Decitabine 化学構造
分子量: 228.21

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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 NG\Ne4JHfW6ldHnvckBCe3OjeR?= MljXNE42yqEQvF2= Ml3wNlQhcA>? M{HVepdifGW{ MWjtc4R2dGG2ZYOgeIhmKGenbnWg[ZhxemW|c3nvckBw\iCPQVfFMWEhdWWvYnXydy=> MmfKNlUyOjNyOEK=
Eca109 M1jSS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSwMlUwOi53L{Wg{txO NYHMdHlJOjRxNEivO|IhcA>? NVPxW4VCf2G2ZYK= NEf2emlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NIjUUWkzPTF{M{C4Ni=>
Eca109 NV7PdHpiTnWwY4Tpc44hSXO|YYm= M4joW|AvPcLizszN MoTjOk8yOi9{NDDo NHuxfWx4[XSnch?= MYXpcohq[mm2czDj[YxtKG2rZ4LheIlwdsLi M2n5XVI2OTJ|MEiy
Eca109 M4f3WWZ2dmO2aX;uJGF{e2G7 MoXQNE42yqEQvF2= M1vod|I1KGh? M3G1TZdifGW{ NUT0[mxQcW6qaXLpeJMh[2WubDDpcpZie2mxbh?= NHHoTYszPTF{M{C4Ni=>
Eca109 NXrFfJJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTZNE42yqEQvF2= MV[yOEBp MVr3ZZRmeg>? NVTKdmxPcW6mdXPld{BIOi:PIHHydoV{fCCrbjD0bIUh[2WubDDjfYNt\Q>? Ml\3NlUyOjNyOEK=
Eca109 M4iwc2Z2dmO2aX;uJGF{e2G7 MoLBNE42NzFizszN MmjhNlQhcA>? M17WeJdifGW{ MWjk[YNz\WG|ZYOg[ZhxemW|c3nvckBw\iCQRj5OvmIzKGGwZDDNUXAz M3uzflI2OTJ|MEiy
SW1116  MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYiwMlUwOS9{L{Wg{txO MnTBOFghcA>? NVm0eIw{TE2VTx?= MkHB[Y5p[W6lZYOgeIhmKEenZnn0bY5q[iCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> MXKyOFg4PDJ6Nh?=
LOVO M2PYS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zYelAvPS9zL{KvOUDPxE1? M3vz[VQ5KGh? MVrEUXNQ MYnlcohidmOnczD0bIUhT2WoaYTpcoljKGmwZIXj[YQh[2WubDDpcohq[mm2aX;u MVyyOFg4PDJ6Nh?=
SW1116  M37SbGZ2dmO2aX;uJGF{e2G7 NGDOUmkyOCEQvF2= MYK0PEBp NID6NGFFVVOR M13idYlv[3KnYYPld{B1cGViZX\m[YN1cX[nIHH0JIlvcGmkaYTpcochSUuWIHHu[EBuXE:UIIPp[45idGmwZzDwZZRpf2G7czDjc41jcW6nZDD3bZRpKGenZnn0bY5q[g>? NX;Z[nVNOjR6N{SyPFY>
LOVO M4KwRmZ2dmO2aX;uJGF{e2G7 Mn7vNVAh|ryP MnvzOFghcA>? MVXEUXNQ M2TYbIlv[3KnYYPld{B1cGViZX\m[YN1cX[nIHH0JIlvcGmkaYTpcochSUuWIHHu[EBuXE:UIIPp[45idGmwZzDwZZRpf2G7czDjc41jcW6nZDD3bZRpKGenZnn0bY5q[g>? M1H4eVI1QDd2Mki2
SW1116  MVHBdI9xfG:|aYOgRZN{[Xl? MoDJNVAh|ryP NHLY[VQ1QCCq M4nve2ROW09? NFXaTG5mdmijbnPld{BI\W[rdHnubYIucW6mdXPl[EBieG:ydH;zbZM> MoWwNlQ5PzR{OE[=
LOVO M1nRZmFxd3C2b4Ppd{BCe3OjeR?= M4\pcFExKM7:TR?= NGfaWVM1QCCq NWTOcVBsTE2VTx?= M4LDT4VvcGGwY3XzJGdm\mm2aX7pZk1qdmS3Y3XkJIFxd3C2b4Ppdy=> NIPkXXUzPDh5NEK4Oi=>
