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 MnzLSpVv[3Srb36gRZN{[Xl? NXTTSHh1OC53wrFOwG0> NEW1bnQzPCCq M1noW5difGW{ NX7DRZdwdW:mdXzheIV{KHSqZTDn[Y5mKGW6cILld5Nqd25ib3[gUWFITS2DIH3lcYJmenN? NUC0b3d3OjVzMkOwPFI>
Eca109 NWj1[Xp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfRNE42NzJwNT:1JO69VQ>? MYSyOE81QC95MjDo M4\pZZdifGW{ M4r3cYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= MXeyOVEzOzB6Mh?=
Eca109 MlT3SpVv[3Srb36gRZN{[Xl? NVjjcZh4OC53wrFOwG0> NU[5WnR3Pi9zMj:yOEBp NUTaOIhHf2G2ZYK= MX7pcohq[mm2czDj[YxtKG2rZ4LheIlwdsLi MlfCNlUyOjNyOEK=
Eca109 Mn\pSpVv[3Srb36gRZN{[Xl? MWKwMlXDqM7:TR?= M333RVI1KGh? MoPje4F1\XJ? M4HqWIlvcGmkaYTzJINmdGxiaX72ZZNqd25? M4O5O|I2OTJ|MEiy
Eca109 NYe2T3hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\KUppCOC53wrFOwG0> NX;JV2tIOjRiaB?= MVn3ZZRmeg>? MojUbY5lfWOnczDHNk9OKGG{cnXzeEBqdiC2aHWgZ4VtdCCleXPs[S=> NXXnZYJkOjVzMkOwPFI>
Eca109 MonzSpVv[3Srb36gRZN{[Xl? M1j6blAvPS9zIN88US=> NHvNbXAzPCCq NXfqVpQ2f2G2ZYK= MUjk[YNz\WG|ZYOg[ZhxemW|c3nvckBw\iCQRj5OvmIzKGGwZDDNUXAz NI[zUIczPTF{M{C4Ni=>
SW1116  NU\WbmU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPFenUxNjVxMT:yM|Uh|ryP MojJOFghcA>? NHu4TZNFVVOR MnvQ[Y5p[W6lZYOgeIhmKEenZnn0bY5q[iCrbnT1Z4VlKGOnbHygbY5pcWKrdHnvci=> M3;K[lI1QDd2Mki2
LOVO NVS3[21OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXQNE42NzFxMj:1JO69VQ>? NWrYZ4lVPDhiaB?= NVLMVYJZTE2VTx?= M2fJWIVvcGGwY3XzJJRp\SCJZX\peIlvcWJiaX7keYNm\CClZXzsJIlvcGmkaYTpc44> NXLYWZE{OjR6N{SyPFY>
SW1116  Ml\qSpVv[3Srb36gRZN{[Xl? NVK1[XY6OTBizszN NY\1b|ZSPDhiaB?= NXTzeXIzTE2VTx?= NGrmblRqdmO{ZXHz[ZMhfGinIHXm[oVkfGm4ZTDheEBqdmirYnn0bY5oKEGNVDDhcoQhdVSRUjDzbYdv[WyrbnegdIF1cHejeYOgZ49u[mmwZXSge4l1cCCpZX\peIlvcWJ? NGnMPGYzPDh5NEK4Oi=>
LOVO NGi1UnVHfW6ldHnvckBCe3OjeR?= M3XKXlExKM7:TR?= MUi0PEBp Mn3iSG1UVw>? MmrmbY5kemWjc3XzJJRp\SCnZn\lZ5RqfmViYYSgbY5pcWKrdHnu[{BCU1RiYX7kJI1VV1Jic3nncoFtcW6pIIDheIh4[Xm|IHPvcYJqdmWmIIfpeIgh\2WoaYTpcolj MkK4NlQ5PzR{OE[=
SW1116  MkfURZBweHSxc3nzJGF{e2G7 NXL3bHlwOTBizszN M1q2TVQ5KGh? NH3Yb4VFVVOR M1;pdIVvcGGwY3XzJGdm\mm2aX7pZk1qdmS3Y3XkJIFxd3C2b4Ppdy=> MUiyOFg4PDJ6Nh?=
