Nutlin-3

Nutlin-3は、強力で選択的なMDM-2拮抗剤で、IC50 が 90 nMです。Mdm2は、それ自体とp53のためのRING指依存的なユビキチン・タンパク質リガーゼです。

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Nutlin-3 化学構造
分子量: 581.5

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Quality Control & MSDS

製品説明

  • Compare Mdm2 Inhibitors
    Mdm2製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 Nutlin-3は、強力で選択的なMDM-2拮抗剤で、IC50 が 90 nMです。Mdm2は、それ自体とp53のためのRING指依存的なユビキチン・タンパク質リガーゼです。
ターゲット Mdm2
IC50 90 nM [1]
In vitro試験 Nutlin-3 potently inhibits the MDM2-p53 interaction, leading to the activation of the p53 pathway. Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM, only in cells with wild-type p53 such as HCT116, RKO and SJSA-1, but not in the mutant p53 cell lines SW480 and MDA-MB-435. In SJSA-1 cells, Nutlin-3 treatment at 10 μM for 48 hours significantly induces caspase-dependent cell apoptosis by ~45%. Although Nutlin-3 also inhibits the growth and viability of human skin (1043SK) and mouse embryo (NIH/3T3) with IC50 of 2.2 μM and 1.3 μM, respectively, cells remain viable 1 week post-treatment even at 10 μM of Nutlin-3, in contrast with the SJSA-1 cells with viability lost at 3 μM of Nutlin-3 treatment. [1] Nutlin-3 does not induce the phosphorylation of p53 on key serine residues and reveals no difference in their sequence-specific DNA binding and ability to transactivate p53 target genes compared with phosphorylated p53 induced by the genotoxic drugs doxorubicin and etoposide, demonstrating that phosphorylation of p53 on key serines is dispensable for transcriptional activation and apoptosis. [2] Although binding less efficiently to MDMX than to MDM2, Nutlin-3 can block the MDMX–p53 interaction and induce the p53 pathway in retinoblastoma cells (Weri1) with IC50 of 0.7 μM. [3] Nutlin-3 at 30 μM also disrupts endogenous p73-HDM2 interaction and enhances the stability and proapoptotic activities of p73, leading to the dose-dependent cell growth inhibition and apoptosis induction in cells without wild-type p53. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MCF7 NITie2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrTNlV5PcLizszN NXvoWItxPDkEoHi= NWPWd4F1[myxY3vzJFI4NU:KQz3pcoR2[2WmIHPlcIwheHKxbHnm[ZJifGmxbjDjc41x[XKjYnzlJJRwKHSqYYSgc4Yh[mG|YXygcIV3\Wy| NUPTOJd5OjZ|NUC1OlU>
NP69 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjK[lBEUUN3ME2zNU43QcLzMj61OEDPxE1? M4nPWlI3OjV{NUe1
NP460 NWrZOmcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzyTWM2OD1{Mj64OeKyOS5zODFOwG0> M3:wS|I3OjV{NUe1
C666-1 NUjmbHkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfPNIlKSzVyPUG5Mlk2yrF6LkmzJO69VQ>? Ml:0NlYzPTJ3N{W=
C666-1 M1LHcWNmdGxiVnnhZoltcXS7IFHzd4F6 MXexNEDDvU1? MoXNOFghcA>? MVTEUXNQ MXPz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzD0bIUh[3m2b4TvfIlkKGWoZnXjeEBw\iClaYPwcIF1cW5? NVvMZlN2OjZ{NUK1O|U>
