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 MYDGeY5kfGmxbjDBd5NigQ>? MnrpNE42yqEQvF2= MnXnNlQhcA>? MXT3ZZRmeg>? Mof5cY9lfWyjdHXzJJRp\SCpZX7lJIV5eHKnc4Ppc44hd2ZiTVHHSU1CKG2nbXLldpM> MX2yOVEzOzB6Mh?=
Eca109 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnrNoJnOC53L{KuOU82KM7:TR?= NHvnS|gzPC92OD:3NkBp MlrFe4F1\XJ? MU\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ MUSyOVEzOzB6Mh?=
Eca109 MlnlSpVv[3Srb36gRZN{[Xl? M4jBVFAvPcLizszN NIjaOmg3NzF{L{K0JIg> M3jZfpdifGW{ NIDHOZNqdmirYnn0d{Bk\WyuIH3p[5JifGmxbtMg NFrCcGwzPTF{M{C4Ni=>
Eca109 MWPGeY5kfGmxbjDBd5NigQ>? NHzlZmkxNjYEoN88US=> M2DhVFI1KGh? MUX3ZZRmeg>? NXy0XmhKcW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MXqyOVEzOzB6Mh?=
Eca109 M3XU[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml71NE42yqEQvF2= MUSyOEBp NELGOld4[XSnch?= NUP2cHdFcW6mdXPld{BIOi:PIHHydoV{fCCrbjD0bIUh[2WubDDjfYNt\Q>? MmftNlUyOjNyOEK=
Eca109 Mlv6SpVv[3Srb36gRZN{[Xl? MUSwMlUwOSEQvF2= M2PyZ|I1KGh? NUPvcWl4f2G2ZYK= MWnk[YNz\WG|ZYOg[ZhxemW|c3nvckBw\iCQRj5OvmIzKGGwZDDNUXAz M2jYU|I2OTJ|MEiy
SW1116  M1fj[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnkNnIxNjVxMT:yM|Uh|ryP M2K0W|Q5KGh? MULEUXNQ MWnlcohidmOnczD0bIUhT2WoaYTpcoljKGmwZIXj[YQh[2WubDDpcohq[mm2aX;u NF3LWZUzPDh5NEK4Oi=>
LOVO NIfMZodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;6NE42NzFxMj:1JO69VQ>? MUi0PEBp NH3QfGlFVVOR NFvDeVlmdmijbnPld{B1cGViR3XmbZRqdmmkIHnu[JVk\WRiY3XscEBqdmirYnn0bY9v MlfDNlQ5PzR{OE[=
SW1116  NXTHNnZYTnWwY4Tpc44hSXO|YYm= NWm2UXNZOTBizszN Mm[zOFghcA>? NWKwUG5bTE2VTx?= NYfhT|FncW6lcnXhd4V{KHSqZTDl[oZm[3SrdnWgZZQhcW6qaXLpeIlv\yCDS2SgZY5lKG2WT2Kgd4lodmGuaX7nJJBifGi5YYnzJINwdWKrbnXkJJdqfGhiZ3XmbZRqdmmk NYjuXJNJOjR6N{SyPFY>
LOVO NYjoXphoTnWwY4Tpc44hSXO|YYm= Mnm2NVAh|ryP MUW0PEBp M3jJPWROW09? NHyxN5NqdmO{ZXHz[ZMhfGinIHXm[oVkfGm4ZTDheEBqdmirYnn0bY5oKEGNVDDhcoQhdVSRUjDzbYdv[WyrbnegdIF1cHejeYOgZ49u[mmwZXSge4l1cCCpZX\peIlvcWJ? MorwNlQ5PzR{OE[=
SW1116  NEPLfpRCeG:ydH;zbZMhSXO|YYm= NX3OfFZrOTBizszN M4P5blQ5KGh? M1W2VGROW09? NE\icIFmdmijbnPld{BI\W[rdHnubYIucW6mdXPl[EBieG:ydH;zbZM> MXuyOFg4PDJ6Nh?=
LOVO NWXIU49[SXCxcITvd4l{KEG|c3H5 NFv6VHoyOCEQvF2= MoDpOFghcA>? NX3oUZozTE2VTx?= NITNTGRmdmijbnPld{BI\W[rdHnubYIucW6mdXPl[EBieG:ydH;zbZM> MoP0NlQ5PzR{OE[=
