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 M3HiZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYqzeJg2PcLizszN NGnBO2s1QMLiaB?= MnTaZoxw[2u|IEK3MW9JSy2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiClb33wZZJi[mynIITvJJRp[XRib3[gZoF{[WxibHX2[Yx{ NUfpUXZIOjZ|NUC1OlU>
NP69 M{L1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LybWlEPTB;M{GuOlnDuTJwNUSg{txO M3zzWlI3OjV{NUe1
NP460 M3TScmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjnTWM2OD1{Mj64OeKyOS5zODFOwG0> MXeyOlI2OjV5NR?=
C666-1 NVXLUop[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojMTWM2OD1zOT65OeKyQC57MzFOwG0> Mle5NlYzPTJ3N{W=
C666-1 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXixNEDDvU1? MmHDOFghcA>? NXzRclUzTE2VTx?= M2CxO5NmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJJRp\SCleYTveI95cWNiZX\m[YN1KG:oIHPpd5Bt[XSrbh?= NF;GVW0zPjJ3MkW3OS=>
C666-1  MW\GeY5kfGmxbjDBd5NigQ>? NE\pPVQyOCEEtV2= MoT1NlQhcA>? NH\I[ZZFVVOR M{HHOIFkfGm4YYTld{B1cGVicEWzJJBifGi5YYmsJJVxemWpdXzheIlv\yCyNUOsJJAzOSCjbnSgUYRuOg>? NGW3[HUzPjJ3MkW3OS=>
C666-1 Mn3rRZBweHSxc3nzJGF{e2G7 M1XSblExKML3TR?= NH3JdFE1QC95MjDo NF7PPYNFVVOR NH[xUFF{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{BkcXOybHH0bY4ucW6mdXPl[EBieG:ydH;zbZM> NInZO4EzPjJ3MkW3OS=>
A549 NFi0cpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSyOEBp MkDYTWM2OD1zNz62PEDDuSB2LkWyJO69VQ>? MXuyOlEzPTJ|MB?=
A549-NTC M4HDVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{KxcFI1KGh? MU\JR|UxRTF7LkSyJOKyKDFwOU[g{txO MU[yOlEzPTJ|MB?=
A549-920 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnFTngzPCCq NE\DSo1KSzVyPUOzMlg2KMLzIESuPFQh|ryP NGL0PXczPjF{NUKzNC=>
CRL-5908 NXzJZYh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXeyOEBp MWLJR|UxRTN6LkexJOKyKDJwNEOg{txO MUSyOlEzPTJ|MB?=
L6 Mnj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[xNOKh|ryPwrC= M3v3XlI1NzR6L{eyJIg> MnXmSG1UVw>? M4PXTIlvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? NEHFPIMzPTh5MUe5OC=>
C2C12 NV7RTGxHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXWxNOKh|ryPwrC= MVqyOE81QC95MjDo NUCzNVNkTE2VTx?= MlywbY5pcWKrdIOgZ4VtdHNicILvcIln\XKjdHnvckBidmRiZHnm[oVz\W62aXH0bY9v Mom2NlU5PzF5OUS=
MCF-7  M{PIdWZ2dmO2aX;uJGF{e2G7 MXKxNOKh|ryP MY\EUXNQ NV\4UYJ7cW6qaXLpeJMh[3mlbHnuJGQyKGGwZDDEbYNmesLi MnHLNlU4ODJ5MEO=
DU4475  NVvP[ZJiTnWwY4Tpc44hSXO|YYm= NUHDNVI3PS9zMD:yNEDPxE1? M4n2UlI1yqCq NGnSTotld3ewcnXneYxifGW|IGTvZ4EuOSCmb4PlJIRmeGWwZHXueIx6 MnmzNlU2PDdzN{S=
SMMC-7721 M2TTUGZ2dmO2aX;uJGF{e2G7 M4C3cVExKM7:TR?= M1vueFQ5KGh? M4LrfGROW09? NF3tXW9k[XW|ZYOgSG5CKESVQjDkZY1i\2V? M4Hp[|I2PTR2M{[x
SMMC-7721 NXLyWpdUTnWwY4Tpc44hSXO|YYm= MXOxNEDPxE1? NFnvNpY1QCCq MX\EUXNQ M{f3cYlv\HWlZYOgeIhmKGOqcn;tZZRqdi2kb4Xu[EBxem:2ZXnuJGlHUTF4IITvJJBienSrYXzsfUBtd2OjbHn6[UBqdiC2aHWgZ5l1d3CuYYPtxsA> M4LMT|I2PTR2M{[x