C666-1  MmH4SpVv[3Srb36gRZN{[Xl? MUSxNEDDvU1? MVSyOEBp NWnsVVF1TE2VTx?= NFjRZ|Zi[3SrdnH0[ZMhfGinIIC1N{Bx[XSqd3H5MEB2eHKnZ4XsZZRqdmdicEWzMEBxOjFiYX7kJG1ldTJ? Mn3VNlYzPTJ3N{W=
C666-1 M1fNZ2Fxd3C2b4Ppd{BCe3OjeR?= MWSxNEDDvU1? NIq4OYU1QC95MjDo NWLQNI9DTE2VTx?= MX;z[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzDjbZNxdGG2aX6tbY5lfWOnZDDhdI9xfG:|aYO= MYSyOlI2OjV5NR?=
A549 M3Sydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr3UZNZOjRiaB?= MVTJR|UxRTF5Lk[4JOKyKDRwNUKg{txO MmfVNlYyOjV{M{C=
A549-NTC MnjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDGNlQhcA>? MULJR|UxRTF7LkSyJOKyKDFwOU[g{txO MnriNlYyOjV{M{C=
A549-920 MoX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzkU3FqOjRiaB?= NHzxdlFKSzVyPUOzMlg2KMLzIESuPFQh|ryP MX[yOlEzPTJ|MB?=
CRL-5908 NXvTTYZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrzNlQhcA>? MkHMTWM2OD1|OD63NUDDuSB{LkSzJO69VQ>? M{nwWFI3OTJ3MkOw
L6 M4XGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuxNOKh|ryPwrC= M1XoSFI1NzR6L{eyJIg> NWrOU3Q4TE2VTx?= M4eyOIlvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? MXyyOVg4OTd7NB?=
C2C12 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M333O|ExyqEQvF5CpC=> M1z4WVI1NzR6L{eyJIg> NFLGb|lFVVOR MXzpcohq[mm2czDj[YxteyCycn;sbYZmemG2aX;uJIFv\CCmaX\m[ZJmdnSrYYTpc44> NVz1eok5OjV6N{G3PVQ>
MCF-7  NITBOoRHfW6ldHnvckBCe3OjeR?= NHG5cGUyOMLizszN Ml;SSG1UVw>? NVLFZopKcW6qaXLpeJMh[3mlbHnuJGQyKGGwZDDEbYNmesLi NV7tZppVOjV5MEK3NFM>
DU4475  MnrHSpVv[3Srb36gRZN{[Xl? NGPaelU2NzFyL{KwJO69VQ>? M1P6bVI1yqCq NFLTRXdld3ewcnXneYxifGW|IGTvZ4EuOSCmb4PlJIRmeGWwZHXueIx6 MnXMNlU2PDdzN{S=
SMMC-7721 NEHpTGlHfW6ldHnvckBCe3OjeR?= M3rvOFExKM7:TR?= Mlm5OFghcA>? MXvEUXNQ MUnjZZV{\XNiRF7BJGRUSiCmYX3h[4U> NYXGXWptOjV3NESzOlE>
SMMC-7721 MULGeY5kfGmxbjDBd5NigQ>? NVzwS3ZKOTBizszN M4PDd|Q5KGh? MoLMSG1UVw>? NYLpe|d5cW6mdXPld{B1cGViY3jyc41ifGmwLXLveY5lKHC{b4TlbY4hUU[LMU[geI8heGG{dHnhcIx6KGyxY3HsbZpmKGmwIITo[UBkgXSxcHzhd43DqA>? Mn\SNlU2PDR|NkG=
SMMC-7721 MmPPSpVv[3Srb36gRZN{[Xl? M1nWPFExKM7:TR?= MlLOOFghcA>? M2PTT2ROW09? NGq1VXRqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3dCpGlHVkJzwrDtVm5C M2LpT|I2PTR2M{[x
SMMC-7721 M4DZSmZ2dmO2aX;uJGF{e2G7 MVmxNEDPxE1? NIjoSYI{PiCq M2G5PGROW09? MlzvZ4F2e2W|IITo[UBm[3SxcHnjJIV5eHKnc4Ppc44hd2ZiSV\JNVY> NYjXcVJ4OjV3NESzOlE>
MCF-7 NFXMTJBHfW6ldHnvckBCe3OjeR?= M1z5ZVExyqEQvF2= M4ThXlAuOjRiaB?= M3rLNIlv\HWlZYOgdFU{KGGwZDDwNlEwS2myMR?= NV\zPIFVOjV2OEKzO|M>
OVCAR10 NXy1XVJiTnWwY4Tpc44hSXO|YYm= MVSxNOKh|ryP Mkf0NlFpyqB? Ml;kSG1UVw>? M3LTXolv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> NIG3cnkzPTR{NkW0PC=>
NCI-H23 NWG3cYFHTnWwY4Tpc44hSXO|YYm= NV;mT49oOTEEoN88US=> NGDrS|MzOWkEoB?= M1;YPGROW09? MnXvbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> M1jlN|I2PDJ4NUS4
A2780 NEfaO|NHfW6ldHnvckBCe3OjeR?= NF7TT28yOMLizszN NEXmOoszOWkEoB?= M3rES2ROW09? MoHZbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> MojoNlU1OjZ3NEi=