LOVO NUH4WpFHSXCxcITvd4l{KEG|c3H5 MVyxNEDPxE1? MXy0PEBp Mne5SG1UVw>? MVvlcohidmOnczDH[YZqfGmwaXKtbY5lfWOnZDDhdI9xfG:|aYO= M37nT|I1QDd2Mki2
RPMI-8226 MmDSRZBweHSxc3nzJGF{e2G7 MoDMNU8zKM7:TR?= MlH6OFgwPzJxOU[gbC=> MXvEUXNQ NUPUR3c3cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MUKyOFg{OzFyOB?=
OPM-2  MXfBdI9xfG:|aYOgRZN{[Xl? MonENU8zKM7:TR?= M{foUlczNzl4L{GyNEBp MVvEUXNQ NWDCendocW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NUDIPGdbOjR6M{OxNFg>
JJN3  M{XCS2Fxd3C2b4Ppd{BCe3OjeR?= NETCZXQxNjVxMTFOwG0> MX6yOE81QCCq M{[4Z2ROW09? MmDSbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NWXyWmdpOjR6M{OxNFg>
NCI-H929  NVKwU|hNSXCxcITvd4l{KEG|c3H5 M33scVEwOiEQvF2= MXu3Nk86Pi9zMkCgbC=> M4TQXGROW09? NYDMU5pmcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= M{\HNVI1QDN|MUC4
RPMI-8226 NWWzOlhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYexM|Ih|ryP NV;0NmNWOjRxNEivO|IhcA>? NVjZcoR7TE2VTx?= M{jsfYFn\mWldIOgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCwZXfheIl3\Wy7 NIfSb2wzPDh|M{GwPC=>
OPM-2  MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTId3djOS9{IN88US=> NH\nbo4zPC92OD:3NkBp NY\HZ5lHTE2VTx?= NFG4VnNi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= MYeyOFg{OzFyOB?=
JJN3  MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;WNlAvPS9zIN88US=> NX;CVlRZOjRxNEivO|IhcA>? NEj6cIRFVVOR NEKzRYZi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= MnTYNlQ5OzNzMEi=
NCI-H929  M1WxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxM|Ih|ryP MXKyOE81QC95MjDo NUPLPWVQTE2VTx?= NH3Bfndi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= Ml22NlQ5OzNzMEi=
HeLa MmTET4lv[XOnIFHzd4F6 M{[1Z2tqRTFyMEFihLM2ODByIN88UUBnd3JiaFXOWFE> NWfjWIRSOjR5OECwPVg>
HeLa MVnLbY5ie2ViQYPzZZk> M4\I[mtqRTVwNjFCtUAxNjVizszNJIZweiCqRV7UNi=> NHfHeo0zPDd6MEC5PC=>
HeLa NE[wd5VMcW6jc3WgRZN{[Xl? MlroT4k:OjFwNjFCtUA{NjBizszNJIZweiCqQ17UNS=> MlPsNlQ4QDByOUi=
HeLa M4L4N2tqdmG|ZTDBd5NigQ>? NWLvRVRFU2l;MUSuOEDDuSB2Lk[g{txOKG[xcjDoR25VOw>? MlLoNlQ4QDByOUi=
NB4 M3fKfmZ2dmO2aX;uJGF{e2G7 M4nFclIvPS93L{euOU8yOCEQvF2= M3zFdFI1KGh? MofkSG1UVw>? M3fZcolv[3KnYYPlZUB1cGViZYjwdoV{e2mxbjDv[kBxemWldYLzc5IhdWmULUGyOYE> NVflPFZJOjR2OES4O|A>