RPMI-8226 Mn3PRZBweHSxc3nzJGF{e2G7 MlrtNU8zKM7:TR?= M3:zUlQ5Nzd{L{m2JIg> M4jFbWROW09? NUTXT3lncW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MVuyOFg{OzFyOB?=
OPM-2  MoDiRZBweHSxc3nzJGF{e2G7 NELGO3AyNzJizszN MnrSO|IwQTZxMUKwJIg> MYTEUXNQ NXGwZmllcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NIT2dZIzPDh|M{GwPC=>
JJN3  MUHBdI9xfG:|aYOgRZN{[Xl? M2PYOFAvPS9zIN88US=> NVzRTG5SOjRxNEigbC=> MmqwSG1UVw>? M4izNolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NH20dnUzPDh|M{GwPC=>
NCI-H929  MUXBdI9xfG:|aYOgRZN{[Xl? NV;6epZOOS9{IN88US=> MlWyO|IwQTZxMUKwJIg> MXLEUXNQ MX\pcoR2[2W|IHPlcIwh[XCxcITvd4l{ M2XK[|I1QDN|MUC4
RPMI-8226 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn2NU8zKM7:TR?= MnTsNlQwPDhxN{KgbC=> M3TLOGROW09? MUHh[oZm[3S|IHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44hdmWpYYTpeoVtgQ>? NYTLWIV1OjR6M{OxNFg>
OPM-2  MnvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmToNU8zKM7:TR?= M1X0UlI1NzR6L{eyJIg> MYLEUXNQ M4f0TYFn\mWldIOgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCwZXfheIl3\Wy7 MmG5NlQ5OzNzMEi=
JJN3  MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfK[3lLOC53L{Gg{txO Mmf6NlQwPDhxN{KgbC=> NVXRWnZZTE2VTx?= NF:1UGdi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= NFTpRZQzPDh|M{GwPC=>
NCI-H929  MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPsNU8zKM7:TR?= Mn3jNlQwPDhxN{KgbC=> M4jxPWROW09? MYjh[oZm[3S|IHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44hdmWpYYTpeoVtgQ>? MVGyOFg{OzFyOB?=
HeLa NFO0SZBMcW6jc3WgRZN{[Xl? NXvuPYg4U2l;MUCwNQKBmzVyMECg{txOKG[xcjDoSW5VOQ>? NGHyNJEzPDd6MEC5PC=>
HeLa MUDLbY5ie2ViQYPzZZk> MkD4T4k:PS54INMxJFAvPSEQvF2g[o9zKGiHTmSy MmfMNlQ4QDByOUi=
HeLa M16wcWtqdmG|ZTDBd5NigQ>? NU\xR2t4U2l;MkGuOkDDuSB|LkCg{txOKG[xcjDoR25VOQ>? NEjl[ZUzPDd6MEC5PC=>
HeLa NWjNcoZQU2mwYYPlJGF{e2G7 M3zwRWtqRTF2LkSgxtEhPC54IN88UUBnd3JiaFPOWFM> NWXBfJdyOjR5OECwPVg>
NB4 MmjlSpVv[3Srb36gRZN{[Xl? NV3POodGOi53L{WvO{42NzFyIN88US=> MofXNlQhcA>? MYTEUXNQ NGDMb2hqdmO{ZXHz[YEhfGinIHX4dJJme3Orb36gc4YheHKnY4Xyd49zKG2rUj2xNlVi NVrwblZROjR2OES4O|A>
CD4+ CD25− T  M17ZUWZ2dmO2aX;uJGF{e2G7 MX:xM|Uh|ryP M{HyfJJm\HWlZWOg[4xw[mGuIFTORUBu\XSqeXzheIlwdg>? MYeyOFQ4PjN4MB?=
