Nutlin-3

Nutlin-3は一種の有効で、選択性的なMdm2 (自身とp53に対するRING finger-dependent ubiquitin protein ligase) 拮抗剤で、無細胞試験でIC50値が90 nMですが、p53欠陥細胞中のp73を安定させられます。

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Nutlin-3 化学構造
分子量: 581.5

高品質保証

カスタマーフィードバック(3)

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は一種の有効で、選択性的なMdm2 (自身とp53に対するRING finger-dependent ubiquitin protein ligase) 拮抗剤で、無細胞試験でIC50値が90 nMですが、p53欠陥細胞中のp73を安定させられます。
ターゲット

Mdm2

IC50

180 nM [5]

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 NF3wRnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXHeVJQPcLizszN NVqxPWcxPDkEoHi= MnPRZoxw[2u|IEK3MW9JSy2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiClb33wZZJi[mynIITvJJRp[XRib3[gZoF{[WxibHX2[Yx{ NFnHRoozPjN3MEW2OS=>
NP69 Mn7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXmTWM2OD1|MT62PeKyOi53NDFOwG0> M3fJXVI3OjV{NUe1
NP460 M{HZemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjFSXh4UUN3ME2yNk45PcLzMT6xPEDPxE1? NEjVVGQzPjJ3MkW3OS=>
C666-1 M4G0fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTF7Lkm1xtE5Njl|IN88US=> MnTMNlYzPTJ3N{W=
C666-1 M{fofGNmdGxiVnnhZoltcXS7IFHzd4F6 MVKxNEDDvU1? NW\E[JZ7PDhiaB?= M3TUNmROW09? Mn3nd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:geIhmKGO7dH;0c5hq[yCnZn\lZ5Qhd2ZiY3nzdIxifGmw NGjm[pIzPjJ3MkW3OS=>
C666-1  MWnGeY5kfGmxbjDBd5NigQ>? MX:xNEDDvU1? M2[xOlI1KGh? M3jOT2ROW09? NG[zN2di[3SrdnH0[ZMhfGinIIC1N{Bx[XSqd3H5MEB2eHKnZ4XsZZRqdmdicEWzMEBxOjFiYX7kJG1ldTJ? MXKyOlI2OjV5NR?=
C666-1 MVHBdI9xfG:|aYOgRZN{[Xl? M37vc|ExKML3TR?= NVPrXoxIPDhxN{KgbC=> NEnTdHZFVVOR MVrz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzDjbZNxdGG2aX6tbY5lfWOnZDDhdI9xfG:|aYO= MmfXNlYzPTJ3N{W=
A549 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXyyOEBp NIe1XlZKSzVyPUG3MlY5KMLzIESuOVIh|ryP NW[2N3N3OjZzMkWyN|A>
A549-NTC NILWTnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvxNlQhcA>? NV3hUYxXUUN3ME2xPU41OiEEsTCxMlk3KM7:TR?= NW\GZWlwOjZzMkWyN|A>
A549-920 NYfpRWJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rldFI1KGh? NHLzTXZKSzVyPUOzMlg2KMLzIESuPFQh|ryP NXvRZot5OjZzMkWyN|A>
CRL-5908 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moe4NlQhcA>? M4LFZ2lEPTB;M{iuO|EhyrFiMj60N{DPxE1? M{S2d|I3OTJ3MkOw
L6 MmPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfwZYwyOMLizszNxsA> NILXV3AzPC92OD:3NkBp MXXEUXNQ M{nIVolvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? NH\md|czPTh5MUe5OC=>
C2C12 NXHMTWJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVyxNOKh|ryPwrC= M2mweVI1NzR6L{eyJIg> M2f4d2ROW09? NU\wPZcxcW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w NY\jTGtlOjV6N{G3PVQ>
