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 NHjEUmJHfW6ldHnvckBCe3OjeR?= NUjrWIRVOC53wrFOwG0> NY\COYpPOjRiaB?= NFz6WIt4[XSnch?= NEO5dJZud2S3bHH0[ZMhfGinIHflcoUh\XiycnXzd4lwdiCxZjDNRWdGNUFibXXtZoVzew>? MWSyOVEzOzB6Mh?=
Eca109 NUT1cohsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\ENE42NzJwNT:1JO69VQ>? NYTMRmxlOjRxNEivO|IhcA>? MlLqe4F1\XJ? NWDIOYdlcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> MVOyOVEzOzB6Mh?=
Eca109 NEHjfIlHfW6ldHnvckBCe3OjeR?= MlnVNE42yqEQvF2= NGPMVWo3NzF{L{K0JIg> NXHOUYljf2G2ZYK= NIO4V|dqdmirYnn0d{Bk\WyuIH3p[5JifGmxbtMg MYqyOVEzOzB6Mh?=
Eca109 MoW5SpVv[3Srb36gRZN{[Xl? NYPlZZdOOC53wrFOwG0> MlmwNlQhcA>? NEHjV294[XSnch?= MYfpcohq[mm2czDj[YxtKGmwdnHzbY9v MUSyOVEzOzB6Mh?=
Eca109 NIrqXmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjaNE42yqEQvF2= NIDtWFYzPCCq Mo\Xe4F1\XJ? MWLpcoR2[2W|IFeyM20h[XK{ZYP0JIlvKHSqZTDj[YxtKGO7Y3zl Mn;XNlUyOjNyOEK=
Eca109 M1LxTGZ2dmO2aX;uJGF{e2G7 MlmzNE42NzFizszN MUOyOEBp MoDje4F1\XJ? Mly5[IVkemWjc3XzJIV5eHKnc4Ppc44hd2ZiTl[t{tpDOiCjbnSgUW1ROg>? MVSyOVEzOzB6Mh?=
SW1116  NHzC[HVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnlNE42NzFxMj:1JO69VQ>? MYO0PEBp M4jzdWROW09? M2DmNYVvcGGwY3XzJJRp\SCJZX\peIlvcWJiaX7keYNm\CClZXzsJIlvcGmkaYTpc44> M2LEZ|I1QDd2Mki2
LOVO M1rNWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGwMlUwOS9{L{Wg{txO NYCzTm4xPDhiaB?= MkDFSG1UVw>? M3O0coVvcGGwY3XzJJRp\SCJZX\peIlvcWJiaX7keYNm\CClZXzsJIlvcGmkaYTpc44> MUCyOFg4PDJ6Nh?=
SW1116  MnnhSpVv[3Srb36gRZN{[Xl? NX\zO3JZOTBizszN M2LKO|Q5KGh? NH;KTmlFVVOR NWe1[5dHcW6lcnXhd4V{KHSqZTDl[oZm[3SrdnWgZZQhcW6qaXLpeIlv\yCDS2SgZY5lKG2WT2Kgd4lodmGuaX7nJJBifGi5YYnzJINwdWKrbnXkJJdqfGhiZ3XmbZRqdmmk Ml\kNlQ5PzR{OE[=
LOVO NIni[5dHfW6ldHnvckBCe3OjeR?= NFzXTlYyOCEQvF2= NVSybHNnPDhiaB?= M2nh[mROW09? NGHQXnZqdmO{ZXHz[ZMhfGinIHXm[oVkfGm4ZTDheEBqdmirYnn0bY5oKEGNVDDhcoQhdVSRUjDzbYdv[WyrbnegdIF1cHejeYOgZ49u[mmwZXSge4l1cCCpZX\peIlvcWJ? MYWyOFg4PDJ6Nh?=
SW1116  NIDucFFCeG:ydH;zbZMhSXO|YYm= M3TDdFExKM7:TR?= NV3TVFBKPDhiaB?= M3T4Z2ROW09? MVnlcohidmOnczDH[YZqfGmwaXKtbY5lfWOnZDDhdI9xfG:|aYO= NEHaNFUzPDh5NEK4Oi=>