NCI-H23 NHrQPXlHfW6ldHnvckBCe3OjeR?= M3fieVExyqEQvF2= M{K1RVIycMLi M1e3cWROW09? MoTv[IVkemWjc3XzJJRp\SCIb4jNNUBt\X[nbIO= M{D4bVI2PDJ4NUS4
A2780 MVnGeY5kfGmxbjDBd5NigQ>? NFPTVJIyOMLizszN NXq4bWFROjGqwrC= MUDEUXNQ MX\k[YNz\WG|ZYOgeIhmKE[xeF2xJIxmfmWucx?= MnGzNlU1OjZ3NEi=
HCT116  M3v1dGZ2dmO2aX;uJGF{e2G7 NFzmfWIyOCEEtV2= NFjpPJkzPCCq NXfFRmtI[2G3c3XzJIEheDV|LXTldIVv\GWwdDD0[ZRz[XCub3nkJGcyNWG{cnXzeEBqdiCmaYDsc4llKEiFVEGxOkBkdG:wZYOgSFMh[W6mIFS4 NHjYSlAzPTN6MEC1OS=>
MCF-10CA1a Mn\hSpVv[3Srb36gRZN{[Xl? MoDGNVDDqM7:TR?= M2TOS|Q5KGh? MmXQSG1UVw>? NXrFe21scW6qaXLpeJMh[mG|YXygbY53[XOrb36gZY5lKHKnZIXj[YQhXEeILd8yN{1qdmS3Y3XkJIlvfmG|aX;uJJRwKGKjc3HsJIxmfmWucx?= NITlS3czPTJ3N{eyPS=>
MCF-10A1  M2DJPGZ2dmO2aX;uJGF{e2G7 M2L0V|ExyqEQvF2= MWCyOE81QCCq NYe4TmZVTE2VTx?= MknJbY5pcWKrdIOgcYloemG2aX;uJI9nKG6xcn3hcEBjemWjc4Sg[ZBqfGinbHnhcOKh NXKyfYdtOjV{NUe3Nlk>
MCF-10CA1a NX:zWnlnTnWwY4Tpc44hSXO|YYm= MkLINVDDqM7:TR?= MkPnNlQhcA>? NHXZNmRFVVOR MkfT[IVkemWjc3XzJJRp\SCWR1[t{tI{NWmwZIXj[YQhdVKQQTDs[ZZmdHNib3\NUXAzNMLiTV3QPUwh[W6mwrDpcpRm\3KrbtMg{tLDqDN? NInwZpkzPTJ3N{eyPS=>
MCF-10CA1a NF[wbnRHfW6ldHnvckBCe3OjeR?= MWCxNOKh|ryP M1zie|I1KGh? NYnMRmpXTE2VTx?= MVjpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? NEDjb4YzPTJ3N{eyPS=>
SK-BR-7 NIX1NlVHfW6ldHnvckBCe3OjeR?= NHf6TlIyOMLizszN NFq4UHUzPCCq NGPBWYVFVVOR MVnpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? NIruZogzPTJ3N{eyPS=>
SUM102PT NWDJRodqTnWwY4Tpc44hSXO|YYm= MmHGNVDDqM7:TR?= M3Hu[FI1KGh? NFnobYRFVVOR MX3pcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? MnPONlUzPTd5Mkm=
RAW 264.7 Mo\TSpVv[3Srb36gRZN{[Xl? NX7OSYo1OTEEoN88US=> MYKzNEBucW5? NXnSXXVxeHKndnXueJMhfGinIIC1N{Bz\WS3Y4Tpc44hcW5icnXzdI9ve2VidH:gUHBU M1zaclI2OTd{NUS3
RAW 264.7 M{\ZdWZ2dmO2aX;uJGF{e2G7 MYqxNOKh|ryP NVHlU5pbOzBibXnu MmXsdoVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= NGT0W3czPTF5MkW0Oy=>
RAW 264.7 NHvybYZHfW6ldHnvckBCe3OjeR?= M13oeFExyqEQvF2= MYezNEBucW5? MXrpcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= MmTLNlUyPzJ3NEe=
MCF7  MVLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWXrVYZUOi53INM1US=> M2LvPVUh\A>? MmnUSG1UVw>? MlXRd4Vve2m2aYrld{BOS0Z5IITvJHBCWlBiaX7obYJqfGmxbh?= MYOyOVA5PTlyMh?=
MCF7  MkfmSpVv[3Srb36gRZN{[Xl? NEO3cVUzNjViwsXN Mn7NOFghcA>? Mlr5SG1UVw>? MnLw[IVkemWjc3XzJJRp\SCqb33vcI9od3W|IFTTRkBz\XCjaYKg[pJmeXWnbnPp[ZM> NVzTZlFSOjVyOEW5NFI>
ACHN MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnLjNE42NTFyIN88US=> NUHYSYJnOC14IHS= Ml3lSG1UVw>? NV3BcGdRcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MY[yOVA3Pzd6Nx?=
Caki-2 NX;RT4tNS2WubDDWbYFjcWyrdImgRZN{[Xl? M3j2TlAvPS1zMDFOwG0> MWewMVYh\A>? MWLEUXNQ MXrpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3GyfFI2ODZ5N{i3
A498 NYizZpFSS2WubDDWbYFjcWyrdImgRZN{[Xl? NHTP[YUxNjVvMUCg{txO M3fKVVAuPiCm MYDEUXNQ MmLubY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHTMWokzPTB4N{e4Oy=>
