvfCCvYX7u[ZI> MYWyOFQzOzZzMx?=
HL-60 MUjBdI9xfG:|aYOgRZN{[Xl? MlPLNE4zPS9yLkWvNE44PS9zIN88US=> NYLITo14PDhxN{KvPVYhcA>? MkXCxsBRSlN? NVj0N3cxcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NVLEWVJ3OjR2MkO2NVM>
KG-1a NETSOHNCeG:ydH;zbZMhSXO|YYm= M17s[VAvOjVxMD61M|AvPzVxMTFOwG0> M2PKZlQ5Nzd{L{m2JIg> M{nYeeKhWEKV NY\IR4hscW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NFnNRYszPDR{M{[xNy=>
BV-173 NXfx[IozTnWwY4Tpc44hSXO|YYm= MoDjNlUxNzVyMH7N NXXXVo0zPDhiaB?= MkLMxsBRSlN? NWn5XZNwcW6mdXPld{Bl\WyjeXXkJIFv\CC|dYP0ZYlv\WRiUl;TJIlv[3KnYYPl MUGyOFQzOzZzMx?=
CEM MnTOSpVv[3Srb36gRZN{[Xl? MkiwNlUxNzVyMH7N MkPUOFghcA>? M4myWuKhWEKV MU\pcoR2[2W|IHTlcIF6\WRiYX7kJJN2e3SjaX7l[EBTV1NiaX7jdoVie2V? NYjmOYM1OjR2MkO2NVM>
HL-60 MYfGeY5kfGmxbjDBd5NigQ>? MW[yOVAwPTBybl2= M2rM[FQ5KGh? M1LFXuKhWEKV MlW5bY5lfWOnczDk[YxigWWmIHHu[EB{fXO2YXnu[YQhWk:VIHnuZ5Jm[XOn M1TiSFI1PDJ|NkGz
ML-1 MnLYSpVv[3Srb36gRZN{[Xl? MVuyOVAwPTBybl2= MojTOFghcA>? Mn7NxsBRSlN? NIP1do9qdmS3Y3XzJIRmdGG7ZXSgZY5lKHO3c4ThbY5m\CCUT2OgbY5kemWjc3W= NUfzPWRKOjR2MkO2NVM>
DLD-1 M3rzV2Z2dmO2aX;uJGF{e2G7 NUK2NmtjOjVyL{WwNI5O M1jjO|Q5KGh? NVfMN4tDyqCSQmO= Mlny[I8hdm:2IHnu[JVk\XNiZHXsZZlm\CCjbnSgd5V{fGGrbnXkJHJQWyCrbnPy[YF{\Q>? MoXmNlQ1OjN4MUO=
HCT-116 Mn[2SpVv[3Srb36gRZN{[Xl? NGXpd5EzPTBxNUCwcm0> NXjLSHh6PDhiaB?= NVXlcnlryqCSQmO= M1\wVYRwKG6xdDDpcoR2[2W|IHTlcIF6\WRiYX7kJJN2e3SjaX7l[EBTV1NiaX7jdoVie2V? NGDOPWkzPDR{M{[xNy=>
U937-A/E-9/14/18  NX3FcmY4SXCxcITvd4l{KEG|c3H5 NV6z[nd5OC5yMT:wMlEwOS9zMDFOwG0> M2\G[|Q5KGh? NXrDVIxGcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NEftW|MzPDNyMES1Oi=>
HT29 NVjMbWhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVThdoN4PzJiaB?= M323dGlEPTB;MUSwNOKyOTd7IN88US=> M3HFTFI1OTd{ME[x
SW48 M{jNU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrvV45mPzJiaB?= NHvYXWFKSzVyPUG1MlLDuTZwMjFOwG0> NHGzXlUzPDF5MkC2NS=>
HCT116 NVnSUIVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVe3NkBp NWnQcWVDUUN3ME2xMlfDuTBwNDFOwG0> MYeyOFE4OjB4MR?=
HepG2 MoXRSpVv[3Srb36gRZN{[Xl? M1u0NVAvPS9zIN88US=> MUiyOEBp NXrZ[5RRTE2VTx?= M2myb5VxNXKnZ4XsZZRm\CC2aHWgdoVt[XSrdnWgU2NVVjJibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:w MVOyOFE1Pjh5NB?=
LS174T MoTQSpVv[3Srb36gRZN{[Xl? NGTJR3YxNjVxMTFOwG0> MofLNlQhcA>? NE\hUGZFVVOR NH74[2Rt\WGmIITvJIFvKGmwY4LlZZNmKG:oIF;DWG4zKGyndnXsdy=> MUmyOFE1Pjh5NB?=
HepG2 NXTVcXVsSXCxcITvd4l{KEG|c3H5 MVKxM|ExNzFyMDFOwG0> M17SUVch\A>? NHXie5lFVVOR MXnpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mn7oNlQyPDZ6N{S=
LS174T MnfmRZBweHSxc3nzJGF{e2G7 Ml\6NU8yOC9zMECg{txO NXnyPIsyPyCm M4XldGROW09? NIfkfpNqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MX2yOFE1Pjh5NB?=
QBC-939 NWDlPXBESXCxcITvd4l{KEG|c3H5 MonENU8yOC9zMECg{txO NUfTU|FTPyCm MVjEUXNQ NXrEdlVscW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NUfwZZlmOjRzNE[4O|Q>
U251 M3zzc2Fxd3C2b4Ppd{BCe3OjeR?= M1XvNlEwOTBxMUCwJO69VQ>? MUm3JIQ> MVLEUXNQ MVXpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUC3PGFZOjRzNE[4O|Q>