BV-173 NIHS[5NCeG:ydH;zbZMhSXO|YYm= MXiwMlI2NzBwNT:wMlc2NzFizszN M1\WfVQ5Nzd{L{m2JIg> M2ftSeKhWEKV M{fabYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> NX;jcnNjOjR2MkO2NVM>
ML-1 NV[5VpExSXCxcITvd4l{KEG|c3H5 MWqwMlI2NzBwNT:wMlc2NzFizszN NXHmbWkyPDhxN{KvPVYhcA>? NFiwZW7DqFCEUx?= NXHtToMxcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NU\WZY4xOjR2MkO2NVM>
HL-60 NUOzbIZrSXCxcITvd4l{KEG|c3H5 NVLPcnE{OC5{NT:wMlUwOC55NT:xJO69VQ>? NGfVNVI1QC95Mj:5OkBp NX7pTnp2yqCSQmO= MnvCbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NWHGXVFMOjR2MkO2NVM>
KG-1a NIjIcFdCeG:ydH;zbZMhSXO|YYm= MVewMlI2NzBwNT:wMlc2NzFizszN M2TXclQ5Nzd{L{m2JIg> Mln6xsBRSlN? MUnpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= M3T0bFI1PDJ|NkGz
BV-173 NFrPcZhHfW6ldHnvckBCe3OjeR?= NGTlWoszPTBxNUCwcm0> MWC0PEBp M1LIWeKhWEKV M1XXeolv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= NHvvOXUzPDR{M{[xNy=>
CEM NGHoOFNHfW6ldHnvckBCe3OjeR?= MV6yOVAwPTBybl2= NHvXfmk1QCCq MoL3xsBRSlN? NX7lSHd3cW6mdXPld{Bl\WyjeXXkJIFv\CC|dYP0ZYlv\WRiUl;TJIlv[3KnYYPl M3;yS|I1PDJ|NkGz
HL-60 M1;TdmZ2dmO2aX;uJGF{e2G7 MYCyOVAwPTBybl2= NYrnT|NsPDhiaB?= MXJCpHBDWw>? NYqyVGZjcW6mdXPld{Bl\WyjeXXkJIFv\CC|dYP0ZYlv\WRiUl;TJIlv[3KnYYPl MofXNlQ1OjN4MUO=
ML-1 M33rTWZ2dmO2aX;uJGF{e2G7 M3nBOVI2OC93MEDuUS=> NHTtcnk1QCCq NIKzWIbDqFCEUx?= NUPXdolrcW6mdXPld{Bl\WyjeXXkJIFv\CC|dYP0ZYlv\WRiUl;TJIlv[3KnYYPl NWL1UmdoOjR2MkO2NVM>
DLD-1 M3jOfGZ2dmO2aX;uJGF{e2G7 NWHGZnJYOjVyL{WwNI5O M1fPVlQ5KGh? NUXiXVVbyqCSQmO= NVfMdZBS\G9ibn;0JIlv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= MYKyOFQzOzZzMx?=
HCT-116 MWLGeY5kfGmxbjDBd5NigQ>? M3npVFI2OC93MEDuUS=> M3ThVVQ5KGh? NXHXeIZjyqCSQmO= MYfkc{Bvd3RiaX7keYNmeyCmZXzhfYVlKGGwZDDzeZN1[WmwZXSgVm9UKGmwY4LlZZNm NYfze2lxOjR2MkO2NVM>
U937-A/E-9/14/18  Mn;kRZBweHSxc3nzJGF{e2G7 MVuwMlAyNzBwMT:xM|ExKM7:TR?= MVS0PEBp NGnRdVdqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M2LWOlI1OzByNEW2
HT29 NGnOPG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnvdnEyPzJiaB?= NYDPNHdxUUN3ME2xOFAxyrFzN{mg{txO M2SxPFI1OTd{ME[x
SW48 NEHjbYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jLOFczKGh? M3rteGlEPTB;MUWuNuKyPi5{IN88US=> NETUVoQzPDF5MkC2NS=>
HCT116 MkflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC5ems4OiCq NXr4TmkzUUN3ME2xMlfDuTBwNDFOwG0> M1nBc|I1OTd{ME[x
