Decitabine

Decitabineは一種のDNA methylationの有効な阻害剤で、骨髄異形成症候群(MDS)を治療することに使用されます。

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電話番号: + 81 3-5632-9610mail@cosmobio.co.jp

Decitabine 化学構造
分子量: 228.21

高品質保証

カスタマーフィードバック(3)

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 Decitabineは一種のDNA methylationの有効な阻害剤で、骨髄異形成症候群(MDS)を治療することに使用されます。
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 MV\GeY5kfGmxbjDBd5NigQ>? MXSwMlXDqM7:TR?= NXLKTnVxOjRiaB?= M1rKcZdifGW{ M4j4eI1w\HWuYYTld{B1cGViZ3Xu[UBmgHC{ZYPzbY9vKG:oIF3BS2UuSSCvZX3i[ZJ{ MU[yOVEzOzB6Mh?=
Eca109 NETLOWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TheVAvPS9{LkWvOUDPxE1? MWOyOE81QC95MjDo NXPVXIpEf2G2ZYK= NXvZeZcxcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> M4DyelI2OTJ|MEiy
Eca109 NYmxVXlwTnWwY4Tpc44hSXO|YYm= MUCwMlXDqM7:TR?= NH3MNHI3NzF{L{K0JIg> MkXGe4F1\XJ? NGHvZYtqdmirYnn0d{Bk\WyuIH3p[5JifGmxbtMg MXiyOVEzOzB6Mh?=
Eca109 M1q5WGZ2dmO2aX;uJGF{e2G7 NUDafG1JOC53wrFOwG0> MnvZNlQhcA>? M4O3bJdifGW{ NWP6ZVBOcW6qaXLpeJMh[2WubDDpcpZie2mxbh?= MY[yOVEzOzB6Mh?=
Eca109 Ml73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYCwMlXDqM7:TR?= M4TBNlI1KGh? NUPZOppkf2G2ZYK= NXTjc2lVcW6mdXPld{BIOi:PIHHydoV{fCCrbjD0bIUh[2WubDDjfYNt\Q>? M4XKVVI2OTJ|MEiy
Eca109 MWLGeY5kfGmxbjDBd5NigQ>? Mon6NE42NzFizszN Mmq4NlQhcA>? M3\6[ZdifGW{ MnLI[IVkemWjc3XzJIV5eHKnc4Ppc44hd2ZiTl[t{tpDOiCjbnSgUW1ROg>? NXXEPJBoOjVzMkOwPFI>
SW1116  MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqwMlUwOS9{L{Wg{txO M3v1U|Q5KGh? M1nQNWROW09? M1nBPYVvcGGwY3XzJJRp\SCJZX\peIlvcWJiaX7keYNm\CClZXzsJIlvcGmkaYTpc44> M33ze|I1QDd2Mki2
LOVO NGDVepJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzDc4hmOC53L{GvNk82KM7:TR?= MnnMOFghcA>? M{XFcWROW09? NV7oWXFt\W6qYX7j[ZMhfGinIFfl[ol1cW6rYjDpcoR2[2WmIHPlcIwhcW6qaXLpeIlwdg>? MoGwNlQ5PzR{OE[=
SW1116  NGWyOohHfW6ldHnvckBCe3OjeR?= MmLmNVAh|ryP NVXtSFc6PDhiaB?= NFLiO4tFVVOR NW\6VVZ{cW6lcnXhd4V{KHSqZTDl[oZm[3SrdnWgZZQhcW6qaXLpeIlv\yCDS2SgZY5lKG2WT2Kgd4lodmGuaX7nJJBifGi5YYnzJINwdWKrbnXkJJdqfGhiZ3XmbZRqdmmk MkfhNlQ5PzR{OE[=
LOVO MkjrSpVv[3Srb36gRZN{[Xl? M{DhfFExKM7:TR?= MnnEOFghcA>? MlLkSG1UVw>? MWPpcoNz\WG|ZYOgeIhmKGWoZnXjeIl3\SCjdDDpcohq[mm2aX7nJGFMXCCjbnSgcXRQWiC|aXfuZYxqdmdicHH0bJdigXNiY3;tZolv\WRid3n0bEBo\W[rdHnubYI> M3:5NlI1QDd2Mki2
