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 MoTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHlOeKh|ryP NGLtXYg1QMLiaB?= MWLicI9kc3NiMketU2hENWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKGOxbYDhdoFjdGVidH:geIhifCCxZjDiZZNidCCuZY\lcJM> NUfZV5ZpOjZ|NUC1OlU>
NP69 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHxeY5KSzVyPUOxMlY6yrF{LkW0JO69VQ>? MoT6NlYzPTJ3N{W=
NP460 NFrNcHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml76TWM2OD1{Mj64OeKyOS5zODFOwG0> M4LFcVI3OjV{NUe1
C666-1 M1v3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTF7Lkm1xtE5Njl|IN88US=> MYmyOlI2OjV5NR?=
C666-1 M4CzRWNmdGxiVnnhZoltcXS7IFHzd4F6 M4jUOFExKML3TR?= Mle1OFghcA>? NH22eopFVVOR Mn7Rd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:geIhmKGO7dH;0c5hq[yCnZn\lZ5Qhd2ZiY3nzdIxifGmw NVW2[3pMOjZ{NUK1O|U>
C666-1  MYPGeY5kfGmxbjDBd5NigQ>? NF7V[JYyOCEEtV2= MWCyOEBp NVvYRnJITE2VTx?= NHnQcnVi[3SrdnH0[ZMhfGinIIC1N{Bx[XSqd3H5MEB2eHKnZ4XsZZRqdmdicEWzMEBxOjFiYX7kJG1ldTJ? Mmq2NlYzPTJ3N{W=
C666-1 M1r1[GFxd3C2b4Ppd{BCe3OjeR?= NHyxTFAyOCEEtV2= NUjkUHN7PDhxN{KgbC=> NWDZZopJTE2VTx?= M1rXVpNmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJINqe3CuYYTpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> NF3IXZkzPjJ3MkW3OS=>
A549 M1rOXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKyOEBp Ml\qTWM2OD1zNz62PEDDuSB2LkWyJO69VQ>? Moj6NlYyOjV{M{C=
A549-NTC NXfRWIROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG3RZQzPCCq MXjJR|UxRTF7LkSyJOKyKDFwOU[g{txO MUWyOlEzPTJ|MB?=
A549-920 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfzOGczPCCq MojQTWM2OD1|Mz64OUDDuSB2Lki0JO69VQ>? MYiyOlEzPTJ|MB?=
CRL-5908 NVjYZ4d2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTzWZBjOjRiaB?= MW\JR|UxRTN6LkexJOKyKDJwNEOg{txO M{TU[FI3OTJ3MkOw
L6 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2[4V|ExyqEQvF5CpC=> MVqyOE81QC95MjDo MVrEUXNQ MmfYbY5pcWKrdIOgZ4VtdHNicILvcIln\XKjdHnvckBidmRiZHnm[oVz\W62aXH0bY9v Mn3vNlU5PzF5OUS=
C2C12 MlTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonrNVDDqM7:TdMg NU[0RlNGOjRxNEivO|IhcA>? NWPwc4ptTE2VTx?= MkfVbY5pcWKrdIOgZ4VtdHNicILvcIln\XKjdHnvckBidmRiZHnm[oVz\W62aXH0bY9v MWKyOVg4OTd7NB?=
MCF-7  NIixTHJHfW6ldHnvckBCe3OjeR?= MU[xNOKh|ryP MkDOSG1UVw>? MknpbY5pcWKrdIOgZ5lkdGmwIFSxJIFv\CCGaXPlduKh MYOyOVcxOjdyMx?=
DU4475  MVfGeY5kfGmxbjDBd5NigQ>? M37MUFUwOTBxMkCg{txO M{\qRVI1yqCq Mnr3[I94dnKnZ4XsZZRmeyCWb3PhMVEh\G:|ZTDk[ZBmdmSnboTsfS=> NIjub2EzPTV2N{G3OC=>