LOVO NFnRdoRCeG:ydH;zbZMhSXO|YYm= MW[xNEDPxE1? M13qclQ5KGh? NGHmbmpFVVOR NIfB[XZmdmijbnPld{BI\W[rdHnubYIucW6mdXPl[EBieG:ydH;zbZM> NVTYbmxtOjR6N{SyPFY>
RPMI-8226 NYS0d2VJSXCxcITvd4l{KEG|c3H5 NUfnRVdHOS9{IN88US=> MXu0PE84Oi97NjDo M2fJTWROW09? NUjPc3BpcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MmfVNlQ5OzNzMEi=
OPM-2  MUXBdI9xfG:|aYOgRZN{[Xl? M{DIV|EwOiEQvF2= M4\rVVczNzl4L{GyNEBp NF31WlhFVVOR MnrqbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NXKyeVdzOjR6M{OxNFg>
JJN3  M3LyUGFxd3C2b4Ppd{BCe3OjeR?= NGDhb3MxNjVxMTFOwG0> MlnONlQwPDhiaB?= MmXpSG1UVw>? Ml3KbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NF3C[IszPDh|M{GwPC=>
NCI-H929  MW\BdI9xfG:|aYOgRZN{[Xl? MXWxM|Ih|ryP NHHKU2Q4Oi97Nj:xNlAhcA>? MnXGSG1UVw>? MVHpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NE\LNm0zPDh|M{GwPC=>
RPMI-8226 NV3scYVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPqN|VGOS9{IN88US=> MlztNlQwPDhxN{KgbC=> NWr4VFBSTE2VTx?= NHPnbldi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= MYWyOFg{OzFyOB?=
OPM-2  NXjJUoNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofHNU8zKM7:TR?= MojvNlQwPDhxN{KgbC=> MUfEUXNQ NVz1[oY2[W[oZXP0d{Bk\WyuIHP5Z4xmKHC{b3fy[ZN{cW:wIH7l[4F1cX[nbIm= M4LhRlI1QDN|MUC4
JJN3  NX3SfVQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDKNE42NzFizszN MV2yOE81QC95MjDo NXnydGNrTE2VTx?= Mmm0ZYZn\WO2czDj[YxtKGO7Y3zlJJBzd2e{ZYPzbY9vKG6nZ3H0bZZmdHl? NX;iRlV{OjR6M{OxNFg>
NCI-H929  NWDXZ3dtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUWxM|Ih|ryP M1rzdFI1NzR6L{eyJIg> NFrXVpBFVVOR MYrh[oZm[3S|IHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44hdmWpYYTpeoVtgQ>? M13HVFI1QDN|MUC4
HeLa MV;LbY5ie2ViQYPzZZk> NEiyR|VMcT1zMECw5qCUPTByMDFOwG0h\m:{IHjFUnQy MorENlQ4QDByOUi=
HeLa NVjHUId5U2mwYYPlJGF{e2G7 MYnLbV02NjZiwsGgNE42KM7:TTDmc5IhcEWQVEK= MV2yOFc5ODB7OB?=
HeLa NVj2WnQzU2mwYYPlJGF{e2G7 M17lXmtqRTJzLk[gxtEhOy5yIN88UUBnd3JiaFPOWFE> NIXGN48zPDd6MEC5PC=>
HeLa NY[xcpRSU2mwYYPlJGF{e2G7 Mnn6T4k:OTRwNDFCtUA1NjZizszNJIZweiCqQ17UNy=> NUDNPZM{OjR5OECwPVg>
NB4 M2LOcGZ2dmO2aX;uJGF{e2G7 MUKyMlUwPS95LkWvNVAh|ryP NFLoSpozPCCq MoHOSG1UVw>? NXzyenV5cW6lcnXhd4ViKHSqZTDlfJBz\XO|aX;uJI9nKHC{ZXP1dpNweiCvaWKtNVI2[Q>? NXvPOmJJOjR2OES4O|A>