SW1116  MlTpRZBweHSxc3nzJGF{e2G7 NEPCR5IyOCEQvF2= M3\r[FQ5KGh? NIf4eXFFVVOR MYflcohidmOnczDH[YZqfGmwaXKtbY5lfWOnZDDhdI9xfG:|aYO= NXXGXoFZOjR6N{SyPFY>
LOVO NXGwb4JpSXCxcITvd4l{KEG|c3H5 M1;4SVExKM7:TR?= MkDEOFghcA>? NFXyW4tFVVOR NFrXS5hmdmijbnPld{BI\W[rdHnubYIucW6mdXPl[EBieG:ydH;zbZM> M1Ky[|I1QDd2Mki2
RPMI-8226 NH22O3pCeG:ydH;zbZMhSXO|YYm= M1HlfFEwOiEQvF2= NUPnXnE1PDhxN{KvPVYhcA>? NXv2[oRzTE2VTx?= MmjHbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MYGyOFg{OzFyOB?=
OPM-2  Mmm3RZBweHSxc3nzJGF{e2G7 NI[yRYkyNzJizszN M3Wxb|czNzl4L{GyNEBp MVzEUXNQ MYrpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NXO4R5ltOjR6M{OxNFg>
JJN3  NFW2cG1CeG:ydH;zbZMhSXO|YYm= NFTIcWwxNjVxMTFOwG0> MYSyOE81QCCq MV7EUXNQ MlzpbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MX[yOFg{OzFyOB?=
NCI-H929  MlryRZBweHSxc3nzJGF{e2G7 MVGxM|Ih|ryP Mlu3O|IwQTZxMUKwJIg> MnjCSG1UVw>? M4fidIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NUXodYRrOjR6M{OxNFg>
RPMI-8226 NFrrXG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEiyb3YyNzJizszN NIHSXlkzPC92OD:3NkBp MmXJSG1UVw>? NGPhcoti\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= M3nz[|I1QDN|MUC4
OPM-2  MnzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPhNU8zKM7:TR?= NXfIRos4OjRxNEivO|IhcA>? MlO0SG1UVw>? NFjNN|Fi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= NUXYTllTOjR6M{OxNFg>
JJN3  NGH0R2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPNPI0xNjVxMTFOwG0> M1PLUlI1NzR6L{eyJIg> NGPVNVNFVVOR NFrueXRi\m[nY4TzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25ibnXnZZRqfmWueR?= MUOyOFg{OzFyOB?=
NCI-H929  NFfR[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH4VnUyNzJizszN M4jB[lI1NzR6L{eyJIg> NXXnOJAxTE2VTx?= M{L6[YFn\mWldIOgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCwZXfheIl3\Wy7 NFrJe2QzPDh|M{GwPC=>
HeLa M1rQcWtqdmG|ZTDBd5NigQ>? MkLrT4k:OTByMPMAl|UxODBizszNJIZweiCqRV7UNS=> MX2yOFc5ODB7OB?=
HeLa MnvGT4lv[XOnIFHzd4F6 M3Pmb2tqRTVwNjFCtUAxNjVizszNJIZweiCqRV7UNi=> NUXhS3JpOjR5OECwPVg>
HeLa NYm5SGlpU2mwYYPlJGF{e2G7 MkCwT4k:OjFwNjFCtUA{NjBizszNJIZweiCqQ17UNS=> MUiyOFc5ODB7OB?=
HeLa NGTNXVJMcW6jc3WgRZN{[Xl? M4XtcGtqRTF2LkSgxtEhPC54IN88UUBnd3JiaFPOWFM> MlnsNlQ4QDByOUi=