SMMC-7721 MV\GeY5kfGmxbjDBd5NigQ>? MkX6NVAh|ryP NV7kWld[PDhiaB?= M4\YR2ROW09? NYXQT2lHcW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mxsBKTk6EMdMgcXJPSQ>? NHTEenAzPTV2NEO2NS=>
SMMC-7721 NWGwV3d1TnWwY4Tpc44hSXO|YYm= Mom1NVAh|ryP Mly1N|YhcA>? M4HQSmROW09? Mm[1Z4F2e2W|IITo[UBm[3SxcHnjJIV5eHKnc4Ppc44hd2ZiSV\JNVY> M3;xfVI2PTR2M{[x
MCF-7 MXzGeY5kfGmxbjDBd5NigQ>? NYK3cWEyOTEEoN88US=> Ml;PNE0zPCCq NYnqb2JJcW6mdXPld{BxPTNiYX7kJJAzOS:FaYCx M2[3fVI2PDh{M{ez
OVCAR10 M4nES2Z2dmO2aX;uJGF{e2G7 NW[ySnpMOTEEoN88US=> Ml7hNlFpyqB? NYjIS|FQTE2VTx?= MlHqbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> M{H2clI2PDJ4NUS4
NCI-H23 M3\HfmZ2dmO2aX;uJGF{e2G7 M3;SfFExyqEQvF2= MVKyNYjDqA>? NYnrbGV[TE2VTx?= MXTpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz NFHYfmkzPTR{NkW0PC=>
A2780 NFfzOZlHfW6ldHnvckBCe3OjeR?= NV7GWWg5OTEEoN88US=> M1jMW|IycMLi M3rsNWROW09? NYWxWINzcW6lcnXhd4V{KHB3MzDwdo91\WmwIHzleoVtew>? M3H0V|I2PDJ4NUS4
NCI-H23 M3HPbmZ2dmO2aX;uJGF{e2G7 NWrxZnV[OTEEoN88US=> NIXwc4szOWkEoB?= Mni4SG1UVw>? NGjZRmRl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> MkSzNlU1OjZ3NEi=
A2780 NU[zbWVxTnWwY4Tpc44hSXO|YYm= M1XQOlExyqEQvF2= NULXcZhTOjGqwrC= MXrEUXNQ NH7VTmZl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> M2DqfVI2PDJ4NUS4
HCT116  MUjGeY5kfGmxbjDBd5NigQ>? MUmxNEDDvU1? MmXYNlQhcA>? MXPjZZV{\XNiYTDwOVMu\GWyZX7k[Y51KHSndILhdIxwcWRiR{GtZZJz\XO2IHnuJIRqeGyxaXSgTGNVOTF4IHPsc45meyCGMzDhcoQhTDh? MX:yOVM5ODB3NR?=
MCF-10CA1a M3PMW2Z2dmO2aX;uJGF{e2G7 NFnySXoyOMLizszN NHm0VY41QCCq M{nMXmROW09? M4\WVIlvcGmkaYTzJIJie2GuIHnueoF{cW:wIHHu[EBz\WS3Y3XkJHRITi4QskOtbY5lfWOnZDDpcpZie2mxbjD0c{Bj[XOjbDDs[ZZmdHN? MmfHNlUzPTd5Mkm=
MCF-10A1  M4TtU2Z2dmO2aX;uJGF{e2G7 NGHJR2gyOMLizszN MmrvNlQwPDhiaB?= NFj0PXlFVVOR MVTpcohq[mm2czDtbYdz[XSrb36gc4Yhdm:{bXHsJIJz\WG|dDDldIl1cGWuaXHsxsA> M{LleFI2OjV5N{K5
MCF-10CA1a NHW2NJRHfW6ldHnvckBCe3OjeR?= MnTBNVDDqM7:TR?= NWHzNlJXOjRiaB?= NXLyfm86TE2VTx?= NXHlU|Vk\GWlcnXhd4V{KHSqZTDUS2Yu|rJ|LXnu[JVk\WRibWLORUBt\X[nbIOgc4ZOVVB{LNMgUW1RQSxiYX7kxsBqdnSnZ4LpcuKh|rMEoEO= MXiyOVI2Pzd{OR?=
MCF-10CA1a M{\PcGZ2dmO2aX;uJGF{e2G7 NWHte485OTEEoN88US=> MmjVNlQhcA>? M1zHeWROW09? MWHpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? NV6yZZoyOjV{NUe3Nlk>
SK-BR-7 NVrLfpZMTnWwY4Tpc44hSXO|YYm= MkLSNVDDqM7:TR?= NFvlfVUzPCCq M1XveWROW09? M3;UV4lvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= NFHlbWszPTJ3N{eyPS=>
SUM102PT MoXQSpVv[3Srb36gRZN{[Xl? Mn35NVDDqM7:TR?= MVSyOEBp MXPEUXNQ M3fYdYlvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= MV:yOVI2Pzd{OR?=
RAW 264.7 M1Tn[2Z2dmO2aX;uJGF{e2G7 MlXGNVDDqM7:TR?= MYGzNEBucW5? NGXxcZJxemW4ZX70d{B1cGVicEWzJJJm\HWldHnvckBqdiC{ZYPwc45{\SC2bzDMVHM> NHmwV44zPTF5MkW0Oy=>
RAW 264.7 NF\jfIJHfW6ldHnvckBCe3OjeR?= MnrUNVDDqM7:TR?= MW[zNEBucW5? NXPPSpZGemWmdXPld{B1cGViTGDTMYF2\22nboTl[EB1cGViTl[t{tpDKGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBi[3Srdnn0fS=> NWXVfFhkOjVzN{K1OFc>