RPMI-8226 M2P5[2Fxd3C2b4Ppd{BCe3OjeR?= M{W1[lEwOiEQvF2= NWPWVYVVPDhxN{KvPVYhcA>? MlX3SG1UVw>? MmXObY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? Moq2NlQ5OzNzMEi=
OPM-2  M1LCVmFxd3C2b4Ppd{BCe3OjeR?= MkfkNU8zKM7:TR?= M1zkNVczNzl4L{GyNEBp MV\EUXNQ NXTWRW1NcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= M3;JcFI1QDN|MUC4
JJN3  MoLGRZBweHSxc3nzJGF{e2G7 NUfqNoN2OC53L{Gg{txO M{nhU|I1NzR6IHi= Mly3SG1UVw>? M4fueYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MmjDNlQ5OzNzMEi=
NCI-H929  MoDlRZBweHSxc3nzJGF{e2G7 MXexM|Ih|ryP NEW3Wmg4Oi97Nj:xNlAhcA>? NVq1W25KTE2VTx?= NUO3N4hScW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NHXpdZQzPDh|M{GwPC=>
RPMI-8226 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX:xM|Ih|ryP MYWyOE81QC95MjDo M{TLVWROW09? NUPPZodE[W[oZXP0d{Bk\WyuIHP5Z4xmKHC{b3fy[ZN{cW:wIH7l[4F1cX[nbIm= MonkNlQ5OzNzMEi=
OPM-2  M2\GTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTsNU8zKM7:TR?= M4jVV|I1NzR6L{eyJIg> NGT2NXFFVVOR MlTpZYZn\WO2czDj[YxtKGO7Y3zlJJBzd2e{ZYPzbY9vKG6nZ3H0bZZmdHl? NHT6VGwzPDh|M{GwPC=>
JJN3  MnfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\kZYVROC53L{Gg{txO MnLUNlQwPDhxN{KgbC=> NH7oOYNFVVOR MUjh[oZm[3S|IHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44hdmWpYYTpeoVtgQ>? MUmyOFg{OzFyOB?=
NCI-H929  NVvoWIlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13Jc|EwOiEQvF2= NVrrW3U3OjRxNEivO|IhcA>? MX\EUXNQ NYe1bHlt[W[oZXP0d{Bk\WyuIHP5Z4xmKHC{b3fy[ZN{cW:wIH7l[4F1cX[nbIm= M37BZVI1QDN|MUC4
HeLa MWTLbY5ie2ViQYPzZZk> NWL5NIlpU2l;MUCwNQKBmzVyMECg{txOKG[xcjDoSW5VOQ>? NIHSPZQzPDd6MEC5PC=>
HeLa NV[zRZRoU2mwYYPlJGF{e2G7 MXjLbV02NjZiwsGgNE42KM7:TTDmc5IhcEWQVEK= MWeyOFc5ODB7OB?=
HeLa M3fWPWtqdmG|ZTDBd5NigQ>? NF7rflNMcT1{MT62JOKyKDNwMDFOwG0h\m:{IHjDUnQy M3XKZVI1PzhyMEm4
HeLa M3HkemtqdmG|ZTDBd5NigQ>? NXviToVZU2l;MUSuOEDDuSB2Lk[g{txOKG[xcjDoR25VOw>? M4jhXVI1PzhyMEm4
NB4 NXfRbWFrTnWwY4Tpc44hSXO|YYm= MYiyMlUwPS95LkWvNVAh|ryP NUnEc4VbOjRiaB?= Mn22SG1UVw>? NYDkWIF6cW6lcnXhd4ViKHSqZTDlfJBz\XO|aX;uJI9nKHC{ZXP1dpNweiCvaWKtNVI2[Q>? M4rIWVI1PDh2OEew