CD4+ CD25− T  NEe0eWdHfW6ldHnvckBCe3OjeR?= M4G3NVEwPSEQvF2= NF7ENpFz\WS3Y3XTJIdtd2KjbDDEUmEhdWW2aInsZZRqd25? Ml[zNlQ1PzZ|NkC=
BV-173 NIDV[VdCeG:ydH;zbZMhSXO|YYm= NFfSRXgxNjJ3L{CuOU8xNjd3L{Gg{txO NITnV4Y1QC95Mj:5OkBp NFHFWHPDqFCEUx?= M2HkfYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> NVvIRpVbOjR2MkO2NVM>
ML-1 NGn1ToZCeG:ydH;zbZMhSXO|YYm= MnvYNE4zPS9yLkWvNE44PS9zIN88US=> MXm0PE84Oi97NjDo NVn0S5RqyqCSQmO= Mn\EbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NHrje5YzPDR{M{[xNy=>
HL-60 NELvbppCeG:ydH;zbZMhSXO|YYm= M2PqdlAvOjVxMD61M|AvPzVxMTFOwG0> MYm0PE84Oi97NjDo NUS4WXc1yqCSQmO= M4WwdYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> NEKyXGEzPDR{M{[xNy=>
KG-1a MYTBdI9xfG:|aYOgRZN{[Xl? MYqwMlI2NzBwNT:wMlc2NzFizszN M{TlflQ5Nzd{L{m2JIg> M1LUSuKhWEKV MUfpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= MlrMNlQ1OjN4MUO=
BV-173 NIPid41HfW6ldHnvckBCe3OjeR?= MoLLNlUxNzVyMH7N MVS0PEBp MUdCpHBDWw>? M1fmTIlv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= MYOyOFQzOzZzMx?=
CEM MWDGeY5kfGmxbjDBd5NigQ>? MnjqNlUxNzVyMH7N M4\qT|Q5KGh? M{fvWuKhWEKV NES1eGZqdmS3Y3XzJIRmdGG7ZXSgZY5lKHO3c4ThbY5m\CCUT2OgbY5kemWjc3W= NX7ObWU5OjR2MkO2NVM>
HL-60 Mn7lSpVv[3Srb36gRZN{[Xl? MVSyOVAwPTBybl2= M2Kw[FQ5KGh? MojsxsBRSlN? MWHpcoR2[2W|IHTlcIF6\WRiYX7kJJN2e3SjaX7l[EBTV1NiaX7jdoVie2V? NFHFTowzPDR{M{[xNy=>
ML-1 NV\qSmczTnWwY4Tpc44hSXO|YYm= NXnJe4EyOjVyL{WwNI5O NEPVZZo1QCCq MoKzxsBRSlN? NIDFTYxqdmS3Y3XzJIRmdGG7ZXSgZY5lKHO3c4ThbY5m\CCUT2OgbY5kemWjc3W= NV;wTodNOjR2MkO2NVM>
DLD-1 MWnGeY5kfGmxbjDBd5NigQ>? MX[yOVAwPTBybl2= NWPnU2NzPDhiaB?= NH25e5XDqFCEUx?= NX[wWnlt\G9ibn;0JIlv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= M4rOVVI1PDJ|NkGz
HCT-116 M4iycWZ2dmO2aX;uJGF{e2G7 NUPNboFvOjVyL{WwNI5O NIfufGw1QCCq NHzSVJjDqFCEUx?= NEKweYxldyCwb4SgbY5lfWOnczDk[YxigWWmIHHu[EB{fXO2YXnu[YQhWk:VIHnuZ5Jm[XOn NFnMOJYzPDR{M{[xNy=>
U937-A/E-9/14/18  NXv5bZZkSXCxcITvd4l{KEG|c3H5 NHnIbogxNjBzL{CuNU8yNzFyIN88US=> MVS0PEBp M3KzSIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MmfENlQ{ODB2NU[=
HT29 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHYO|IhcA>? MWTJR|UxRTF2MEFCtVE4QSEQvF2= MnTFNlQyPzJyNkG=