115 MoCyR4VtdCCYaXHibYxqfHliQYPzZZk> MVywMlUuOTBizszN NV\sdG5iOC14IHS= NFrwPWVFVVOR MVTpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXjofJBnOjVyNke3PFc>
117 NXjlcFRtS2WubDDWbYFjcWyrdImgRZN{[Xl? M4r0clAvPS1zMDFOwG0> MmntNE03KGR? NHvvcFZFVVOR MXvpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIj0epIzPTB4N{e4Oy=>
ACHN Mn;YSpVv[3Srb36gRZN{[Xl? MmHONE42NzFxNTFOwG0> NUnhSZhvPDhiaB?= MmLTSG1UVw>? NWPsO4VydGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= MXqyOVA3Pzd6Nx?=
Caki-2 M1[2d2Z2dmO2aX;uJGF{e2G7 M4fwW|AvPS9zL{Wg{txO M1L2cVQ5KGh? MULEUXNQ MXzs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NVj2bpVIOjVyNke3PFc>
A498 NVv5Zo1HTnWwY4Tpc44hSXO|YYm= NH7YPIMxNjVxMT:1JO69VQ>? NUXrOopsPDhiaB?= Mm\2SG1UVw>? MXLs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NIrkO44zPTB4N{e4Oy=>
115 NIrKXGhHfW6ldHnvckBCe3OjeR?= NU\BcXJTOC53L{GvOUDPxE1? NIS5WWU1QCCq M4\ETGROW09? M1:5dIxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz NYXjS2ZFOjVyNke3PFc>
ACHN M3fYXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7McJBxPSEQvF2= M1fjOVQ5KGh? MnH5SG1UVw>? NGPZZpBqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NHT0N2QzPTB4N{e4Oy=>
Caki-2 NXG3dYlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvWbmx{PSEQvF2= MlWxOFghcA>? M{DCSWROW09? MXrpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NITXNoszPTB4N{e4Oy=>
A498 NGrtbY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfQSoE2KM7:TR?= NVm2UlFnPDhiaB?= M4HKdGROW09? M1XIbYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NYXodpZiOjVyNke3PFc>
115 M2DsXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWG1JO69VQ>? NXPBOHgyPDhiaB?= NIDjdIRFVVOR NEf1N25qdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> M{\MOVI2ODZ5N{i3
ACHN M4X6dmZ2dmO2aX;uJGF{e2G7 MmTiOUDPxE1? MUW0PEBp M1\FZmROW09? MnfkbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NEHXNY0zPTB4N{e4Oy=>
Caki-2 NGfZTGJHfW6ldHnvckBCe3OjeR?= MnH2OUDPxE1? NE[0S2E1QCCq MV\EUXNQ MVHpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NWnmTXBOOjVyNke3PFc>
A498 M1XmcGZ2dmO2aX;uJGF{e2G7 M4DnPFUh|ryP NFLxT|Q1QCCq MXHEUXNQ NWHYNWpNcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> M2TvVFI2ODZ5N{i3
115 MVvGeY5kfGmxbjDBd5NigQ>? MWK1JO69VQ>? MlqxOFghcA>? M3n4VmROW09? M1;lSYlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= NX[z[JVNOjVyNke3PFc>
MOLM-13 MlzQSpVv[3Srb36gRZN{[Xl? M4K0[FbDqM7:TR?= NVTIT4xOOC16IHi= NUnNXGpuTE2VTx?= Mn3IbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZicEWzMEBOTE1{LDDwNlEh[W6mIHHj[ZR6dGG2ZXSgdFU{ MYqyOFg5PTB6Mh?=
MOLM-13 MXzGeY5kfGmxbjDBd5NigQ>? NUL1fJVoPsLizszN MV22JIg> NHPL[GpFVVOR M{DtPIVvcGGwY3XzJJRp\SCjY3X0fYxifGmxbjDv[kBpcXO2b37lJGgzSiCjbnSgbIVifCC|aH;jb{Bxem:2ZXnud{BJe3B{NzDhcoQhUHOyOUC= NIjtZ2kzPDh6NUC4Ni=>
HepG2 M2fPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M361WlczKGh? NUS3NppXTE2VTx?= NF3pVmNKSzVyPUO1Mlg3KMLzIEKuPUDPxE1? M{PPblI1QDh2OEC5