CD4+ CD25− T  NY\VSINCTnWwY4Tpc44hSXO|YYm= Mn3PNU82KM7:TR?= M{PqW5Jm\HWlZWOg[4xw[mGuIFTORUBu\XSqeXzheIlwdg>? M1mxNFI1PDd4M{[w
BV-173 NVi1dWtKSXCxcITvd4l{KEG|c3H5 Mn3sNE4zPS9yLkWvNE44PS9zIN88US=> NGLVcWg1QC95Mj:5OkBp M4nQOuKhWEKV NEXuOIJqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIJwfGhiZH;z[U0h[W6mIITpcYUuKGSncHXu[IVvfCCvYX7u[ZI> NVXDfndYOjR2MkO2NVM>
ML-1 MXrBdI9xfG:|aYOgRZN{[Xl? M2rOfFAvOjVxMD61M|AvPzVxMTFOwG0> NHGwbXY1QC95Mj:5OkBp M3fGOuKhWEKV NHTJTllqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIJwfGhiZH;z[U0h[W6mIITpcYUuKGSncHXu[IVvfCCvYX7u[ZI> M1TvSVI1PDJ|NkGz
HL-60 MWrBdI9xfG:|aYOgRZN{[Xl? M1XCelAvOjVxMD61M|AvPzVxMTFOwG0> M4H6fFQ5Nzd{L{m2JIg> NWi0NZhoyqCSQmO= MWXpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= NE\KToYzPDR{M{[xNy=>
KG-1a NFm3OlVCeG:ydH;zbZMhSXO|YYm= M3r5WlAvOjVxMD61M|AvPzVxMTFOwG0> MWS0PE84Oi97NjDo NHzY[XDDqFCEUx?= NXPMcWpCcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz MlftNlQ1OjN4MUO=
BV-173 NETTO|BHfW6ldHnvckBCe3OjeR?= MnPvNlUxNzVyMH7N MYO0PEBp MUlCpHBDWw>? M3L4SIlv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= MnO4NlQ1OjN4MUO=
CEM M3LUPWZ2dmO2aX;uJGF{e2G7 NYnqU41mOjVyL{WwNI5O NU\JOXVMPDhiaB?= NUj3W2lZyqCSQmO= MUnpcoR2[2W|IHTlcIF6\WRiYX7kJJN2e3SjaX7l[EBTV1NiaX7jdoVie2V? NGfsNoIzPDR{M{[xNy=>
HL-60 M4PWNmZ2dmO2aX;uJGF{e2G7 MmK2NlUxNzVyMH7N MlGyOFghcA>? M{DJcuKhWEKV MVTpcoR2[2W|IHTlcIF6\WRiYX7kJJN2e3SjaX7l[EBTV1NiaX7jdoVie2V? MX6yOFQzOzZzMx?=
ML-1 M1i1cWZ2dmO2aX;uJGF{e2G7 NVnabWJROjVyL{WwNI5O MXe0PEBp NHPNb3HDqFCEUx?= M4DUNIlv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= M1S4SVI1PDJ|NkGz
DLD-1 NVLzU2Y{TnWwY4Tpc44hSXO|YYm= NHzJNXkzPTBxNUCwcm0> NIPiUGE1QCCq MVVCpHBDWw>? NIjVRWJldyCwb4SgbY5lfWOnczDk[YxigWWmIHHu[EB{fXO2YXnu[YQhWk:VIHnuZ5Jm[XOn M2PFdlI1PDJ|NkGz
HCT-116 NUH2RWZrTnWwY4Tpc44hSXO|YYm= NIHEOWgzPTBxNUCwcm0> MUO0PEBp MUdCpHBDWw>? NXPZPJJY\G9ibn;0JIlv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= NFTpN5IzPDR{M{[xNy=>
U937-A/E-9/14/18  NXnlUGVRSXCxcITvd4l{KEG|c3H5 NV;vPIVyOC5yMT:wMlEwOS9zMDFOwG0> NF;ueFk1QCCq NXK1e5E{cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MmLjNlQ{ODB2NU[=
HT29 M{K3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr2XGs4OiCq NV\SXotWUUN3ME2xOFAxyrFzN{mg{txO M132WVI1OTd{ME[x