RAW 264.7 MlTmSpVv[3Srb36gRZN{[Xl? M1HWclExyqEQvF2= M3\ubFMxKG2rbh?= MYfpcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= Mnq1NlUyPzJ3NEe=
MCF7  NVHidY5lS2WubDDWbYFjcWyrdImgRZN{[Xl? MlnpNk42KML3TR?= M1POXVUh\A>? NH7a[2NFVVOR M17ES5NmdnOrdHn6[ZMhVUOINzD0c{BRSVKSIHnubIljcXSrb36= MYqyOVA5PTlyMh?=
MCF7  NFPOeYZHfW6ldHnvckBCe3OjeR?= MX6yMlUhyrWP M2r3eFQ5KGh? MlLDSG1UVw>? MVfk[YNz\WG|ZYOgeIhmKGixbX;sc4dwfXNiRGPCJJJmeGGrcjDmdoVyfWWwY3nldy=> MWOyOVA5PTlyMh?=
ACHN NVrxUGlQS2WubDDWbYFjcWyrdImgRZN{[Xl? MUiwMlUuOTBizszN MXKwMVYh\A>? M4riPGROW09? NEXqV3VqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M3XIdFI2ODZ5N{i3
Caki-2 NGHR[YJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVOwMlUuOTBizszN M2PCOVAuPiCm MWjEUXNQ NHHZd2FqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M3S3fFI2ODZ5N{i3
A498 NF3sWlRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4XiclAvPS1zMDFOwG0> MUCwMVYh\A>? MVvEUXNQ MV7pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkGxNlUxPjd5OEe=
115 NIntZY9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4TVVFAvPS1zMDFOwG0> MWqwMVYh\A>? NVu0UIw3TE2VTx?= Mo\kbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NY\BWZNtOjVyNke3PFc>
117 NETxSppE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NV7sc3R1OC53LUGwJO69VQ>? MUmwMVYh\A>? NX7xTlgyTE2VTx?= M4nLeolvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYDjO2JDOjVyNke3PFc>
ACHN MVjGeY5kfGmxbjDBd5NigQ>? M1;3O|AvPS9zL{Wg{txO NGrpbHI1QCCq NY[xcm5ITE2VTx?= NIr2bYJt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= M{Ht[VI2ODZ5N{i3
Caki-2 NXXHXXhrTnWwY4Tpc44hSXO|YYm= NFLlSVgxNjVxMT:1JO69VQ>? MnzFOFghcA>? M17qeWROW09? NEDIV4dt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= MUKyOVA3Pzd6Nx?=
A498 Mk\ESpVv[3Srb36gRZN{[Xl? Mof0NE42NzFxNTFOwG0> NF2xcJY1QCCq NGXSV|hFVVOR MnvRcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? NUDPSFBUOjVyNke3PFc>
115 NX;FNlJzTnWwY4Tpc44hSXO|YYm= MYewMlUwOS93IN88US=> NGDZfYo1QCCq NH:xZ2pFVVOR MoOwcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? M3:xblI2ODZ5N{i3
ACHN MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV61JO69VQ>? NHvkS2g1QCCq M{PkT2ROW09? NHrxN3lqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> MX6yOVA3Pzd6Nx?=
Caki-2 NVuzfm9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzQZ4dXPSEQvF2= MYi0PEBp MkjMSG1UVw>? M4nRdolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> Ml25NlUxPjd5OEe=
A498 Ml\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjGOUDPxE1? MnfsOFghcA>? MXfEUXNQ MYLpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NHTGXI0zPTB4N{e4Oy=>
115 NH7KOYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXe1JO69VQ>? MmnPOFghcA>? MorHSG1UVw>? M2KyNYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NYDyeo06OjVyNke3PFc>