SMMC-7721 MXvGeY5kfGmxbjDBd5NigQ>? NInyW3oyOCEQvF2= MkfUOFghcA>? MUXEUXNQ NUTmVZJb[2G3c3XzJGRPSSCGU1Kg[IFu[Wen M4jnRVI2PTR2M{[x
SMMC-7721 MVrGeY5kfGmxbjDBd5NigQ>? M1HldlExKM7:TR?= NV;jcZVCPDhiaB?= MlLRSG1UVw>? Mn7ybY5lfWOnczD0bIUh[2i{b33heIlvNWKxdX7kJJBzd3SnaX6gTWZKOTZidH:gdIFzfGmjbHz5JIxw[2GuaYrlJIlvKHSqZTDjfZRweGyjc35CpC=> MlLoNlU2PDR|NkG=
SMMC-7721 MnnqSpVv[3Srb36gRZN{[Xl? NWDHdlVtOTBizszN M{LGXFQ5KGh? MX7EUXNQ NVToc4dHcW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mxsBKTk6EMdMgcXJPSQ>? NIC2VlkzPTV2NEO2NS=>
SMMC-7721 MWLGeY5kfGmxbjDBd5NigQ>? NYfP[VFPOTBizszN MUOzOkBp M1;HbmROW09? MlfnZ4F2e2W|IITo[UBm[3SxcHnjJIV5eHKnc4Ppc44hd2ZiSV\JNVY> NETnTXAzPTV2NEO2NS=>
MCF-7 M4[3bWZ2dmO2aX;uJGF{e2G7 MkHmNVDDqM7:TR?= MmqyNE0zPCCq MX;pcoR2[2W|IIC1N{BidmRicEKxM2NqeDF? MkP5NlU1QDJ|N{O=
OVCAR10 NF7u[ZhHfW6ldHnvckBCe3OjeR?= M3TORVExyqEQvF2= NVTEO3JSOjGqwrC= M2\Qe2ROW09? NHTEeHZqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ M3m1UlI2PDJ4NUS4
NCI-H23 MWfGeY5kfGmxbjDBd5NigQ>? M3;DelExyqEQvF2= Ml3oNlFpyqB? MXLEUXNQ NIXObIRqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ M3z2bVI2PDJ4NUS4
A2780 MojiSpVv[3Srb36gRZN{[Xl? NIfkRmoyOMLizszN M2XzfVIycMLi M{T4WmROW09? NYH2O3lOcW6lcnXhd4V{KHB3MzDwdo91\WmwIHzleoVtew>? MljONlU1OjZ3NEi=
NCI-H23 MmHKSpVv[3Srb36gRZN{[Xl? MW[xNOKh|ryP M3PRbVIycMLi NHf1N4dFVVOR M4GzSoRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz NEPFWnczPTR{NkW0PC=>
A2780 NW\TPYhVTnWwY4Tpc44hSXO|YYm= M4P4SVExyqEQvF2= NUDHO5ZnOjGqwrC= MkPYSG1UVw>? M3HJS4Rm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz M3v0V|I2PDJ4NUS4
HCT116  NHriXGxHfW6ldHnvckBCe3OjeR?= NInsb2syOCEEtV2= MkTqNlQhcA>? M4PHR4NifXOnczDhJJA2Oy2mZYDlcoRmdnRidHX0doFxdG:rZDDHNU1ienKnc4SgbY4h\GmybH;p[EBJS1RzMU[gZ4xwdmW|IFSzJIFv\CCGOB?= NHy1ZpIzPTN6MEC1OS=>
MCF-10CA1a NUPYO4JVTnWwY4Tpc44hSXO|YYm= NEP1cYoyOMLizszN NVPOUnZpPDhiaB?= NH7DfXZFVVOR NEnlfJNqdmirYnn0d{Bj[XOjbDDpcpZie2mxbjDhcoQhemWmdXPl[EBVT0ZvzsKzMYlv\HWlZXSgbY53[XOrb36geI8h[mG|YXygcIV3\Wy| NGm5R5EzPTJ3N{eyPS=>
MCF-10A1  NIrONZNHfW6ldHnvckBCe3OjeR?= M3rEXlExyqEQvF2= NHXucnkzPC92ODDo MWTEUXNQ MXzpcohq[mm2czDtbYdz[XSrb36gc4Yhdm:{bXHsJIJz\WG|dDDldIl1cGWuaXHsxsA> NHGxNnYzPTJ3N{eyPS=>
MCF-10CA1a M4HyfmZ2dmO2aX;uJGF{e2G7 MVOxNOKh|ryP M2nmdFI1KGh? NVvT[FdJTE2VTx?= NEDPbGRl\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= M{ftc|I2OjV5N{K5
MCF-10CA1a MkLySpVv[3Srb36gRZN{[Xl? NX7HR2NkOTEEoN88US=> MXSyOEBp MoPPSG1UVw>? NWjTd3ljcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MlPONlUzPTd5Mkm=