CD4+ CD25− T  MWPGeY5kfGmxbjDBd5NigQ>? MlXzNU82KM7:TR?= M1[xdZJm\HWlZWOg[4xw[mGuIFTORUBu\XSqeXzheIlwdg>? Mki4NlQ1PzZ|NkC=
BV-173 MVTBdI9xfG:|aYOgRZN{[Xl? MXqwMlI2NzBwNT:wMlc2NzFizszN Mlm2OFgwPzJxOU[gbC=> M2TZReKhWEKV M{LBdYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> NGiwUWgzPDR{M{[xNy=>
ML-1 NEfzXGNCeG:ydH;zbZMhSXO|YYm= M3nRVVAvOjVxMD61M|AvPzVxMTFOwG0> NFu4XXA1QC95Mj:5OkBp NVjoO41lyqCSQmO= NI\TfXJqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIJwfGhiZH;z[U0h[W6mIITpcYUuKGSncHXu[IVvfCCvYX7u[ZI> NFW5SpUzPDR{M{[xNy=>
HL-60 M4rBW2Fxd3C2b4Ppd{BCe3OjeR?= M37RUVAvOjVxMD61M|AvPzVxMTFOwG0> M1LFUVQ5Nzd{L{m2JIg> NGXCfFbDqFCEUx?= MlHWbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NYW2Opd[OjR2MkO2NVM>
KG-1a MoLLRZBweHSxc3nzJGF{e2G7 MWGwMlI2NzBwNT:wMlc2NzFizszN NVTGTIh2PDhxN{KvPVYhcA>? NWPndJFMyqCSQmO= NVTwe481cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz M3\XNlI1PDJ|NkGz
BV-173 M3KwbWZ2dmO2aX;uJGF{e2G7 Mlf2NlUxNzVyMH7N M3TieVQ5KGh? NEfzRpLDqFCEUx?= NF7CZlBqdmS3Y3XzJIRmdGG7ZXSgZY5lKHO3c4ThbY5m\CCUT2OgbY5kemWjc3W= M1;1PVI1PDJ|NkGz
CEM NUf2R3dHTnWwY4Tpc44hSXO|YYm= M1GxPFI2OC93MEDuUS=> MXO0PEBp M{Hp[eKhWEKV NYLQb29ncW6mdXPld{Bl\WyjeXXkJIFv\CC|dYP0ZYlv\WRiUl;TJIlv[3KnYYPl MV:yOFQzOzZzMx?=
HL-60 MYrGeY5kfGmxbjDBd5NigQ>? NVfMZlBNOjVyL{WwNI5O M{jWRlQ5KGh? M4r2XOKhWEKV NHvjWY1qdmS3Y3XzJIRmdGG7ZXSgZY5lKHO3c4ThbY5m\CCUT2OgbY5kemWjc3W= NGHUPJczPDR{M{[xNy=>
ML-1 MlPNSpVv[3Srb36gRZN{[Xl? NV72TnR2OjVyL{WwNI5O NHrwb3Y1QCCq MYhCpHBDWw>? M3\QZYlv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= Mm\tNlQ1OjN4MUO=
DLD-1 NWTHRohkTnWwY4Tpc44hSXO|YYm= M4m4NFI2OC93MEDuUS=> NFz6ZlU1QCCq MVdCpHBDWw>? NXW0bFlv\G9ibn;0JIlv\HWlZYOg[IVt[XmnZDDhcoQhe3W|dHHpcoVlKFKRUzDpcoNz\WG|ZR?= NX;BSXlwOjR2MkO2NVM>
HCT-116 M373[mZ2dmO2aX;uJGF{e2G7 NX7lT4Q1OjVyL{WwNI5O NVf6OmY1PDhiaB?= Moq5xsBRSlN? M4LGTYRwKG6xdDDpcoR2[2W|IHTlcIF6\WRiYX7kJJN2e3SjaX7l[EBTV1NiaX7jdoVie2V? M1rKeVI1PDJ|NkGz
U937-A/E-9/14/18  MnTLRZBweHSxc3nzJGF{e2G7 Mni0NE4xOS9yLkGvNU8yOCEQvF2= MmPvOFghcA>? NWTtOXhicW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MUOyOFMxODR3Nh?=
HT29 M3TudWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnKO|IhcA>? NV3pVVVPUUN3ME2xOFAxyrFzN{mg{txO NWXPPVcyOjRzN{KwOlE>