SW48 Ml\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj3O|IhcA>? NVG3NXdOUUN3ME2xOU4zyrF4LkKg{txO MmPENlQyPzJyNkG=
HCT116 NUfjSYNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYK3NkBp M1jCXGlEPTB;MT63xtExNjRizszN MoP0NlQyPzJyNkG=
HepG2 M{nsV2Z2dmO2aX;uJGF{e2G7 NGDmb3oxNjVxMTFOwG0> NFG1ZpkzPCCq NVnCdm5UTE2VTx?= MoXueZAuemWpdXzheIVlKHSqZTDy[YxifGm4ZTDPR3RPOiCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? MUGyOFE1Pjh5NB?=
LS174T MknzSpVv[3Srb36gRZN{[Xl? NX3FcXVUOC53L{Gg{txO MX[yOEBp MljCSG1UVw>? NUS0Vm5CdGWjZDD0c{BidiCrbnPy[YF{\SCxZjDPR3RPOiCuZY\lcJM> MVWyOFE1Pjh5NB?=
HepG2 NXjjWmxzSXCxcITvd4l{KEG|c3H5 NVzaUGxIOS9zMD:xNFAh|ryP MVG3JIQ> MmPpSG1UVw>? NUHTWYxCcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NWDJfHZFOjRzNE[4O|Q>
LS174T M{j3ZWFxd3C2b4Ppd{BCe3OjeR?= MlfrNU8yOC9zMECg{txO NILrU5Y4KGR? M3zPPGROW09? MlTUbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3Xr[lI1OTR4OEe0
QBC-939 MlLjRZBweHSxc3nzJGF{e2G7 NHvuWnAyNzFyL{GwNEDPxE1? MYC3JIQ> NHzaVmtFVVOR NHraN5dqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M4WxelI1OTR4OEe0
U251 NEfNR3pCeG:ydH;zbZMhSXO|YYm= NHXmdVMyNzFyL{GwNEDPxE1? MYe3JIQ> NYG4TGpGTE2VTx?= NX62U2ZIcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MUSyOFE1Pjh5NB?=
HL-60 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjHR3AyKM7:TR?= NVrvTJk5PDhiaB?= M3HaSYlv[3KnYYPld{BIOi2yaHHz[UBk\WyuIH\yZYN1cW:w NVjpfVJnOjRyMECzNlQ>
MDA‑MB‑453 Mm\iSpVv[3Srb36gRZN{[Xl? MlPjNE4zNzFizszN MUC3NkBp MkTFZ4F2e2W|IILlMYV5eHKnc4Ppc44hd2ZiY3zheYRqdsLiMdMg MmXMNlM5PDR{Mki=
HCC1569 MXrGeY5kfGmxbjDBd5NigQ>? MV6wMlIwOSEQvF2= MkSzO|IhcA>? NF2yboJk[XW|ZYOgdoUu\XiycnXzd4lwdiCxZjDjcIF2\GmwwrCxxsA> NFvkXVIzOzh2NEKyPC=>
BT‑474 MlnuSpVv[3Srb36gRZN{[Xl? NUPpSot4OC5{L{Gg{txO Ml;0O|IhcA>? NID1[WNk[XW|ZYOgdoUu\XiycnXzd4lwdiCxZjDjcIF2\GmwwrCxxsA> MUKyN|g1PDJ{OB?=
AGS M3zVbmFxd3C2b4Ppd{BCe3OjeR?= MXS1M|ExNzJyL{WwJO69VQ>? NXu3W|FUPDkEoHlCpC=> M2WyZ2ROW09? NEHYRYhqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJnDqA>? M3fkc|I{PTh{N{i0
A549 NGnHb25CeG:ydH;zbZMhSXO|YYm= MmK1OU8yOC9{MD:1NEDPxE1? M3fZS|Q5yqCqwrC= NWnQWJl4TE2VTx?= M3T4fIlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0feKh M2fnWlI{PTh{N{i0