SW48 NVTMZopxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO4WYl1PzJiaB?= MX7JR|UxRTF3LkNCtVYvOiEQvF2= MUCyOFE4OjB4MR?=
HCT116 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXy3NkBp M2HTNmlEPTB;MT63xtExNjRizszN MWWyOFE4OjB4MR?=
HepG2 MlPjSpVv[3Srb36gRZN{[Xl? NFPlbHIxNjVxMTFOwG0> MkP0NlQhcA>? M17yb2ROW09? MVz1dE1z\We3bHH0[YQhfGinIILlcIF1cX[nIF;DWG4zKG2UTlGgZY5lKHC{b4TlbY4h\XiycnXzd4lwdg>? NEL6T3gzPDF2Nki3OC=>
LS174T NXi2d2pvTnWwY4Tpc44hSXO|YYm= MlSwNE42NzFizszN MlH1NlQhcA>? M2PYd2ROW09? MkO4cIVi\CC2bzDhckBqdmO{ZXHz[UBw\iCRQ2TONkBt\X[nbIO= Ml7XNlQyPDZ6N{S=
HepG2 NU\TV5ZESXCxcITvd4l{KEG|c3H5 M3;jcVEwOTBxMUCwJO69VQ>? NWTqemdEPyCm NEH5V2xFVVOR NI\teplqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M3XtfFI1OTR4OEe0
LS174T NGDT[FlCeG:ydH;zbZMhSXO|YYm= MnP3NU8yOC9zMECg{txO NX7kVZZnPyCm NHjXU5pFVVOR MWPpcoR2[2W|IHPlcIwh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEX4RngzPDF2Nki3OC=>
QBC-939 NWfnOIdKSXCxcITvd4l{KEG|c3H5 NHnBbWcyNzFyL{GwNEDPxE1? NET4flA4KGR? NHfNPXdFVVOR M3XKTYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2TwSVI1OTR4OEe0
U251 MmDHRZBweHSxc3nzJGF{e2G7 MYSxM|ExNzFyMDFOwG0> NYTJXmVlPyCm Mmm5SG1UVw>? NV3hcGdkcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NVKzO2w{OjRzNE[4O|Q>
HL-60 M3XlSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTo[llEOSEQvF2= MWe0PEBp M4L2OIlv[3KnYYPld{BIOi2yaHHz[UBk\WyuIH\yZYN1cW:w M1;TTFI1ODByM{K0
MDA‑MB‑453 NVy3b|dxTnWwY4Tpc44hSXO|YYm= NUDRTYtOOC5{L{Gg{txO NIjGSY44OiCq NWSyO5cz[2G3c3XzJJJmNWW6cILld5Nqd25ib3[gZ4xifWSrbtMgNeKh MkTsNlM5PDR{Mki=
HCC1569 NVrTfWp2TnWwY4Tpc44hSXO|YYm= MY[wMlIwOSEQvF2= NIfRN2c4OiCq MnLlZ4F2e2W|IILlMYV5eHKnc4Ppc44hd2ZiY3zheYRqdsLiMdMg NHfKNZkzOzh2NEKyPC=>
BT‑474 NE\vc5JHfW6ldHnvckBCe3OjeR?= NVzh[IlZOC5{L{Gg{txO MWK3NkBp MVzjZZV{\XNicnWt[ZhxemW|c3nvckBw\iClbHH1[IlvyqBzwrC= MYiyN|g1PDJ{OB?=
AGS M3XqOWFxd3C2b4Ppd{BCe3OjeR?= NYPmT5VPPS9zMD:yNE82OCEQvF2= MnO4OFjDqGkEoB?= MnfsSG1UVw>? M1e4[olvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0feKh NFfKd2wzOzV6Mke4OC=>
A549 MULBdI9xfG:|aYOgRZN{[Xl? NHv2dIs2NzFyL{KwM|UxKM7:TR?= M2H1NlQ5yqCqwrC= M1zFUWROW09? MnPObY5pcWKrdIOgeIhmKGOnbHygeoli[mmuaYT5xsA> NHLYO3UzOzV6Mke4OC=>