HepG2/As M2Hvdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLXO|IhcA>? M3jOUGROW09? M4XucWlEPTB;NkiuNVMhyrFiOT62JO69VQ>? Ml6zNlQ5QDR6MEm=
SMMC7721 M2\HNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:3NkBp M{PJcWROW09? Mm\BTWM2OD1|MT6yPEDDuSB2LkKg{txO NXT1Umx5OjR6OES4NFk>
SMMC7721/Ac MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nwUlczKGh? Mme2SG1UVw>? MVzJR|UxRTV3LkKxJOKyKDVwMEOg{txO MXKyOFg5PDhyOR?=
Huh-7 NWfpN20{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLGO|IhcA>? MmPWSG1UVw>? MlzTTWM2OD1|Mz65OkDDuSB|Lkmg{txO NIHFcJkzPDh6NEiwPS=>
Hep3B MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXyZok4OiCq NEXZXmxFVVOR NGHteWFKSzVyPUKwMlE5KMLzIEGuPFQh|ryP NV\GXZI3OjR6OES4NFk>
HepG2 NHfq[odCeG:ydH;zbZMhSXO|YYm= Mn7zbY5lfWOnczDhdI9xfG:|aYO= NUi4TJpiOjR6OES4NFk>
SMMC7721 MV;BdI9xfG:|aYOgRZN{[Xl? MVTpcoR2[2W|IHHwc5B1d3Orcx?= NUn6e|I1OjR6OES4NFk>
Huh-7 MkDoRZBweHSxc3nzJGF{e2G7 MVvpcoR2[2W|IHHwc5B1d3Orcx?= NVm1PI92OjR6OES4NFk>
Hep3B NIPvOoZCeG:ydH;zbZMhSXO|YYm= MoDGbY5lfWOnczDhdI9xfG:|aYO= MWmyOFg5PDhyOR?=
U2OS  M3zVZmZ2dmO2aX;uJGF{e2G7 NI\YPFgzOCEQvF2= Mn;YNlQhcA>? MVLpcoNz\WG|ZYOgeIhmKG2UTlGgcIV3\Wy|IH;mxsBDS0x{QUGsJGJEVFiOwrDhcoRDS0yZ NHWwVJgzPDh4N{K1PS=>
AML2 NYrpRYVySXCxcITvd4l{KEG|c3H5 NF\M[nUzNzFyIN88US=> MYqyOE81QCCq MkDybY5lfWOnczDhdI9xfG:|aYO= Mn\oNlQ3PTl5NEm=
MOML13 MnvMRZBweHSxc3nzJGF{e2G7 NH3KWZEzNzFyIN88US=> NH\kV4UzPC92ODDo NXftRYZxcW6mdXPld{BieG:ydH;zbZM> NWrPSmlPOjR4NUm3OFk>
AML2 NHP5Z3ZHfW6ldHnvckBCe3OjeR?= NF7rWJcyOM7:TR?= NVH6WIhvOi92IHi= MWjpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= MVyyOFY2QTd2OR?=
AML3 MmnPSpVv[3Srb36gRZN{[Xl? NXXteG9POTEQvF2= NH7Cc4szNzRiaB?= NIXvOG5qdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NIHCdHYzPDZ3OUe0PS=>
MOML13 NF;heJdHfW6ldHnvckBCe3OjeR?= M1PPUVEx|ryP NF3ZWWgzNzRiaB?= M13yNYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NY\GfJcyOjR4NUm3OFk>
BeWo M2X5eGZ2dmO2aX;uJGF{e2G7 NUjxd5lxOzBiwsXN MmfZNlQhcA>? MVvpcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= MkPhNlQ1QThzNUS=
BeWo NHnnbo1CeG:ydH;zbZMhSXO|YYm= NYnRWZdnOzBiwsXN MnX1NlQhcA>? M3ToTolv[3KnYYPld{BieG:ydH;zbZM> MmPUNlQ1QThzNUS=
OCI MV;GeY5kfGmxbjDBd5NigQ>? MkWxNVAh|ryP MlfGNlQhcA>? NGnWXlV2eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= MYCyOFQ4OzV4Mh?=
MOLM NHXT[ZlHfW6ldHnvckBCe3OjeR?= NF\rVlEyOCEQvF2= MmDjNlQhcA>? MX;1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? Mo\xNlQ1PzN3NkK=
U2OS  NFTHWZRHfW6ldHnvckBCe3OjeR?= MV[yNEDPxE1? MorzNlQhcA>? NGPNUYNqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw MmDMNlQ{PjZyMEe=
RKO M37WNGZ2dmO2aX;uJGF{e2G7 MnHONlAh|ryP Mn71NlQhcA>? MUXpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv MmCxNlQ{PjZyMEe=
U2OS  M4HFXWZ2dmO2aX;uJGF{e2G7 M1TIZlIxKM7:TR?= NE\ZVHAzPCCq MlrTbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= MWGyOFM3PjByNx?=