HL-60 NWHibng5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqxJO69VQ>? M4jIWFQ5KGh? MY\pcoNz\WG|ZYOgS|IueGijc3WgZ4VtdCCocnHjeIlwdg>? MWeyOFAxODN{NB?=
MDA‑MB‑453 MmXySpVv[3Srb36gRZN{[Xl? NFL2[o0xNjJxMTFOwG0> Ml7nO|IhcA>? NHfEVWxk[XW|ZYOgdoUu\XiycnXzd4lwdiCxZjDjcIF2\GmwwrCxxsA> NFjVfoozOzh2NEKyPC=>
HCC1569 NVr4OIR1TnWwY4Tpc44hSXO|YYm= MoDlNE4zNzFizszN M2\RelczKGh? MXTjZZV{\XNicnWt[ZhxemW|c3nvckBw\iClbHH1[IlvyqBzwrC= MXOyN|g1PDJ{OB?=
BT‑474 MV7GeY5kfGmxbjDBd5NigQ>? MnPsNE4zNzFizszN MmGwO|IhcA>? MX7jZZV{\XNicnWt[ZhxemW|c3nvckBw\iClbHH1[IlvyqBzwrC= MoK1NlM5PDR{Mki=
AGS M165VGFxd3C2b4Ppd{BCe3OjeR?= NWXZblQxPS9zMD:yNE82OCEQvF2= Mn7tOFjDqGkEoB?= NHvrN2JFVVOR M3r0[olvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0feKh NX\DO3FYOjN3OEK3PFQ>
A549 MV\BdI9xfG:|aYOgRZN{[Xl? MljTOU8yOC9{MD:1NEDPxE1? MV[0POKhcMLi MV\EUXNQ NVXQfYc4cW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6yqB? MWWyN|U5Ojd6NB?=
AGS  NFLrNo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[1M|ExNzJyL{WwJO69VQ>? NFLoXmE1QMLiaNMg NV25[YxpTE2VTx?= M1:2colv\HWlZYOgS|IwVSCyaHHz[UBienKnc4VCpC=> M3z3R|I{PTh{N{i0
Kasumi-1 MUfBdI9xfG:|aYOgRZN{[Xl? NWnKO4U3OC53IN88US=> M1TqUFQ5yqCqwrC= Mk\2[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBkdy22cnXheIVlKHerdHigWIYuVlBvc3O= MYWyN|Q6OzN2OB?=
OCI-AML3 M17ufGFxd3C2b4Ppd{BCe3OjeR?= MXOyMlUh|ryP Mor4OFjDqGkEoB?= M2jLOoRm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkh[29vdILlZZRm\CC5aYToJHRnNU6SLYPj NUPMfZpnOjN2OUOzOFg>
MV4-11 NVLNbI9[SXCxcITvd4l{KEG|c3H5 NHvVVpczNjVizszN MVu0POKhcMLi MUnk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JINwNXS{ZXH0[YQhf2m2aDDU[k1PWC2|Yx?= NUW1dJBZOjN2OUOzOFg>
NK  MmDWR5l1d3SxeHn0fUBCe3OjeR?= MXuwMlAzNTJyIN88US=> M4DsRlUh\A>? NHPUTGVl\WO{ZXHz[ZMhfGinIHP5eI9tgXSrYzDhZ5Rqfmm2eTDv[kBPUyClZXzsd{BifCCrboTldo1m\GmjdHWgZ49v[2WwdILheIlwdnNicnXzeYx1cW6pIHnuJIEhXS2|aHHw[YQh\G:|ZfMAl5Jme3CxboPlJIN2en[n MUiyN|MzQDB6OB?=
NK  MVTBdI9xfG:|aYOgRZN{[Xl? NXPxZmNmOC5yMj2yNEDPxE1? NH62[Iw2KGR? M{LtbIRm[3KnYYPlJG5MKGOnbHygdJJwdGmoZYLheIlwdiCjbnSgeoli[mmuaYT5JIF{KHSqZTDjc45k\W62cnH0bY9vKGmwY4LlZZNm\A>? NGDLeHczOzN{OEC4PC=>
NK  NX3mSYg6TnWwY4Tpc44hSXO|YYm= M4rrZVAvODFvMkCg{txO MnzMOUBl MYjjZZV{\XNiaInwc41mfGi7bHH0bY9vKG:oIF7LJINmdGy|IHnuJIEh\G:|ZfMAl5Jme3CxboPl MWiyN|MzQDB6OB?=
MOLT4/DNR MlHJSpVv[3Srb36gRZN{[Xl? NHn1bZk2KM7:TR?= NXThVGQ1PCCm NWj6O2pOemWmdXPld{BCSkOEMTDtVm5CKGW6cILld5Nqd25? NHr5S|MzOzB4MEW3NC=>
Jurkat/DOX NIL0eotHfW6ldHnvckBCe3OjeR?= MWi1JO69VQ>? NVm2b4tLPCCm NYTwRZZJemWmdXPld{BCSkOEMTDtVm5CKGW6cILld5Nqd25? M3rZWVI{ODZyNUew
MOLT4/DNR NU\jc2xlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnQR2V3PSEQvF2= M3jyNVQh\A>? NXjSd2ZJemWmdXPld{B1cGViSVO1NOKhfmGudXWg[o9zKGSjdX7vdpVjcWOrbjDz[Y5{cXSrdnn0fS=> MkfTNlMxPjB3N{C=
Jurkat/DOX M3P6bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrXZ2JuPSEQvF2= MVW0JIQ> M2Xx[ZJm\HWlZYOgeIhmKEmFNUFCpJZidHWnIH\vdkBl[XWwb4L1ZolkcW5ic3Xud4l1cX[rdIm= NIP4[mszOzB4MEW3NC=>
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... Click to View More Cell Line Experimental Data