MCF-7  NWCwUlhITnWwY4Tpc44hSXO|YYm= MmLGNVDDqM7:TR?= NFXpbFlFVVOR NIjQb4xqdmirYnn0d{BkgWOuaX6gSFEh[W6mIFTpZ4VzyqB? NGOzPJIzPTdyMkewNy=>
DU4475  M3TjdWZ2dmO2aX;uJGF{e2G7 NF\xd2g2NzFyL{KwJO69VQ>? NXeze3FvOjUEoHi= MUXkc5dvemWpdXzheIV{KFSxY3GtNUBld3OnIHTldIVv\GWwdHz5 M1vQU|I2PTR5MUe0
SMMC-7721 MmHySpVv[3Srb36gRZN{[Xl? NYfvUY9vOTBizszN MXy0PEBp MVjEUXNQ M4HqfoNifXOnczDEUmEhTFOEIHThcYFo\Q>? MoTCNlU2PDR|NkG=
SMMC-7721 M4\RVmZ2dmO2aX;uJGF{e2G7 M{TPPFExKM7:TR?= M1v4cVQ5KGh? MYTEUXNQ NUWyT2Q5cW6mdXPld{B1cGViY3jyc41ifGmwLXLveY5lKHC{b4TlbY4hUU[LMU[geI8heGG{dHnhcIx6KGyxY3HsbZpmKGmwIITo[UBkgXSxcHzhd43DqA>? NXHhdpRtOjV3NESzOlE>
SMMC-7721 NH7oOlhHfW6ldHnvckBCe3OjeR?= NYWwfJc6OTBizszN NYfNdVI1PDhiaB?= NG[0SlZFVVOR NE\zTJhqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3dCpGlHVkJzwrDtVm5C M1jZVVI2PTR2M{[x
SMMC-7721 NYPoV|JGTnWwY4Tpc44hSXO|YYm= NV\6[YlOOTBizszN Mn3XN|YhcA>? MnfRSG1UVw>? MnfJZ4F2e2W|IITo[UBm[3SxcHnjJIV5eHKnc4Ppc44hd2ZiSV\JNVY> NUPhNHE5OjV3NESzOlE>
MCF-7 MXXGeY5kfGmxbjDBd5NigQ>? MXuxNOKh|ryP NF\PS3kxNTJ2IHi= Mm\obY5lfWOnczDwOVMh[W6mIICyNU9EcXBz M17FO|I2PDh{M{ez
OVCAR10 MoDKSpVv[3Srb36gRZN{[Xl? NVnLVHVlOTEEoN88US=> M2\IeFIycMLi MVrEUXNQ Mmr5bY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> MUCyOVQzPjV2OB?=
NCI-H23 MXLGeY5kfGmxbjDBd5NigQ>? M3vobFExyqEQvF2= NH7ObFEzOWkEoB?= MWjEUXNQ NULtXnN{cW6lcnXhd4V{KHB3MzDwdo91\WmwIHzleoVtew>? MViyOVQzPjV2OB?=
A2780 NUmwZoRITnWwY4Tpc44hSXO|YYm= MWOxNOKh|ryP NV\Yd4M2OjGqwrC= M1jFVmROW09? MkT3bY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NXrjZnlzOjV2Mk[1OFg>
NCI-H23 MlrUSpVv[3Srb36gRZN{[Xl? MlPMNVDDqM7:TR?= NHe3U4QzOWkEoB?= MkD3SG1UVw>? NE\RfJhl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> NGDPWoMzPTR{NkW0PC=>
A2780 MlPLSpVv[3Srb36gRZN{[Xl? MnLNNVDDqM7:TR?= NF7MPVczOWkEoB?= NWPGdGNETE2VTx?= M1r5bYRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz NWjDcJBZOjV2Mk[1OFg>
HCT116  NVXWZZV{TnWwY4Tpc44hSXO|YYm= NULUXpZtOTBiwsXN NGDy[oEzPCCq M2rsUoNifXOnczDhJJA2Oy2mZYDlcoRmdnRidHX0doFxdG:rZDDHNU1ienKnc4SgbY4h\GmybH;p[EBJS1RzMU[gZ4xwdmW|IFSzJIFv\CCGOB?= Mmf2NlU{QDByNUW=
MCF-10CA1a MXjGeY5kfGmxbjDBd5NigQ>? NYTYTJYzOTEEoN88US=> M1rvW|Q5KGh? NGH4d3ZFVVOR MXzpcohq[mm2czDiZZNidCCrbo\hd4lwdiCjbnSgdoVlfWOnZDDUS2Yu|rJ|LXnu[JVk\WRiaX72ZZNqd25idH:gZoF{[WxibHX2[Yx{ NIDhZ4QzPTJ3N{eyPS=>
MCF-10A1  Mn\jSpVv[3Srb36gRZN{[Xl? NUDB[I1TOTEEoN88US=> NVzufohGOjRxNEigbC=> MV7EUXNQ MojsbY5pcWKrdIOgcYloemG2aX;uJI9nKG6xcn3hcEBjemWjc4Sg[ZBqfGinbHnhcOKh MWOyOVI2Pzd{OR?=
MCF-10CA1a M{\n[WZ2dmO2aX;uJGF{e2G7 M2TiVVExyqEQvF2= M1r5[FI1KGh? M3;ndWROW09? NIH3e5ll\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= MUSyOVI2Pzd{OR?=
MCF-10CA1a NYr6XGpuTnWwY4Tpc44hSXO|YYm= MWOxNOKh|ryP M3fUXFI1KGh? MX\EUXNQ NEXBU3lqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= NYT2OZhxOjV{NUe3Nlk>