NB4 NXzod292TnWwY4Tpc44hSXO|YYm= NYPhRWR4Oi53L{WvO{42NzFyIN88US=> MknUNlQhcA>? MVrEUXNQ M1fMW4lv[3KnYYPlZUB1cGViZYjwdoV{e2mxbjDv[kBxemWldYLzc5IhdWmULUGyOYE> Mn;jNlQ1QDR6N{C=
CD4+ CD25− T  MnrPSpVv[3Srb36gRZN{[Xl? NXftZo5KOS93IN88US=> MXTy[YR2[2WVIHfsc4JidCCGTlGgcYV1cHmuYYTpc44> Mlq3NlQ1PzZ|NkC=
BV-173 Mn22RZBweHSxc3nzJGF{e2G7 NU\YNIVrOC5{NT:wMlUwOC55NT:xJO69VQ>? M2q5dFQ5Nzd{L{m2JIg> MlezxsBRSlN? NWT1XVM2cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NHHOTmozPDR{M{[xNy=>
ML-1 NUHTNpJwSXCxcITvd4l{KEG|c3H5 NVSy[3NkOC5{NT:wMlUwOC55NT:xJO69VQ>? NVqzblZpPDhxN{KvPVYhcA>? NG\6cXbDqFCEUx?= NWXOSFlNcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz M4C0PFI1PDJ|NkGz
HL-60 M1L1O2Fxd3C2b4Ppd{BCe3OjeR?= M{nudFAvOjVxMD61M|AvPzVxMTFOwG0> NEDNTHg1QC95Mj:5OkBp M{nYRuKhWEKV NEHUdnlqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIJwfGhiZH;z[U0h[W6mIITpcYUuKGSncHXu[IVvfCCvYX7u[ZI> NXmyWXhpOjR2MkO2NVM>
KG-1a NVXwe5VNSXCxcITvd4l{KEG|c3H5 M1vGflAvOjVxMD61M|AvPzVxMTFOwG0> NE\aVXM1QC95Mj:5OkBp NXHlb4tqyqCSQmO= M1e4Rolv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> M{XUd|I1PDJ|NkGz
BV-173 MmHLSpVv[3Srb36gRZN{[Xl? NILocHgzPTBxNUCwcm0> NWfub2l1PDhiaB?= MkDWxsBRSlN? MmewbY5lfWOnczDk[YxigWWmIHHu[EB{fXO2YXnu[YQhWk:VIHnuZ5Jm[XOn MXWyOFQzOzZzMx?=
CEM MYjGeY5kfGmxbjDBd5NigQ>? NFftb|AzPTBxNUCwcm0> MkTlOFghcA>? MlPyxsBRSlN? MnPjbY5lfWOnczDk[YxigWWmIHHu[EB{fXO2YXnu[YQhWk:VIHnuZ5Jm[XOn M3HJUFI1PDJ|NkGz
HL-60 MWfGeY5kfGmxbjDBd5NigQ>? M4KwdFI2OC93MEDuUS=> MXO0PEBp MUlCpHBDWw>? Mnz3bY5lfWOnczDk[YxigWWmIHHu[EB{fXO2YXnu[YQhWk:VIHnuZ5Jm[XOn MkHDNlQ1OjN4MUO=
ML-1 M3[xOWZ2dmO2aX;uJGF{e2G7 MWOyOVAwPTBybl2= M33RdFQ5KGh? MnvsxsBRSlN? MlTMbY5lfWOnczDk[YxigWWmIHHu[EB{fXO2YXnu[YQhWk:VIHnuZ5Jm[XOn M1qydlI1PDJ|NkGz
DLD-1 MnjqSpVv[3Srb36gRZN{[Xl? NHTyclkzPTBxNUCwcm0> Mlz1OFghcA>? MmDpxsBRSlN? M4fQTIRwKG6xdDDpcoR2[2W|IHTlcIF6\WRiYX7kJJN2e3SjaX7l[EBTV1NiaX7jdoVie2V? MW[yOFQzOzZzMx?=
HCT-116 MXLGeY5kfGmxbjDBd5NigQ>? NV;HTpg1OjVyL{WwNI5O MVO0PEBp NUnRXmxQyqCSQmO= MXPkc{Bvd3RiaX7keYNmeyCmZXzhfYVlKGGwZDDzeZN1[WmwZXSgVm9UKGmwY4LlZZNm MYmyOFQzOzZzMx?=
U937-A/E-9/14/18  M4Xq[GFxd3C2b4Ppd{BCe3OjeR?= NIHwVlYxNjBzL{CuNU8yNzFyIN88US=> NVrPeYs1PDhiaB?= NXuyOphlcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NGXlN|UzPDNyMES1Oi=>