RKO MmewSpVv[3Srb36gRZN{[Xl? M1\meFIxKM7:TR?= M37IPFI1KGh? NYLxbopKcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MoPuNlQ{PjZyMEe=
SMMC-7721  MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGC2[5EyNjJ3LUKwJO69VQ>? MXKyOE81QC95MjDo Mkn1SG1UVw>? M4DvR4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MkjENlQzQDZ|MUK=
HuH-7 Mk\qR4VtdCCYaXHibYxqfHliQYPzZZk> NI[wTIwyNjJ3LUKwJO69VQ>? MmW1NlQwPDhxN{KgbC=> NX\ueYlwTE2VTx?= NVTUd|U1cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> M{LkfVI1Ojh4M{Gy
SMMC-7721  MWTBdI9xfG:|aYOgRZN{[Xl? M12zXFIxKM7:TR?= NIfsXXk1QCCq NWW5[nNLTE2VTx?= NFTlSGdqdmS3Y3XzJIFxd3C2b4Ppdy=> NF7aNIwzPDJ6NkOxNi=>
HuH-7 MUHBdI9xfG:|aYOgRZN{[Xl? NGrkfGszOCEQvF2= NEP0epY1QCCq NILmW|BFVVOR MlTUbY5lfWOnczDhdI9xfG:|aYO= MnLuNlQzQDZ|MUK=
SMMC-7721  Mmr3SpVv[3Srb36gRZN{[Xl? NXO2T4lkOTBizszN MlG4N|YhcA>? M2TsSGROW09? NYm4PHN2\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NYHqTVlWOjR{OE[zNVI>
HuH-7 NFzvV5FHfW6ldHnvckBCe3OjeR?= NGHOSpoyOCEQvF2= NUflN4JsOzZiaB?= NUDLc|d{TE2VTx?= NYDvfHQ5\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NEnnRpIzPDJ6NkOxNi=>
AT2 MoXpSpVv[3Srb36gRZN{[Xl? M4DhN|UwOTBizszN M4PzNoxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li NUnURWZMOjR{NECyNFM>
REH MlnPSpVv[3Srb36gRZN{[Xl? MofuOU8yOCEQvF2= NX\ZdmhpdGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NEOwZYszPDJ2MEKwNy=>
UoCB6 M2fwd2Z2dmO2aX;uJGF{e2G7 MnTQOU8yOCEQvF2= M3HBZYxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li NWS0e2V5OjR{NECyNFM>
AT2 NGTJVnlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NEDUOFUxNTJ3IN88US=> M2fUbYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NXTVXnJnOjR{NECyNFM>
REH NEfvNGRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHXGUmIxNTJ3IN88US=> M4n4[YlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M2D1eVI1OjRyMkCz
UoCB6 NFvoR5JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Ml3HNE0zPSEQvF2= MWPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MUSyOFI1ODJyMx?=
A2780 MYXGeY5kfGmxbjDBd5NigQ>? NFP5Om82NzFyL{KwJO69VQ>? MVyyOEBp M2rxNpVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NXS5bnlyOjRzM{[xOFc>
H460 NULuZ4pNTnWwY4Tpc44hSXO|YYm= Mn3iOU8yOC9{MDFOwG0> NVmxdZJEOjRiaB?= MmTXeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? MW[yOFE{PjF2Nx?=
Lovo  NHLyOmRHfW6ldHnvckBCe3OjeR?= NYr6T21sPS9zMD:yNEDPxE1? MUCyOEBp NELqUIx2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= Ml7aNlQyOzZzNEe=
A2780 NFHOWnBCeG:ydH;zbZMhSXO|YYm= Ml\2OU8yOC9{MDFOwG0> MVOyOEBp NHroU|FmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? M1vscFI1OTN4MUS3
H460 NFv1d3RCeG:ydH;zbZMhSXO|YYm= M134b|UwOTBxMkCg{txO NFfiRlQzPCCq NHjET4FmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? MVuyOFE{PjF2Nx?=
Lovo  NEjCfZJCeG:ydH;zbZMhSXO|YYm= Ml7ROU8yOC9{MDFOwG0> MnHQNlQhcA>? MWflcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> MnvONlQyOzZzNEe=