SK-BR-7 NXnaVXlxTnWwY4Tpc44hSXO|YYm= NV3ob4VsOTEEoN88US=> M3z6WVI1KGh? NXjsO4t{TE2VTx?= NH6yVlFqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= NH;COmMzPTJ3N{eyPS=>
SUM102PT MkDJSpVv[3Srb36gRZN{[Xl? NYDURWxDOTEEoN88US=> MmHDNlQhcA>? MlLBSG1UVw>? NYjhcGM{cW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u NFrXeZIzPTJ3N{eyPS=>
RAW 264.7 MUjGeY5kfGmxbjDBd5NigQ>? NUOzN3NbOTEEoN88US=> NUfjO|NnOzBibXnu MmD4dJJmfmWwdIOgeIhmKHB3MzDy[YR2[3Srb36gbY4hemW|cH;ud4UhfG9iTGDT MYeyOVE4OjV2Nx?=
RAW 264.7 MX7GeY5kfGmxbjDBd5NigQ>? Mn7MNVDDqM7:TR?= MoLoN|AhdWmw M4[3SZJm\HWlZYOgeIhmKEySUz3heYdu\W62ZXSgeIhmKE6ILd86RkBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZYN1cX[rdIm= MXiyOVE4OjV2Nx?=
RAW 264.7 MkPHSpVv[3Srb36gRZN{[Xl? NE\jcYYyOMLizszN MW[zNEBucW5? NWnBe4c6cW6qaXLpeJMhVFCVLXnu[JVk\WRiTl:gdJJw\HWldHnvcuKh MWCyOVE4OjV2Nx?=
MCF7  MkS1R4VtdCCYaXHibYxqfHliQYPzZZk> NXLMeG5mOi53INM1US=> Mo[2OUBl NUezVpdFTE2VTx?= NWT1VIlQe2Wwc3n0bZpmeyCPQ1[3JJRwKFCDUmCgbY5pcWKrdHnvci=> MkK5NlUxQDV7MEK=
MCF7  M4nZeGZ2dmO2aX;uJGF{e2G7 MVuyMlUhyrWP M{ftOlQ5KGh? NFjOdVdFVVOR NVSyS5l[\GWlcnXhd4V{KHSqZTDoc41wdG:pb4XzJGRUSiC{ZYDhbZIh\nKncYXlcoNq\XN? MVKyOVA5PTlyMh?=
ACHN NVK2Nmt1S2WubDDWbYFjcWyrdImgRZN{[Xl? NVvOd2QyOC53LUGwJO69VQ>? NVuzZ|dXOC14IHS= NV[ye5J[TE2VTx?= NEPiSJJqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Mo\BNlUxPjd5OEe=
Caki-2 NYHEWGpoS2WubDDWbYFjcWyrdImgRZN{[Xl? NUTz[mRIOC53LUGwJO69VQ>? NVTEVFVKOC14IHS= NHfjRYtFVVOR MV;pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFfpfnAzPTB4N{e4Oy=>
A498 MVrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFHkS|UxNjVvMUCg{txO MknWNE03KGR? NH3tR2tFVVOR NVXOXGJMcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M2PHTVI2ODZ5N{i3
115 NHvS[WJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1HhPVAvPS1zMDFOwG0> MkjBNE03KGR? M2r5O2ROW09? NHG1d2RqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NHTkdHMzPTB4N{e4Oy=>
117 NIXkdnNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUCwMlUuOTBizszN NXXlO3diOC14IHS= MlzqSG1UVw>? NVjoNI0{cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NIPJUXAzPTB4N{e4Oy=>
ACHN MYfGeY5kfGmxbjDBd5NigQ>? NF;ESFcxNjVxMT:1JO69VQ>? MYm0PEBp NYLwO4tJTE2VTx?= NEHr[I5t\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= MUCyOVA3Pzd6Nx?=
Caki-2 NFXacVBHfW6ldHnvckBCe3OjeR?= MW[wMlUwOS93IN88US=> NV;h[m9IPDhiaB?= NITT[ZpFVVOR MXXs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MWeyOVA3Pzd6Nx?=
A498 NXH1VXRqTnWwY4Tpc44hSXO|YYm= MoDQNE42NzFxNTFOwG0> NUXwXpU4PDhiaB?= M2XlVWROW09? M1v3fYxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz MV6yOVA3Pzd6Nx?=