HepG2 NHvuRXJHfW6ldHnvckBCe3OjeR?= NF;qe5cxNjVxMTFOwG0> Mm\xNlQhcA>? MWHEUXNQ M1HzXJVxNXKnZ4XsZZRm\CC2aHWgdoVt[XSrdnWgU2NVVjJibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:w M2PYfVI1OTR4OEe0
LS174T M1LqS2Z2dmO2aX;uJGF{e2G7 MUewMlUwOSEQvF2= NVfDUmNTOjRiaB?= MVHEUXNQ MkjvcIVi\CC2bzDhckBqdmO{ZXHz[UBw\iCRQ2TONkBt\X[nbIO= Mlz0NlQyPDZ6N{S=
HepG2 MnfyRZBweHSxc3nzJGF{e2G7 MlvSNU8yOC9zMECg{txO NUj4boo2PyCm Mo[4SG1UVw>? MkjBbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXuyOFE1Pjh5NB?=
LS174T MnriRZBweHSxc3nzJGF{e2G7 NVj1PVVROS9zMD:xNFAh|ryP NEj0Wno4KGR? NGTxbJJFVVOR NE\VXoFqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NVj4bW9TOjRzNE[4O|Q>
QBC-939 NXP0bHVpSXCxcITvd4l{KEG|c3H5 NUTpbZJFOS9zMD:xNFAh|ryP NUfVc2dJPyCm MnXVSG1UVw>? NHm3Z2dqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NHnVU3MzPDF2Nki3OC=>
U251 NETFOmZCeG:ydH;zbZMhSXO|YYm= NXXlSZFOOS9zMD:xNFAh|ryP M{X1Z|ch\A>? NETD[FZFVVOR M3nYcIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXPYOVZsOjRzNE[4O|Q>
HL-60 MkfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWL1TZp7OSEQvF2= NEDxZVE1QCCq NXe2OGt5cW6lcnXhd4V{KEd{LYDoZZNmKGOnbHyg[pJi[3Srb36= NWLoNZpkOjRyMECzNlQ>
MDA‑MB‑453 M4DzZmZ2dmO2aX;uJGF{e2G7 NVSzb|BSOC5{L{Gg{txO MYe3NkBp M1PwXINifXOnczDy[U1mgHC{ZYPzbY9vKG:oIHPsZZVlcW8EoEJCpC=> MVeyN|g1PDJ{OB?=
HCC1569 M4rDWWZ2dmO2aX;uJGF{e2G7 M2j2ZlAvOi9zIN88US=> NV;x[3l2PzJiaB?= MULjZZV{\XNicnWt[ZhxemW|c3nvckBw\iClbHH1[IlvyqBzwrC= MXSyN|g1PDJ{OB?=
BT‑474 NETMfXdHfW6ldHnvckBCe3OjeR?= NXXkOXVzOC5{L{Gg{txO NYr4e5l1PzJiaB?= MVvjZZV{\XNicnWt[ZhxemW|c3nvckBw\iClbHH1[IlvyqBzwrC= NFLaWYozOzh2NEKyPC=>
AGS MlHuRZBweHSxc3nzJGF{e2G7 MoewOU8yOC9{MD:1NEDPxE1? NHrZcGM1QMLiaNMg NW\tcFM3TE2VTx?= NVv4dFk2cW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6yqB? M3zsO|I{PTh{N{i0
A549 NF3XXVZCeG:ydH;zbZMhSXO|YYm= NEDoNm02NzFyL{KwM|UxKM7:TR?= MWm0POKhcMLi MoHaSG1UVw>? MUTpcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdIpCpC=> M3eyWVI{PTh{N{i0
AGS  MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y2cVUwOTBxMkCvOVAh|ryP NITmV4Q1QMLiaNMg NFHx[JJFVVOR M1LScolv\HWlZYOgS|IwVSCyaHHz[UBienKnc4VCpC=> NEn5W2szOzV6Mke4OC=>
Kasumi-1 Mm\sRZBweHSxc3nzJGF{e2G7 MWWwMlUh|ryP NVz5XpJMPDkEoHlCpC=> MnO3[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBkdy22cnXheIVlKHerdHigWIYuVlBvc3O= Moq2NlM1QTN|NEi=