AGS  MoTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fXS|UwOTBxMkCvOVAh|ryP NVHvNGtuPDkEoHlCpC=> MVfEUXNQ M4L6colv\HWlZYOgS|IwVSCyaHHz[UBienKnc4VCpC=> NYn4[GpWOjN3OEK3PFQ>
Kasumi-1 MX\BdI9xfG:|aYOgRZN{[Xl? NGTMRYoxNjVizszN M4S0TFQ5yqCqwrC= NIDLUWJl\WO{ZXHz[ZMhfGinIHPlcIwhfmmjYnnsbZR6KGOxLYTy[YF1\WRid3n0bEBV\i2QUD3zZy=> MXGyN|Q6OzN2OB?=
OCI-AML3 MlnYRZBweHSxc3nzJGF{e2G7 NFnrU|QzNjVizszN MWm0POKhcMLi M3L1NoRm[3KnYYPld{B1cGViY3XscEB3cWGkaXzpeJkh[29vdILlZZRm\CC5aYToJHRnNU6SLYPj MX:yN|Q6OzN2OB?=
MV4-11 M2LIemFxd3C2b4Ppd{BCe3OjeR?= MVeyMlUh|ryP NX;mcHRwPDkEoHlCpC=> MWLk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JINwNXS{ZXH0[YQhf2m2aDDU[k1PWC2|Yx?= NVnkfohmOjN2OUOzOFg>
NK  NF;PXFBEgXSxdH;4bZR6KEG|c3H5 MoezNE4xOi1{MDFOwG0> NILXZ|M2KGR? NGLvPWdl\WO{ZXHz[ZMhfGinIHP5eI9tgXSrYzDhZ5Rqfmm2eTDv[kBPUyClZXzsd{BifCCrboTldo1m\GmjdHWgZ49v[2WwdILheIlwdnNicnXzeYx1cW6pIHnuJIEhXS2|aHHw[YQh\G:|ZfMAl5Jme3CxboPlJIN2en[n MnHLNlM{OjhyOEi=
NK  M3LPfWFxd3C2b4Ppd{BCe3OjeR?= MkfFNE4xOi1{MDFOwG0> MV:1JIQ> MmXE[IVkemWjc3WgUmsh[2WubDDwdo9tcW[ncnH0bY9vKGGwZDD2bYFjcWyrdImgZZMhfGinIHPvcoNmdnS{YYTpc44hcW6lcnXhd4Vl NYjLeZR7OjN|MkiwPFg>
NK  NWjmZWdkTnWwY4Tpc44hSXO|YYm= M3XyS|AvODFvMkCg{txO NXG3eXloPSCm MmDvZ4F2e2W|IHj5dI9u\XSqeXzheIlwdiCxZjDOT{Bk\WyuczDpckBiKGSxc3ZihLNz\XOyb37z[S=> MYeyN|MzQDB6OB?=
MOLT4/DNR MUfGeY5kfGmxbjDBd5NigQ>? NGHnTo02KM7:TR?= M3m3NVQh\A>? M3nHNZJm\HWlZYOgRWJESjFibWLORUBmgHC{ZYPzbY9v MXSyN|A3ODV5MB?=
Jurkat/DOX NF20O5ZHfW6ldHnvckBCe3OjeR?= NFzSeJo2KM7:TR?= M2XM[FQh\A>? MlLqdoVlfWOnczDBRmNDOSCvUl7BJIV5eHKnc4Ppc44> MnrONlMxPjB3N{C=
MOLT4/DNR NEXxfolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUC1JO69VQ>? NF6yWJg1KGR? NF\FdFNz\WS3Y3XzJJRp\SCLQ{WwxsB3[Wy3ZTDmc5Ih\GG3bn;yeYJq[2mwIIPlcpNqfGm4aYT5 NHHmR5QzOzB4MEW3NC=>
Jurkat/DOX NUPmfVFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\ySnM2KM7:TR?= MW[0JIQ> NX\JRZVMemWmdXPld{B1cGViSVO1NOKhfmGudXWg[o9zKGSjdX7vdpVjcWOrbjDz[Y5{cXSrdnn0fS=> MkXVNlMxPjB3N{C=
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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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