HT29 MoPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnizO|IhcA>? MVzJR|UxRTF2MEFCtVE4QSEQvF2= NHvnd4IzPDF5MkC2NS=>
SW48 MlzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e0ZlczKGh? NH\tRXRKSzVyPUG1MlLDuTZwMjFOwG0> NIjGSIszPDF5MkC2NS=>
HCT116 NY\Xc|A{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXq3NkBp NWDJXZZJUUN3ME2xMlfDuTBwNDFOwG0> NWHmSG9MOjRzN{KwOlE>
HepG2 M2j4[WZ2dmO2aX;uJGF{e2G7 NGPTUXUxNjVxMTFOwG0> NIqwT|gzPCCq NYTSSJRsTE2VTx?= NIriU2Z2eC2{ZXf1cIF1\WRidHjlJJJmdGG2aY\lJG9EXE5{IH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= NIG5NIczPDF2Nki3OC=>
LS174T NUGz[nl5TnWwY4Tpc44hSXO|YYm= MUSwMlUwOSEQvF2= NFftVnUzPCCq NE[wdGNFVVOR NWHZTZg5dGWjZDD0c{BidiCrbnPy[YF{\SCxZjDPR3RPOiCuZY\lcJM> NYTxN2c6OjRzNE[4O|Q>
HepG2 NFXLboVCeG:ydH;zbZMhSXO|YYm= NXi4bFlWOS9zMD:xNFAh|ryP NVPhZWdlPyCm NYXMXlN1TE2VTx?= NYC0WpNQcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NGrubYozPDF2Nki3OC=>
LS174T NXS4U4hiSXCxcITvd4l{KEG|c3H5 NUfCfI9UOS9zMD:xNFAh|ryP NYXJW4dtPyCm NWXPTVNQTE2VTx?= NV:1[5pVcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MVKyOFE1Pjh5NB?=
QBC-939 MUfBdI9xfG:|aYOgRZN{[Xl? MnnuNU8yOC9zMECg{txO MnXOO{Bl MXPEUXNQ NE\vU3NqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NEXrb5EzPDF2Nki3OC=>
U251 NGjxcFVCeG:ydH;zbZMhSXO|YYm= MVKxM|ExNzFyMDFOwG0> MVG3JIQ> NIfXRnRFVVOR NIDjN|dqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MXSyOFE1Pjh5NB?=
HL-60 NYXLb4s6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrrRnMyKM7:TR?= M3;JdlQ5KGh? M1jXT4lv[3KnYYPld{BIOi2yaHHz[UBk\WyuIH\yZYN1cW:w M13wd|I1ODByM{K0
MDA‑MB‑453 NHLGbnVHfW6ldHnvckBCe3OjeR?= NYT6PYF1OC5{L{Gg{txO NWfMNllKPzJiaB?= M{X1ZYNifXOnczDy[U1mgHC{ZYPzbY9vKG:oIHPsZZVlcW8EoEJCpC=> NYPGfVF6OjN6NESyNlg>
HCC1569 M36yNWZ2dmO2aX;uJGF{e2G7 MkH2NE4zNzFizszN MV63NkBp M2HMTYNifXOnczDy[U1mgHC{ZYPzbY9vKG:oIHPsZZVlcW8EoEJCpC=> MmTtNlM5PDR{Mki=
BT‑474 NIrUTJhHfW6ldHnvckBCe3OjeR?= M2L1PVAvOi9zIN88US=> NGDVflk4OiCq NIDkSVdk[XW|ZYOgdoUu\XiycnXzd4lwdiCxZjDjcIF2\GmwwrCxxsA> NELqPJczOzh2NEKyPC=>
AGS M{jmOGFxd3C2b4Ppd{BCe3OjeR?= NVPFV|R4PS9zMD:yNE82OCEQvF2= MVy0POKhcMLi M4HNcmROW09? NXLye3pocW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6yqB? NUnWN|BrOjN3OEK3PFQ>