115 NH3STYRHfW6ldHnvckBCe3OjeR?= MljmNE42NzFxNTFOwG0> NEjDXJE1QCCq M{jpc2ROW09? NWHNPYVmdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= M{GyWVI2ODZ5N{i3
ACHN Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvPOUDPxE1? MVi0PEBp MYHEUXNQ MlnFbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg Mk\QNlUxPjd5OEe=
Caki-2 NGTsRmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkexOUDPxE1? NUHkOJZxPDhiaB?= MnXCSG1UVw>? M1vt[4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MXWyOVA3Pzd6Nx?=
A498 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jMZlUh|ryP NHPH[3M1QCCq NWTO[JR6TE2VTx?= M3Tkeolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NUXJ[I5HOjVyNke3PFc>
115 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHHRVE5PSEQvF2= MkXqOFghcA>? NXy0[YQxTE2VTx?= NGrrd5BqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NVnqU|JDOjVyNke3PFc>
ACHN NIjEPZpHfW6ldHnvckBCe3OjeR?= MkLpOUDPxE1? NVfQZ4JiPDhiaB?= MWPEUXNQ MnjPbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MkXuNlUxPjd5OEe=
Caki-2 MULGeY5kfGmxbjDBd5NigQ>? Ml;xOUDPxE1? Mm\EOFghcA>? NEfC[HVFVVOR MXzpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NHX3Z3EzPTB4N{e4Oy=>
A498 NUDTUYhQTnWwY4Tpc44hSXO|YYm= Mn\SOUDPxE1? MVK0PEBp MXLEUXNQ MnfMbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= M{C2SlI2ODZ5N{i3
115 M{X5TWZ2dmO2aX;uJGF{e2G7 Mlu4OUDPxE1? M2Hzb|Q5KGh? NFLmc3hFVVOR MoL4bY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NUHBfYVyOjVyNke3PFc>
MOLM-13 MXHGeY5kfGmxbjDBd5NigQ>? NXizNXJQPsLizszN MYSwMVghcA>? M1TZXGROW09? NYDRNpZEcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gdFU{NCCPRF2yMEBxOjFiYX7kJIFk\XS7bHH0[YQheDV| MUKyOFg5PTB6Mh?=
MOLM-13 NX2wc3h2TnWwY4Tpc44hSXO|YYm= M13veFbDqM7:TR?= NFLjTI83KGh? MXfEUXNQ NUfYXpg4\W6qYX7j[ZMhfGinIHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhUDKEIHHu[EBp\WG2IIPoc4NsKHC{b4TlbY5{KEi|cEK3JIFv\CCKc4C5NC=> M3Lr[|I1QDh3MEiy
HepG2 MmP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\TPItOPzJiaB?= M2LicWROW09? M3XURmlEPTB;M{WuPFYhyrFiMj65JO69VQ>? NVfoO2xNOjR6OES4NFk>
HepG2/As MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrkfYo4OiCq NYfG[nBkTE2VTx?= MVTJR|UxRTZ6LkGzJOKyKDlwNjFOwG0> NXnqUoxtOjR6OES4NFk>
SMMC7721 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorYO|IhcA>? NX3iNoNkTE2VTx?= MojxTWM2OD1|MT6yPEDDuSB2LkKg{txO MoG1NlQ5QDR6MEm=
SMMC7721/Ac NGLCOnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDGO|IhcA>? NGnxdnNFVVOR MW\JR|UxRTV3LkKxJOKyKDVwMEOg{txO MlPxNlQ5QDR6MEm=
Huh-7 NEXh[I1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV23NkBp MWLEUXNQ M2q1dmlEPTB;M{OuPVYhyrFiMz65JO69VQ>? MV6yOFg5PDhyOR?=