OCI-AML3 MV;BdI9xfG:|aYOgRZN{[Xl? M{DLblIvPSEQvF2= NVLG[mt1PDkEoHlCpC=> NEPaWoRl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGOxLYTy[YF1\WRid3n0bEBV\i2QUD3zZy=> MY[yN|Q6OzN2OB?=
MV4-11 M1PzSGFxd3C2b4Ppd{BCe3OjeR?= MofINk42KM7:TR?= M3HWflQ5yqCqwrC= NV7nNVk{\GWlcnXhd4V{KHSqZTDj[YxtKH[rYXLpcIl1gSClbz30doVifGWmIIfpeIghXGZvTmCtd4M> NYnFPYtsOjN2OUOzOFg>
NK  NXm1eJV2S3m2b4TvfIl1gSCDc4PhfS=> M2W4eFAvODJvMkCg{txO NWX1dWhwPSCm M3jtUIRm[3KnYYPld{B1cGViY4n0c4x6fGmlIHHjeIl3cXS7IH;mJG5MKGOnbHzzJIF1KGmwdHXycYVlcWG2ZTDjc45k\W62cnH0bY9veyC{ZYP1cJRqdmdiaX6gZUBWNXOqYYDl[EBld3On4pETdoV{eG:wc3WgZ5VzfmV? NUfINGlzOjN|MkiwPFg>
NK  NGXoflhCeG:ydH;zbZMhSXO|YYm= MViwMlAzNTJyIN88US=> M{DvRVUh\A>? MoDG[IVkemWjc3WgUmsh[2WubDDwdo9tcW[ncnH0bY9vKGGwZDD2bYFjcWyrdImgZZMhfGinIHPvcoNmdnS{YYTpc44hcW6lcnXhd4Vl M{T4[|I{OzJ6MEi4
NK  NHvrVYdHfW6ldHnvckBCe3OjeR?= MYewMlAyNTJyIN88US=> M{Hvc|Uh\A>? NFvxU4pk[XW|ZYOgbJlxd22ndHj5cIF1cW:wIH;mJG5MKGOnbHzzJIlvKGFiZH;z[gKBm3Knc4DvcpNm MnH3NlM{OjhyOEi=
MOLT4/DNR NVzGbW5HTnWwY4Tpc44hSXO|YYm= NGPESpM2KM7:TR?= MVG0JIQ> NH\Y[5Zz\WS3Y3XzJGFDS0JzIH3SUmEh\XiycnXzd4lwdg>? M2PRUVI{ODZyNUew
Jurkat/DOX NXXOb5A5TnWwY4Tpc44hSXO|YYm= NGXwSVQ2KM7:TR?= Moj6OEBl M4j3R5Jm\HWlZYOgRWJESjFibWLORUBmgHC{ZYPzbY9v NIPJWVUzOzB4MEW3NC=>
MOLT4/DNR MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1S2OlUh|ryP MmPVOEBl NEHyNWZz\WS3Y3XzJJRp\SCLQ{WwxsB3[Wy3ZTDmc5Ih\GG3bn;yeYJq[2mwIIPlcpNqfGm4aYT5 MnPkNlMxPjB3N{C=
Jurkat/DOX NH3s[WVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fGXFUh|ryP NFzJe3I1KGR? M2LYc5Jm\HWlZYOgeIhmKEmFNUFCpJZidHWnIH\vdkBl[XWwb4L1ZolkcW5ic3Xud4l1cX[rdIm= NIftNnUzOzB4MEW3NC=>
ccRCC  NGe3VGZCeG:ydH;zbZMhSXO|YYm= NXPo[49jOC5yMT2xNO69VQ>? NHvCfoo4OiCq M4DyemROW09? MXLoZZMhdWmwaX3hcEBm\m[nY4Sgc44h[2WubDDwdo9tcW[ncnH0bY9v M4Drb|IzQDJ4NE[3
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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

文献中の引用 (6)

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Tags: Decitabineを買う | Decitabine供給者 | Decitabineを購入する | Decitabine費用 | Decitabine生産者 | オーダーDecitabine | Decitabine代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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