SW48 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljyO|IhcA>? NGDpTGdKSzVyPUG1MlLDuTZwMjFOwG0> MnX5NlQyPzJyNkG=
HCT116 M3\hfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYS3NkBp NHP6VFZKSzVyPUGuO:KyOC52IN88US=> NIPFTVgzPDF5MkC2NS=>
HepG2 NX3FTmNXTnWwY4Tpc44hSXO|YYm= M1;k[lAvPS9zIN88US=> MYCyOEBp NF\adpBFVVOR MmXveZAuemWpdXzheIVlKHSqZTDy[YxifGm4ZTDPR3RPOiCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? NHL0XGYzPDF2Nki3OC=>
LS174T NVqwc|EzTnWwY4Tpc44hSXO|YYm= NFr0XZkxNjVxMTFOwG0> Mm\QNlQhcA>? NYnZSpZLTE2VTx?= M4e3PYxm[WRidH:gZY4hcW6lcnXhd4Uhd2ZiT1PUUlIhdGW4ZXzz M1XnN|I1OTR4OEe0
HepG2 NXjEOlhKSXCxcITvd4l{KEG|c3H5 MUSxM|ExNzFyMDFOwG0> MkTIO{Bl NUPKTYZxTE2VTx?= MknSbY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mmr5NlQyPDZ6N{S=
LS174T M{TPd2Fxd3C2b4Ppd{BCe3OjeR?= MoHtNU8yOC9zMECg{txO MkjDO{Bl MUPEUXNQ Ml\2bY5lfWOnczDj[YxtKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MlHvNlQyPDZ6N{S=
QBC-939 Ml\WRZBweHSxc3nzJGF{e2G7 NFjlUnkyNzFyL{GwNEDPxE1? M2jkVVch\A>? M{C0Z2ROW09? NHu3UIFqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M{jhTlI1OTR4OEe0
U251 M3GycWFxd3C2b4Ppd{BCe3OjeR?= NEO4fYUyNzFyL{GwNEDPxE1? NXHrSHJJPyCm MlzlSG1UVw>? NGrlT2hqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MWqyOFE1Pjh5NB?=
HL-60 M4CxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYexJO69VQ>? NH3QO3c1QCCq MYTpcoNz\WG|ZYOgS|IueGijc3WgZ4VtdCCocnHjeIlwdg>? M{LEVVI1ODByM{K0
MDA‑MB‑453 MWLGeY5kfGmxbjDBd5NigQ>? MVmwMlIwOSEQvF2= M2f3W|czKGh? NUHlS2pI[2G3c3XzJJJmNWW6cILld5Nqd25ib3[gZ4xifWSrbtMgNeKh NFzTUZUzOzh2NEKyPC=>
HCC1569 NFvQZWFHfW6ldHnvckBCe3OjeR?= NG[2[JMxNjJxMTFOwG0> MmHrO|IhcA>? Mn\sZ4F2e2W|IILlMYV5eHKnc4Ppc44hd2ZiY3zheYRqdsLiMdMg M3LU[lI{QDR2MkK4
BT‑474 MnO2SpVv[3Srb36gRZN{[Xl? MkOxNE4zNzFizszN Mlq3O|IhcA>? MXvjZZV{\XNicnWt[ZhxemW|c3nvckBw\iClbHH1[IlvyqBzwrC= NFG3[pUzOzh2NEKyPC=>
AGS MUTBdI9xfG:|aYOgRZN{[Xl? NGLjNII2NzFyL{KwM|UxKM7:TR?= NIO2RVE1QMLiaNMg MYrEUXNQ MlTObY5pcWKrdIOgeIhmKGOnbHygeoli[mmuaYT5xsA> NEHWVXAzOzV6Mke4OC=>
A549 NX7tSZpQSXCxcITvd4l{KEG|c3H5 NFrpRW42NzFyL{KwM|UxKM7:TR?= M4DDfVQ5yqCqwrC= MoT2SG1UVw>? NWjjOI53cW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6yqB? NHX2S3EzOzV6Mke4OC=>