ACHN MoPLSpVv[3Srb36gRZN{[Xl? NHjWZVQ2KM7:TR?= M4PQVlQ5KGh? NV\3WpFRTE2VTx?= NEDPc2tqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MVOyOVA3Pzd6Nx?=
Caki-2 MnmwSpVv[3Srb36gRZN{[Xl? NYrDb2Y2PSEQvF2= NFTyUmM1QCCq MniySG1UVw>? M{f1UYlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= MUWyOVA3Pzd6Nx?=
A498 NVXHd3NPTnWwY4Tpc44hSXO|YYm= M3jnUFUh|ryP M4rwXFQ5KGh? NIHmbGpFVVOR M3nLV4lv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= NF3RO2MzPTB4N{e4Oy=>
115 MYfGeY5kfGmxbjDBd5NigQ>? MmTIOUDPxE1? NEC0cVk1QCCq NVHHcppITE2VTx?= MVjpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi M{LLVlI2ODZ5N{i3
MOLM-13 MU\GeY5kfGmxbjDBd5NigQ>? M2TjWlbDqM7:TR?= NULLT49vOC16IHi= M3H6NGROW09? M{jGTIlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIIC1N{whVUSPMjygdFIyKGGwZDDhZ4V1gWyjdHXkJJA2Ow>? M4raSVI1QDh3MEiy
MOLM-13 NX3tZoN5TnWwY4Tpc44hSXO|YYm= M1PvN|bDqM7:TR?= M4r0SlYhcA>? NFuwblRFVVOR NYjQWIRE\W6qYX7j[ZMhfGinIHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhUDKEIHHu[EBp\WG2IIPoc4NsKHC{b4TlbY5{KEi|cEK3JIFv\CCKc4C5NC=> MlvONlQ5QDVyOEK=
HepG2 M2GzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXW3NkBp NXrhT4hWTE2VTx?= NWnWXmdyUUN3ME2zOU45PiEEsTCyMlkh|ryP NFvRR48zPDh6NEiwPS=>
HepG2/As Ml[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWS3NkBp NFvodJZFVVOR NF;hVGtKSzVyPU[4MlE{KMLzIEmuOkDPxE1? MYWyOFg5PDhyOR?=
SMMC7721 M{fyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\DTFczKGh? Mo\tSG1UVw>? MmjmTWM2OD1|MT6yPEDDuSB2LkKg{txO NEnJb2wzPDh6NEiwPS=>
SMMC7721/Ac MmfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHmc2M4OiCq MoSxSG1UVw>? NWHJNXpJUUN3ME21OU4zOSEEsTC1MlA{KM7:TR?= NVTL[lA4OjR6OES4NFk>
Huh-7 MlTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknDO|IhcA>? MnTHSG1UVw>? NEO5NndKSzVyPUOzMlk3KMLzIEOuPUDPxE1? Mn;aNlQ5QDR6MEm=
Hep3B MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrMO|IhcA>? MXXEUXNQ MVLJR|UxRTJyLkG4JOKyKDFwOESg{txO NVq1UGp7OjR6OES4NFk>
HepG2 M13BbWFxd3C2b4Ppd{BCe3OjeR?= NWC1UIx6cW6mdXPld{BieG:ydH;zbZM> M{\GdVI1QDh2OEC5
SMMC7721 MnfpRZBweHSxc3nzJGF{e2G7 M2qwV4lv\HWlZYOgZZBweHSxc3nz MnrNNlQ5QDR6MEm=
Huh-7 Mkn1RZBweHSxc3nzJGF{e2G7 NIHqbZRqdmS3Y3XzJIFxd3C2b4Ppdy=> M4\2XVI1QDh2OEC5
Hep3B M{LSSmFxd3C2b4Ppd{BCe3OjeR?= MlPObY5lfWOnczDhdI9xfG:|aYO= MVyyOFg5PDhyOR?=
U2OS  NHnOcpBHfW6ldHnvckBCe3OjeR?= MkfQNlAh|ryP MX:yOEBp MWPpcoNz\WG|ZYOgeIhmKG2UTlGgcIV3\Wy|IH;mxsBDS0x{QUGsJGJEVFiOwrDhcoRDS0yZ M4HKZlI1QDZ5MkW5
AML2 MYLBdI9xfG:|aYOgRZN{[Xl? M2\sUFIwOTBizszN MXKyOE81QCCq NFrROIpqdmS3Y3XzJIFxd3C2b4Ppdy=> MVKyOFY2QTd2OR?=
MOML13 MXzBdI9xfG:|aYOgRZN{[Xl? NVPH[I5lOi9zMDFOwG0> M2TqVlI1NzR6IHi= MXnpcoR2[2W|IHHwc5B1d3Orcx?= MVuyOFY2QTd2OR?=
AML2 NILKW|VHfW6ldHnvckBCe3OjeR?= MmLqNVDPxE1? NXLKVJJvOi92IHi= NYrYfm1DcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NF3XZYQzPDZ3OUe0PS=>