In vivo試験 In a ALK+ KARPAS-299 murine xenograft model, Decitabine at a dose of 2.5 mg/kg causes increased apoptosis and reduced proliferation of tumor cells, and also results in demethylation of tumor suppressor p16INK4A. [2]
臨床試験 Decitabine is currently in Phase I clinical trials in patients with Higher-risk MDS and MDS/AML Receiving Allogeneic Stem Cell Transplantation.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

DNA synthesis assay The rate of DNA synthesis is measured by the incorporation of radioactive thymidine into DNA. HL-60 and KG1a cells are suspended in 2 mL RPMI medium containing 10% fetal serum in 6-well (35 mm diameter) dishes and incubated with different concentrations of corresponding drugs for 48 hours (drugs are added simultaneously). At 48 hours, 0.5 μCi [3H] thymidine (6.7 Ci/mmol) is added to each well and incubated for an additional 24 hours. The cells are placed on GF/C glass fiber filters (2.4 cm diameter), washed with cold 0.9% NaCl, 5% cold trichloroacetic acid and ethanol. The filters containing the DNA are then dried, placed in EcoLite scintillation liquid (ICN) and the radioactivity measured using Beckman LS 6000IC scintillation counter. The IC50 is defined as the concentration of drug that inhibits 50% of the DNA synthesis of the leukemic cell lines from the dose–response curve.