Hep3B MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPGO|IhcA>? MWXEUXNQ M1LMUmlEPTB;MkCuNVghyrFiMT64OEDPxE1? NXv2N2F{OjR6OES4NFk>
HepG2 NYS0V2JtSXCxcITvd4l{KEG|c3H5 MYrpcoR2[2W|IHHwc5B1d3Orcx?= M17HXFI1QDh2OEC5
SMMC7721 NV[0Vpl7SXCxcITvd4l{KEG|c3H5 M1fubolv\HWlZYOgZZBweHSxc3nz M3nsclI1QDh2OEC5
Huh-7 M1TSV2Fxd3C2b4Ppd{BCe3OjeR?= MYLpcoR2[2W|IHHwc5B1d3Orcx?= MViyOFg5PDhyOR?=
Hep3B MW\BdI9xfG:|aYOgRZN{[Xl? NES2TplqdmS3Y3XzJIFxd3C2b4Ppdy=> NGHIbmIzPDh6NEiwPS=>
U2OS  NWLGcpgxTnWwY4Tpc44hSXO|YYm= NYTuNJpCOjBizszN NH;oXXQzPCCq MXnpcoNz\WG|ZYOgeIhmKG2UTlGgcIV3\Wy|IH;mxsBDS0x{QUGsJGJEVFiOwrDhcoRDS0yZ M33jTlI1QDZ5MkW5
AML2 M{nlbmFxd3C2b4Ppd{BCe3OjeR?= NYf6SGV[Oi9zMDFOwG0> M3nrblI1NzR6IHi= NUfXXnlCcW6mdXPld{BieG:ydH;zbZM> MXGyOFY2QTd2OR?=
MOML13 MlPPRZBweHSxc3nzJGF{e2G7 M{Pvb|IwOTBizszN M4jtWlI1NzR6IHi= Mn3HbY5lfWOnczDhdI9xfG:|aYO= MYSyOFY2QTd2OR?=
AML2 NI\6e3FHfW6ldHnvckBCe3OjeR?= NH\IdVQyOM7:TR?= MX2yM|QhcA>? NWDDbFljcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MV2yOFY2QTd2OR?=
AML3 M3H0cGZ2dmO2aX;uJGF{e2G7 M1vhR|Ex|ryP NHfNXJczNzRiaB?= NF:yZVZqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NFTieG8zPDZ3OUe0PS=>
MOML13 NX7E[mE4TnWwY4Tpc44hSXO|YYm= MkDzNVDPxE1? NH;6e4ozNzRiaB?= MWPpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= MnrONlQ3PTl5NEm=
BeWo M3TXRWZ2dmO2aX;uJGF{e2G7 MV2zNEDDvU1? MWeyOEBp MnT3bY5kemWjc3XzJJA2OyxiTXTtNkwheDJzIHHu[EBRfW2jIHH0JJRp\SCycn;0[YlvKGyndnXs NHSzd4MzPDR7OEG1OC=>
BeWo M1\sUGFxd3C2b4Ppd{BCe3OjeR?= NVTlT3c1OzBiwsXN M{\HblI1KGh? M3;nfolv[3KnYYPld{BieG:ydH;zbZM> MnXMNlQ1QThzNUS=
OCI NVTpfndTTnWwY4Tpc44hSXO|YYm= MYSxNEDPxE1? NHjUdnEzPCCq MnPSeZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w M2nDWFI1PDd|NU[y
MOLM NELGTHdHfW6ldHnvckBCe3OjeR?= NELRd3YyOCEQvF2= NWPFN|B5OjRiaB?= MXn1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? MojzNlQ1PzN3NkK=
U2OS  MWnGeY5kfGmxbjDBd5NigQ>? M3K0U|IxKM7:TR?= MXmyOEBp NV7OXpRzcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= NWi0NIdNOjR|Nk[wNFc>
RKO NGnGcJdHfW6ldHnvckBCe3OjeR?= NGDWbYQzOCEQvF2= MUWyOEBp M{DXdIlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? Mn;LNlQ{PjZyMEe=
U2OS  MVzGeY5kfGmxbjDBd5NigQ>? MlvhNlAh|ryP M2XLRlI1KGh? MkH3bY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= NYXUbFc3OjR|Nk[wNFc>
RKO M1;q[mZ2dmO2aX;uJGF{e2G7 MWiyNEDPxE1? Mlf2NlQhcA>? M4HuNolv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u NHjmV4QzPDN4NkCwOy=>
SMMC-7721  NIjS[YlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYSxMlI2NTJyIN88US=> NV3LdZZjOjRxNEivO|IhcA>? NWj5foZrTE2VTx?= NGrHRnJqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NYLIUWl7OjR{OE[zNVI>
HuH-7 MlTnR4VtdCCYaXHibYxqfHliQYPzZZk> MUixMlI2NTJyIN88US=> NFz3c2gzPC92OD:3NkBp MYLEUXNQ NIq3W3ZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M33r[|I1Ojh4M{Gy