AML3 M{C4[2Z2dmO2aX;uJGF{e2G7 MV6xNO69VQ>? MWiyM|QhcA>? MknmbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= MmfnNlQ3PTl5NEm=
MOML13 MULGeY5kfGmxbjDBd5NigQ>? MXqxNO69VQ>? MX2yM|QhcA>? NIXaNVZqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> M1jQS|I1PjV7N{S5
BeWo NUmyZopLTnWwY4Tpc44hSXO|YYm= MY[zNEDDvU1? MV6yOEBp NFnh[nRqdmO{ZXHz[ZMheDV|LDDN[I0zNCCyMkGgZY5lKFC3bXGgZZQhfGinIIDyc5RmcW5ibHX2[Yw> MnHZNlQ1QThzNUS=
BeWo MUDBdI9xfG:|aYOgRZN{[Xl? MmPsN|AhyrWP MVOyOEBp M2DuSYlv[3KnYYPld{BieG:ydH;zbZM> M1\jdlI1PDl6MUW0
OCI M4DQfGZ2dmO2aX;uJGF{e2G7 NED1UFUyOCEQvF2= M1y3V|I1KGh? NUXjZ4lKfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u NX\1d2ljOjR2N{O1OlI>
MOLM NUHEWmxbTnWwY4Tpc44hSXO|YYm= NUDhU|VzOTBizszN NIDZfnczPCCq NWf6cpllfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u NITkcoMzPDR5M{W2Ni=>
U2OS  MnfpSpVv[3Srb36gRZN{[Xl? MX6yNEDPxE1? M{mxTVI1KGh? MUDpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv MX6yOFM3PjByNx?=
RKO NYC2eWVWTnWwY4Tpc44hSXO|YYm= NEfnWpYzOCEQvF2= NX;IV2VFOjRiaB?= M2noRolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? NVq1VFJqOjR|Nk[wNFc>
U2OS  MUfGeY5kfGmxbjDBd5NigQ>? MoTZNlAh|ryP NVTLWJU6OjRiaB?= MmnTbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= NETiUlYzPDN4NkCwOy=>
RKO MXzGeY5kfGmxbjDBd5NigQ>? Mn3xNlAh|ryP NE\jVGEzPCCq M2PVdolv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u M2jBV|I1OzZ4MEC3
SMMC-7721  M1\jV2NmdGxiVnnhZoltcXS7IFHzd4F6 MWSxMlI2NTJyIN88US=> NXPsPZJpOjRxNEivO|IhcA>? MlHFSG1UVw>? MnnmbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MlTONlQzQDZ|MUK=
HuH-7 MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MofaNU4zPS1{MDFOwG0> M3L3clI1NzR6L{eyJIg> M3jodWROW09? NYPUZWgxcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MYqyOFI5PjNzMh?=
SMMC-7721  M4XHVWFxd3C2b4Ppd{BCe3OjeR?= NGq5OVMzOCEQvF2= NVnlblM6PDhiaB?= NYL2foZ3TE2VTx?= NFfE[GlqdmS3Y3XzJIFxd3C2b4Ppdy=> NIe2[2IzPDJ6NkOxNi=>
HuH-7 NIrIXGJCeG:ydH;zbZMhSXO|YYm= NIq1NFEzOCEQvF2= MU[0PEBp MmPQSG1UVw>? NWLlUoN5cW6mdXPld{BieG:ydH;zbZM> NGCybnQzPDJ6NkOxNi=>
SMMC-7721  MnHmSpVv[3Srb36gRZN{[Xl? MlfHNVAh|ryP M2\PelM3KGh? NWriOGZsTE2VTx?= MV;kc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> M1XXRVI1Ojh4M{Gy
HuH-7 NIfNTI1HfW6ldHnvckBCe3OjeR?= M3XpO|ExKM7:TR?= M3LlR|M3KGh? NUD6NG86TE2VTx?= MULkc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> NI\aNVkzPDJ6NkOxNi=>
AT2 M3HKSmZ2dmO2aX;uJGF{e2G7 NYnxbph[PS9zMDFOwG0> NIfnNIpt\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= NGXhR3czPDJ2MEKwNy=>
REH MXHGeY5kfGmxbjDBd5NigQ>? Mlj4OU8yOCEQvF2= MWLs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? M3XtcVI1OjRyMkCz
UoCB6 MXnGeY5kfGmxbjDBd5NigQ>? MVW1M|ExKM7:TR?= NIfwbmFt\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= Mmr3NlQzPDB{MEO=
AT2 M{HXNmNmdGxiVnnhZoltcXS7IFHzd4F6 MV6wMVI2KM7:TR?= MX;pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NXS5OY04OjR{NECyNFM>