細胞アッセイ: [1]

細胞株 HL-60 and KG1a
濃度 0-500 nM
反応時間 96 hours
実験の流れ For the growth inhibition assay, cells in log phase are placed in 5 mL of medium. Different concentrations of Decitabine are added to the medium simultaneously. Cell counts are performed at the indicated times using a model ZM Coulter Counter. The concentration that produces 50% inhibition of growth (IC50) is determined from the growth curves of the drug treated leukemic cell lines.

動物実験: [2]

動物モデル KARPAS-299 human cells are inoculated subcutaneously into the right and left flanks of the mice.
製剤 Decitabine is dissolved in sterile PBS .
投薬量 ≤2.5 mg/kg
投与方法 Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Decitabine SDF
分子量 228.21
化学式

C8H12N4O4

CAS No. 2353-33-5
保管 2年-20℃
6月-80℃in solvent
別名 Deoxycytidine
溶解度 (25°C) * In vitro DMSO 45 mg/mL (197.18 mM)
10 mg/mL (43.81 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 4-amino-1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one

カスタマーフィードバック (3)


Click to enlarge
Rating
Source PLoS One, 2014, 9(5), e97719. Decitabine purchased from Selleck
Method Western blot
Cell Lines SW1116, LOVO cells
Concentrations 10 uM
Incubation Time 48 h
Results Decitabine (10 uM) could not lead to significant alterations in AKT, or mTOR activity, as assessed by Western blot for phosphorylation of AKT, mTOR and S6K. Additionally, it observed minimal reductions of phosphorylation of AKT, mTOR and S6K with 5 uM gefitinib in SW1116 and 4 礛 in LOVO cells. However, the combination of decitabine and gefitinib completely abrogated AKT and mTOR activities in SW1116 and LOVO cells.

Click to enlarge
Rating
Source PLoS One, 2014, 9(5), e97719. Decitabine purchased from Selleck
Method Annexin V-FITC/PI analysis
Cell Lines SW1116, LOVO cells
Concentrations 10 uM
Incubation Time 48 h
Results SW1116 and LOVO cells were treated with the two compounds, alone or in combination, for 48 h and then cell apoptosis was determined by Annexin V-FITC and propidium iodide (PI) staining and flow cytometry analysis. Treatment with gefitinib (2 uM) or decitabine (10 uM) alone had weak effects on apoptosis in SW1116 cells. However, there was a significantly higher apoptosis rate found upon treatment with the combination of gefitinib and decitabine.

Click to enlarge
Rating
Source Leuk Res, 2014, 38(3), 402-10. Decitabine purchased from Selleck
Method Bisulfite sequencing analysis
Cell Lines NB4 cells
Concentrations 10 uM
Incubation Time 24 h
Results Mature miR-125a expression increased with increasing amounts of decitabine treatment after 24 hours.

文献中の引用 (6)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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