A549 NInBT29CeG:ydH;zbZMhSXO|YYm= NF3zRmM2NzFyL{KwM|UxKM7:TR?= NF3iWGc1QMLiaNMg Mkn2SG1UVw>? NGnkcZJqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJnDqA>? M{fhfVI{PTh{N{i0
AGS  NVXrZnl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;vSVUwOTBxMkCvOVAh|ryP NI\jRlY1QMLiaNMg NFG5T5BFVVOR M37DRolv\HWlZYOgS|IwVSCyaHHz[UBienKnc4VCpC=> MmLkNlM2QDJ5OES=
Kasumi-1 MmnPRZBweHSxc3nzJGF{e2G7 Moe4NE42KM7:TR?= M{LIPVQ5yqCqwrC= NUew[XVH\GWlcnXhd4V{KHSqZTDj[YxtKH[rYXLpcIl1gSClbz30doVifGWmIIfpeIghXGZvTmCtd4M> Moi2NlM1QTN|NEi=
OCI-AML3 M1jkW2Fxd3C2b4Ppd{BCe3OjeR?= M{HxbFIvPSEQvF2= M1PqN|Q5yqCqwrC= MkDG[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBkdy22cnXheIVlKHerdHigWIYuVlBvc3O= MVyyN|Q6OzN2OB?=
MV4-11 MkXERZBweHSxc3nzJGF{e2G7 NWjsPXdTOi53IN88US=> MXy0POKhcMLi MmXw[IVkemWjc3XzJJRp\SClZXzsJJZq[WKrbHn0fUBkdy22cnXheIVlKHerdHigWIYuVlBvc3O= MkTlNlM1QTN|NEi=
NK  MUfDfZRwfG:6aYT5JGF{e2G7 M1LSR|AvODJvMkCg{txO MWm1JIQ> MVLk[YNz\WG|ZYOgeIhmKGO7dH;sfZRq[yCjY4Tpeol1gSCxZjDOT{Bk\WyuczDheEBqdnSncn3l[IlifGViY3;uZ4VvfHKjdHnvcpMhemW|dXz0bY5oKGmwIHGgWU1{cGGyZXSg[I9{\eLCk4Lld5BwdnOnIHP1dpZm NHfyN4wzOzN{OEC4PC=>
NK  NFftOoFCeG:ydH;zbZMhSXO|YYm= M17NbFAvODJvMkCg{txO MWi1JIQ> M1u2W4Rm[3KnYYPlJG5MKGOnbHygdJJwdGmoZYLheIlwdiCjbnSgeoli[mmuaYT5JIF{KHSqZTDjc45k\W62cnH0bY9vKGmwY4LlZZNm\A>? NGDNR4szOzN{OEC4PC=>
NK  M{nofmZ2dmO2aX;uJGF{e2G7 NHe0doQxNjBzLUKwJO69VQ>? MVy1JIQ> M1rvS4NifXOnczDofZBwdWW2aInsZZRqd25ib3[gUmsh[2WubIOgbY4h[SCmb4Pl5qCUemW|cH;ud4U> MmP4NlM{OjhyOEi=
MOLT4/DNR MXjGeY5kfGmxbjDBd5NigQ>? MV[1JO69VQ>? MnXvOEBl M13lN5Jm\HWlZYOgRWJESjFibWLORUBmgHC{ZYPzbY9v NG\0fGszOzB4MEW3NC=>
Jurkat/DOX NE\WboNHfW6ldHnvckBCe3OjeR?= M{S3S|Uh|ryP NGfXeVQ1KGR? M33TbpJm\HWlZYOgRWJESjFibWLORUBmgHC{ZYPzbY9v NHXPXpUzOzB4MEW3NC=>
MOLT4/DNR NGnIclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[0OUDPxE1? NWnx[YVnPCCm MonzdoVlfWOnczD0bIUhUUN3MNMgeoFtfWViZn;yJIRifW6xcoXibYNqdiC|ZX7zbZRqfmm2eR?= M2D4TlI{ODZyNUew
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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 3年-20℃
2年-80℃in solvent
別名 Deoxycytidine
溶解度 (25°C) * In vitro DMSO 45 mg/mL (197.18 mM)
Water 10 mg/mL (43.81 mM)
Ethanol <1 mg/mL
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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