REH NGjscnNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mlv2NE0zPSEQvF2= NF74VVBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NGC1WIIzPDJ2MEKwNy=>
UoCB6 NYTqbZNQS2WubDDWbYFjcWyrdImgRZN{[Xl? MYKwMVI2KM7:TR?= MXzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4PtUlI1OjRyMkCz
A2780 MUHGeY5kfGmxbjDBd5NigQ>? NVi5e4tvPS9zMD:yNEDPxE1? NX33[m5bOjRiaB?= MUf1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? MnLJNlQyOzZzNEe=
H460 MWnGeY5kfGmxbjDBd5NigQ>? M2\OZlUwOTBxMkCg{txO NF3zUpEzPCCq NU\zZlF6fXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= M{XQOlI1OTN4MUS3
Lovo  NG\UcFlHfW6ldHnvckBCe3OjeR?= M1LIclUwOTBxMkCg{txO NHXicZgzPCCq M4\ZZpVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NVLLRXV5OjRzM{[xOFc>
A2780 MVHBdI9xfG:|aYOgRZN{[Xl? NIPlPIw2NzFyL{KwJO69VQ>? NXyyZ3R5OjRiaB?= NGSxcpFmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? M2\NcVI1OTN4MUS3
H460 NV\DOFExSXCxcITvd4l{KEG|c3H5 NFjq[FM2NzFyL{KwJO69VQ>? NHz4WXAzPCCq Morj[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MVyyOFE{PjF2Nx?=
Lovo  MWTBdI9xfG:|aYOgRZN{[Xl? M2SxN|UwOTBxMkCg{txO MknCNlQhcA>? NYrQdnR7\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? MlLTNlQyOzZzNEe=

... 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

カスタマーフィードバック (3)


Click to enlarge
Rating
Source Cell Death Dis, 2011, 2, e243. Nutlin-3 purchased from Selleck
Method Caspase-Glo 3/7 Assays
Cell Lines UKF-NB-3 cells, UKF-NB-3r cells
Concentrations 10 μM
Incubation Time
Results Investigation of caspase 3/7 activation in response to Nutlin-3 and other cytotoxic drugs revealed that apoptosis induction is reduced and delayed in UKF-NB-3rNutlin10μM cells compared with UKF-NB-3 (Figure 2).

Click to enlarge
Rating
Source Cell death dis, 2012, 3, e294. Nutlin-3 purchased from Selleck
Method Western Blot
Cell Lines UKF-NB cells
Concentrations 10 uM
Incubation Time 24 h
Results Only one study has reported an A76T mutation that was found in benign breast tissue. Interestingly, UKF-NB-3’RITA10 uM IV cells were as sensitive to nutlin-3 treatment as parental UKF-NB-3 cells with nutlin-3 treatment resulting in the induction of p53 response gene expression in these cells.

Click to enlarge
Rating
Source Int J Oncol, 2014, 44, 761-8. Nutlin-3 purchased from Selleck
Method Immunoprecipitation
Cell Lines Hepatoma cells
Concentrations 20 uM
Incubation Time 24 h
Results It conducted in vivo ubiquitination assays with the treatment of Nutlin-3, a small molecule inhibitor of the MDM2/p53 interaction, and found that BIRC6 knockdown still facilitated the degradation of p53 by ubiquitination independent of Mdm2.

文献中の引用 (9)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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