AGS  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr2Wo82NzFyL{KwM|UxKM7:TR?= MYK0POKhcMLi NX;Yb4dWTE2VTx?= MWrpcoR2[2W|IFeyM20heGijc3WgZZJz\XO2wrC= NIOzUWIzOzV6Mke4OC=>
Kasumi-1 MkLjRZBweHSxc3nzJGF{e2G7 MWmwMlUh|ryP M1P6XFQ5yqCqwrC= NWrVfms1\GWlcnXhd4V{KHSqZTDj[YxtKH[rYXLpcIl1gSClbz30doVifGWmIIfpeIghXGZvTmCtd4M> M{LEbFI{PDl|M{S4
OCI-AML3 NYT4SWxsSXCxcITvd4l{KEG|c3H5 M2[2VFIvPSEQvF2= MUC0POKhcMLi MX\k[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JINwNXS{ZXH0[YQhf2m2aDDU[k1PWC2|Yx?= NXjITpU{OjN2OUOzOFg>
MV4-11 MWLBdI9xfG:|aYOgRZN{[Xl? M2jYR|IvPSEQvF2= NELkfoQ1QMLiaNMg NXzld|NX\GWlcnXhd4V{KHSqZTDj[YxtKH[rYXLpcIl1gSClbz30doVifGWmIIfpeIghXGZvTmCtd4M> M2nXflI{PDl|M{S4
NK  NE\ETJNEgXSxdH;4bZR6KEG|c3H5 MXiwMlAzNTJyIN88US=> MkmxOUBl NH;6ZXRl\WO{ZXHz[ZMhfGinIHP5eI9tgXSrYzDhZ5Rqfmm2eTDv[kBPUyClZXzsd{BifCCrboTldo1m\GmjdHWgZ49v[2WwdILheIlwdnNicnXzeYx1cW6pIHnuJIEhXS2|aHHw[YQh\G:|ZfMAl5Jme3CxboPlJIN2en[n NHf2UVAzOzN{OEC4PC=>
NK  NGnXR2VCeG:ydH;zbZMhSXO|YYm= NXywU3BPOC5yMj2yNEDPxE1? M1S3flUh\A>? NHXuU5Vl\WO{ZXHz[UBPUyClZXzsJJBzd2yrZnXyZZRqd25iYX7kJJZq[WKrbHn0fUBieyC2aHWgZ49v[2WwdILheIlwdiCrbnPy[YF{\WR? NXi3blg3OjN|MkiwPFg>
NK  NWr4XJhZTnWwY4Tpc44hSXO|YYm= M1O3TVAvODFvMkCg{txO MXi1JIQ> MnO3Z4F2e2W|IHj5dI9u\XSqeXzheIlwdiCxZjDOT{Bk\WyuczDpckBiKGSxc3ZihLNz\XOyb37z[S=> M2XlOlI{OzJ6MEi4
MOLT4/DNR MWTGeY5kfGmxbjDBd5NigQ>? NIrhS5g2KM7:TR?= Ml;rOEBl M3O4NZJm\HWlZYOgRWJESjFibWLORUBmgHC{ZYPzbY9v NH35NVYzOzB4MEW3NC=>
Jurkat/DOX M4[2[WZ2dmO2aX;uJGF{e2G7 NI[yVVU2KM7:TR?= MUW0JIQ> NYXaboozemWmdXPld{BCSkOEMTDtVm5CKGW6cILld5Nqd25? NEPZOpIzOzB4MEW3NC=>
MOLT4/DNR M{WwWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrLWpU6PSEQvF2= MYC0JIQ> NXzCd3NuemWmdXPld{B1cGViSVO1NOKhfmGudXWg[o9zKGSjdX7vdpVjcWOrbjDz[Y5{cXSrdnn0fS=> MVGyN|A3ODV5MB?=
Jurkat/DOX NIS3b2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHIOUDPxE1? MkSyOEBl MoPadoVlfWOnczD0bIUhUUN3MNMgeoFtfWViZn;yJIRifW6xcoXibYNqdiC|ZX7zbZRqfmm2eR?= MYOyN|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

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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