... Click to View More Cell Line Experimental Data

In vivo試験 Oral administration of Nutlin-3 at 200 mg/kg twice daily for 3 weeks significantly inhibits the tumor growth of SJAS-1 xenografts by 90%, comparable with the effect of doxorubicin treatment with 81% inhibition of tumor growth. [1]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Biacore study Competition assay is performed on a Biacore S51. A Series S Sensor chip CM5 is utilized for the immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~200 response units (1 response unit corresponds to 1 pg of protein per mm2). The concentration of MDM2 protein is kept constant at 300 nM. Nutlin-3 is dissolved in DMSO at 10 mM and further diluted to make a concentration series of Nutlin-3 in each MDM2 test sample. The assay is run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of Nutlin-3 is calculated as a percentage of binding in the absence of Nutlin-3 and IC50 is calculate

細胞アッセイ: [1]

細胞株 HCT116, RKO, SJSA-1, SW480, and MDA-MB-435
濃度 Dissolved in DMSO, final concentrations ~ 30 μM
反応時間 8, 24, and 48 hours
実験の流れ Cells are exposed to various concentrations of Nutlin-3 for 8, 24 and 48 hours. The transcriptional levels of p21 and MDM2 genes are analyzed by real-time PCR, and protein levels by western blotting. Cell viability is measured by the MTT assay. Cell apoptosis is determined by terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick end labeling (TUNEL) staining with flow cytometry and fluorescence microscopy.

動物実験: [1]

動物モデル Athymic female nude mice (Nu/Nu-nuBR) injected subcutaneously with SJSA-1 cells
製剤 Formulated in 2% Klucel, 0.5% Tween 80
投薬量 200 mg/kg
投与方法 Orally, twice a day

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 Nutlin-3 SDF
分子量 581.5
化学式

C30H30Cl2N4O4

CAS No. 890090-75-2
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (171.96 mM)
エタノール 30 mg/mL (51.59 mM)
<1 mg/mL (<1 mM)
* <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-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one

文献中の引用 (9)

Frequently Asked Questions

  • Question 1
    Is this a racemic mixture of Nutlin-3a and Nutlin-3b or just the Nutlin-3a enantiomer?

    Answer: It is a racemate.

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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* 必須

Related Mdm2 阻害剤

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    Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor.

  • MI-773 (SAR405838)

    MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

  • A-1210477

    A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.

  • NSC 207895

    NSC 207895が、リポーター・ベースの薬ふるい分けを通してのMDMX抑制器として発見されます。MDMXは、p53とMDM2(E3リガーゼ)を管理します。

  • Nutlin-3a

    Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM.

    Features:Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.

  • Nutlin-3b

    Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

  • YH239-EE

    YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

  • Z-VAD-FMK

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    Features:A key compound for apoptosis studies.

  • ABT-263 (Navitoclax)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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