SK-BR-7 Ml3VSpVv[3Srb36gRZN{[Xl? M1\NWlExyqEQvF2= Ml30NlQhcA>? NFq4U5FFVVOR MV;pcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? MWmyOVI2Pzd{OR?=
SUM102PT MYrGeY5kfGmxbjDBd5NigQ>? MWmxNOKh|ryP MUmyOEBp NVfPbFdzTE2VTx?= MUfpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? MnKyNlUzPTd5Mkm=
RAW 264.7 M1P3WmZ2dmO2aX;uJGF{e2G7 NXL3SWxTOTEEoN88US=> NV7BWYp{OzBibXnu MVjwdoV3\W62czD0bIUheDV|IILl[JVkfGmxbjDpckBz\XOyb37z[UB1dyCOUGO= M{jhclI2OTd{NUS3
RAW 264.7 M{\vUGZ2dmO2aX;uJGF{e2G7 MmXxNVDDqM7:TR?= MmLKN|AhdWmw MoTGdoVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= NHvXVGszPTF5MkW0Oy=>
RAW 264.7 MoPrSpVv[3Srb36gRZN{[Xl? MYOxNOKh|ryP NXHmVINrOzBibXnu MV7pcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= MoXpNlUyPzJ3NEe=
MCF7  NF23XXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkTBNk42KML3TR?= M4LLdVUh\A>? NXfjSHVLTE2VTx?= M1nxbJNmdnOrdHn6[ZMhVUOINzD0c{BRSVKSIHnubIljcXSrb36= MYqyOVA5PTlyMh?=
MCF7  M2jzfWZ2dmO2aX;uJGF{e2G7 NXfNbId4Oi53INM1US=> MUK0PEBp Ml:ySG1UVw>? MYnk[YNz\WG|ZYOgeIhmKGixbX;sc4dwfXNiRGPCJJJmeGGrcjDmdoVyfWWwY3nldy=> MW[yOVA5PTlyMh?=
ACHN M4DNU2NmdGxiVnnhZoltcXS7IFHzd4F6 M4rYcVAvPS1zMDFOwG0> NYWy[4FVOC14IHS= NU[4Znl6TE2VTx?= NUnhVIpzcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MUWyOVA3Pzd6Nx?=
Caki-2 MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUSwMlUuOTBizszN NIf3c3kxNTZiZB?= M3zmZmROW09? NVq1OmNZcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MWeyOVA3Pzd6Nx?=
A498 NGm5TFZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWXvcVB5OC53LUGwJO69VQ>? MlvoNE03KGR? MlSySG1UVw>? MVvpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MX6yOVA3Pzd6Nx?=
115 MX\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV2wMlUuOTBizszN NELRe2MxNTZiZB?= MkjQSG1UVw>? NXHrTIs{cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NX7keWNNOjVyNke3PFc>
117 MnjkR4VtdCCYaXHibYxqfHliQYPzZZk> MWqwMlUuOTBizszN MmrCNE03KGR? MoftSG1UVw>? MmS1bY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYPaflU5OjVyNke3PFc>
ACHN M{LDZ2Z2dmO2aX;uJGF{e2G7 M1PHUFAvPS9zL{Wg{txO MmDCOFghcA>? NIG1[JFFVVOR NHvY[Wxt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= M3i1Z|I2ODZ5N{i3
Caki-2 M1nacGZ2dmO2aX;uJGF{e2G7 MWWwMlUwOS93IN88US=> NHLTXWs1QCCq MlrrSG1UVw>? NVjQTXlmdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NEj3S44zPTB4N{e4Oy=>
A498 M{DW[mZ2dmO2aX;uJGF{e2G7 M4HlO|AvPS9zL{Wg{txO NGXMXpU1QCCq NHTqUolFVVOR M1S2R4xm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz Ml;JNlUxPjd5OEe=