SMMC-7721  NFfLS|BCeG:ydH;zbZMhSXO|YYm= NH;ub|gzOCEQvF2= NGHwUXk1QCCq MY\EUXNQ MYLpcoR2[2W|IHHwc5B1d3Orcx?= NI\BVYgzPDJ6NkOxNi=>
HuH-7 NUjRZpBsSXCxcITvd4l{KEG|c3H5 M2LVb|IxKM7:TR?= NHHrU4E1QCCq Ml;sSG1UVw>? MYTpcoR2[2W|IHHwc5B1d3Orcx?= NHi3OJUzPDJ6NkOxNi=>
SMMC-7721  M2i4WWZ2dmO2aX;uJGF{e2G7 NWfydmJmOTBizszN MWWzOkBp NIjOPFdFVVOR NWfJXodi\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NHvYcXUzPDJ6NkOxNi=>
HuH-7 NEjZWFFHfW6ldHnvckBCe3OjeR?= NYLhRZdIOTBizszN NEPibYM{PiCq MoXvSG1UVw>? MkP5[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> MlHQNlQzQDZ|MUK=
AT2 MmfVSpVv[3Srb36gRZN{[Xl? M1PQZ|UwOTBizszN M1nzNIxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li MX6yOFI1ODJyMx?=
REH NW\hNXlmTnWwY4Tpc44hSXO|YYm= NEjXSmU2NzFyIN88US=> NXLQU4I6dGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= MmrINlQzPDB{MEO=
UoCB6 M3nEe2Z2dmO2aX;uJGF{e2G7 NGnqXG02NzFyIN88US=> MlPOcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? NH\UXo4zPDJ2MEKwNy=>
AT2 M136W2NmdGxiVnnhZoltcXS7IFHzd4F6 NWX2dmJ3OC1{NTFOwG0> NUPJUII4cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= Ml;WNlQzPDB{MEO=
REH Mn3LR4VtdCCYaXHibYxqfHliQYPzZZk> NWS3WFNsOC1{NTFOwG0> NXzYbmpucW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MX:yOFI1ODJyMx?=
UoCB6 MlTUR4VtdCCYaXHibYxqfHliQYPzZZk> NIXKOXQxNTJ3IN88US=> M3;OUolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M4PwXVI1OjRyMkCz
A2780 MkXySpVv[3Srb36gRZN{[Xl? M4Dx[lUwOTBxMkCg{txO NGPhflAzPCCq M{HFPZVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi MnnqNlQyOzZzNEe=
H460 Mor5SpVv[3Srb36gRZN{[Xl? NYLZOHZpPS9zMD:yNEDPxE1? NIjMVlgzPCCq M4\hUpVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi MXeyOFE{PjF2Nx?=
Lovo  NWSxdW92TnWwY4Tpc44hSXO|YYm= M{LNTlUwOTBxMkCg{txO NELiVnMzPCCq M13sb5VxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NELMS|QzPDF|NkG0Oy=>
A2780 NFHIZZVCeG:ydH;zbZMhSXO|YYm= MX[1M|ExNzJyIN88US=> MknoNlQhcA>? M2fFU4VvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN MoHvNlQyOzZzNEe=
H460 MnTHRZBweHSxc3nzJGF{e2G7 NVzJU2ZlPS9zMD:yNEDPxE1? MXmyOEBp M2jLVoVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN MlrXNlQyOzZzNEe=
Lovo  M4HGdWFxd3C2b4Ppd{BCe3OjeR?= MmrZOU8yOC9{MDFOwG0> MmLaNlQhcA>? MWHlcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> MoPMNlQyOzZzNEe=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (171.96 mM)
Ethanol 30 mg/mL (51.59 mM)
Water <1 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-(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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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