AGS  NFzMbVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;0OU8yOC9{MD:1NEDPxE1? MWS0POKhcMLi MWrEUXNQ M{DBOIlv\HWlZYOgS|IwVSCyaHHz[UBienKnc4VCpC=> NHrKVGczOzV6Mke4OC=>
Kasumi-1 M1Hq[mFxd3C2b4Ppd{BCe3OjeR?= MXywMlUh|ryP MoXkOFjDqGkEoB?= MUPk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JINwNXS{ZXH0[YQhf2m2aDDU[k1PWC2|Yx?= MWmyN|Q6OzN2OB?=
OCI-AML3 NGjtOnZCeG:ydH;zbZMhSXO|YYm= NVvnZY9lOi53IN88US=> NYPNXVVEPDkEoHlCpC=> Ml;m[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBkdy22cnXheIVlKHerdHigWIYuVlBvc3O= MlXXNlM1QTN|NEi=
MV4-11 MmK0RZBweHSxc3nzJGF{e2G7 NX;uepZJOi53IN88US=> NFrkb|c1QMLiaNMg NF[wPZZl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGOxLYTy[YF1\WRid3n0bEBV\i2QUD3zZy=> Mke1NlM1QTN|NEi=
NK  Mme1R5l1d3SxeHn0fUBCe3OjeR?= MnLrNE4xOi1{MDFOwG0> NHLN[JQ2KGR? NH7tfZZl\WO{ZXHz[ZMhfGinIHP5eI9tgXSrYzDhZ5Rqfmm2eTDv[kBPUyClZXzsd{BifCCrboTldo1m\GmjdHWgZ49v[2WwdILheIlwdnNicnXzeYx1cW6pIHnuJIEhXS2|aHHw[YQh\G:|ZfMAl5Jme3CxboPlJIN2en[n MUiyN|MzQDB6OB?=
NK  MVnBdI9xfG:|aYOgRZN{[Xl? NYTsO3dUOC5yMj2yNEDPxE1? MYe1JIQ> NH3US3Rl\WO{ZXHz[UBPUyClZXzsJJBzd2yrZnXyZZRqd25iYX7kJJZq[WKrbHn0fUBieyC2aHWgZ49v[2WwdILheIlwdiCrbnPy[YF{\WR? NUnBVFhwOjN|MkiwPFg>
NK  NWHDfVF7TnWwY4Tpc44hSXO|YYm= NX;SSXlUOC5yMT2yNEDPxE1? MVe1JIQ> M4T6SINifXOnczDofZBwdWW2aInsZZRqd25ib3[gUmsh[2WubIOgbY4h[SCmb4Pl5qCUemW|cH;ud4U> M2fKfFI{OzJ6MEi4
MOLT4/DNR NXTKN5ZmTnWwY4Tpc44hSXO|YYm= MYG1JO69VQ>? MoPOOEBl MmrmdoVlfWOnczDBRmNDOSCvUl7BJIV5eHKnc4Ppc44> NGDFOpQzOzB4MEW3NC=>
Jurkat/DOX M1SyemZ2dmO2aX;uJGF{e2G7 NF3Z[2g2KM7:TR?= MX60JIQ> NISwSlFz\WS3Y3XzJGFDS0JzIH3SUmEh\XiycnXzd4lwdg>? MV[yN|A3ODV5MB?=
MOLT4/DNR NYjRdotZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17MflUh|ryP NH3YTVg1KGR? M2nlWpJm\HWlZYOgeIhmKEmFNUFCpJZidHWnIH\vdkBl[XWwb4L1ZolkcW5ic3Xud4l1cX[rdIm= MWqyN|A3ODV5MB?=
Jurkat/DOX NUHpR2xJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\tcZd7PSEQvF2= NX\udnZkPCCm MofydoVlfWOnczD0bIUhUUN3MNMgeoFtfWViZn;yJIRifW6xcoXibYNqdiC|ZX7zbZRqfmm2eR?= MX2yN|A3ODV5MB?=
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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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