115 NGLQdHFHfW6ldHnvckBCe3OjeR?= MV6wMlUwOS93IN88US=> MnPuOFghcA>? NULre3dtTE2VTx?= M3jNcIxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz MW[yOVA3Pzd6Nx?=
ACHN M2nNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\Me4g2KM7:TR?= MnLqOFghcA>? NYjqOVB2TE2VTx?= MVTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MnHXNlUxPjd5OEe=
Caki-2 MkHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HHO|Uh|ryP M3zTO|Q5KGh? MUPEUXNQ Mm\EbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg NVrXdJJzOjVyNke3PFc>
A498 NF60U|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXe1JO69VQ>? M3fMT|Q5KGh? NFPXb3hFVVOR MXXpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NHzxcnMzPTB4N{e4Oy=>
115 M4nhPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv3OUDPxE1? NV7scFhGPDhiaB?= NETwS3hFVVOR MULpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NV31cGxoOjVyNke3PFc>
ACHN NYPmNpY4TnWwY4Tpc44hSXO|YYm= NIjrN242KM7:TR?= NG\IfJY1QCCq NYn0OmoyTE2VTx?= MV;pcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi M{nyVFI2ODZ5N{i3
Caki-2 NY\HPZF2TnWwY4Tpc44hSXO|YYm= NXj6cmlYPSEQvF2= MX[0PEBp NETZSlNFVVOR M2roRYlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= M{j2XlI2ODZ5N{i3
A498 MmTLSpVv[3Srb36gRZN{[Xl? NV[2OlBbPSEQvF2= NEfYcmg1QCCq NHHGcpBFVVOR NVvnb|hMcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> NV\HT3lWOjVyNke3PFc>
115 NGrv[FFHfW6ldHnvckBCe3OjeR?= M{nV[FUh|ryP NWLWe4ZOPDhiaB?= M{jBUmROW09? Mn7DbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NUTwc|YyOjVyNke3PFc>
MOLM-13 MUnGeY5kfGmxbjDBd5NigQ>? M3j4blbDqM7:TR?= NXPoSFZUOC16IHi= NEnEOJZFVVOR MXjpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyNUOsJG1FVTJuIICyNUBidmRiYXPleJlt[XSnZDDwOVM> MVyyOFg5PTB6Mh?=
MOLM-13 MnTuSpVv[3Srb36gRZN{[Xl? NHHUVVI3yqEQvF2= M{PVPFYhcA>? MV;EUXNQ M1PlVIVvcGGwY3XzJJRp\SCjY3X0fYxifGmxbjDv[kBpcXO2b37lJGgzSiCjbnSgbIVifCC|aH;jb{Bxem:2ZXnud{BJe3B{NzDhcoQhUHOyOUC= M{\kb|I1QDh3MEiy
HepG2 NXjifppET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjCc3M4OiCq NYDMNZkzTE2VTx?= NHrmZ3ZKSzVyPUO1Mlg3KMLzIEKuPUDPxE1? M4nuOFI1QDh2OEC5
HepG2/As MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzyO|IhcA>? Ml3nSG1UVw>? NV;EXYVQUUN3ME22PE4yOyEEsTC5MlYh|ryP MUKyOFg5PDhyOR?=
SMMC7721 MmrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILSfXc4OiCq NF\aUXBFVVOR M2LzTWlEPTB;M{GuNlghyrFiND6yJO69VQ>? MYGyOFg5PDhyOR?=
SMMC7721/Ac NFrLPGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\JdFczKGh? NVj2OlFUTE2VTx?= MnfDTWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? Mn[4NlQ5QDR6MEm=
Huh-7 NF3SdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrCO|IhcA>? MV7EUXNQ MVzJR|UxRTN|Lkm2JOKyKDNwOTFOwG0> M3LKXVI1QDh2OEC5
Hep3B Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLhO2o4OiCq MnPNSG1UVw>? MY\JR|UxRTJyLkG4JOKyKDFwOESg{txO M4TIWVI1QDh2OEC5
HepG2 NGi2XmVCeG:ydH;zbZMhSXO|YYm= NHTCfIlqdmS3Y3XzJIFxd3C2b4Ppdy=> NW\4WZJCOjR6OES4NFk>
SMMC7721 NI\nc3FCeG:ydH;zbZMhSXO|YYm= NYroN3RKcW6mdXPld{BieG:ydH;zbZM> NXPtRpd7OjR6OES4NFk>
Huh-7 MmTmRZBweHSxc3nzJGF{e2G7 M3zEe4lv\HWlZYOgZZBweHSxc3nz MlzUNlQ5QDR6MEm=
Hep3B Mne2RZBweHSxc3nzJGF{e2G7 MU\pcoR2[2W|IHHwc5B1d3Orcx?= NYK2VXVGOjR6OES4NFk>
U2OS  NHvUWVRHfW6ldHnvckBCe3OjeR?= MVqyNEDPxE1? M3HsN|I1KGh? M{LQUIlv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= MlvWNlQ5Pjd{NUm=
AML2 NV;WO2lvSXCxcITvd4l{KEG|c3H5 NEPJTpQzNzFyIN88US=> M3XaV|I1NzR6IHi= M2nUbYlv\HWlZYOgZZBweHSxc3nz NXG5WGd3OjR4NUm3OFk>
MOML13 M3;Jb2Fxd3C2b4Ppd{BCe3OjeR?= NF2zXG8zNzFyIN88US=> MXiyOE81QCCq MoLnbY5lfWOnczDhdI9xfG:|aYO= NW\3bJVOOjR4NUm3OFk>
AML2 MXPGeY5kfGmxbjDBd5NigQ>? NE\iTYUyOM7:TR?= NW[xbIFtOi92IHi= M1vKPYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz M3;m[lI1PjV7N{S5
AML3 NIPQNnlHfW6ldHnvckBCe3OjeR?= NFvKXXoyOM7:TR?= NFjJcnYzNzRiaB?= M1\KdIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NFi4[YIzPDZ3OUe0PS=>
MOML13 MUPGeY5kfGmxbjDBd5NigQ>? NX\KZo05OTEQvF2= NVHQbGdSOi92IHi= NXPEcY1XcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NVrCfnN1OjR4NUm3OFk>
BeWo MnXaSpVv[3Srb36gRZN{[Xl? NV;MOVNVOzBiwsXN NGfWZ|IzPCCq MkDmbY5kemWjc3XzJJA2OyxiTXTtNkwheDJzIHHu[EBRfW2jIHH0JJRp\SCycn;0[YlvKGyndnXs MmfWNlQ1QThzNUS=
BeWo MkW5RZBweHSxc3nzJGF{e2G7 MUOzNEDDvU1? NV;scWZqOjRiaB?= MVHpcoNz\WG|ZYOgZZBweHSxc3nz MlLSNlQ1QThzNUS=
OCI Mn;PSpVv[3Srb36gRZN{[Xl? M3PH[lExKM7:TR?= M2HkSVI1KGh? M1LD[ZVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= M4nFb|I1PDd|NU[y
MOLM M1P2U2Z2dmO2aX;uJGF{e2G7 NH\yWIsyOCEQvF2= NFzSbYwzPCCq NVjte5lxfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u MYWyOFQ4OzV4Mh?=
U2OS  M1raS2Z2dmO2aX;uJGF{e2G7 NFzEUlYzOCEQvF2= NYH3WI4{OjRiaB?= NXXWPHIxcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= M{Ps[FI1OzZ4MEC3
RKO MWjGeY5kfGmxbjDBd5NigQ>? Ml;QNlAh|ryP Mm[5NlQhcA>? Mlm0bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? M4LwdFI1OzZ4MEC3
U2OS  NEXEelVHfW6ldHnvckBCe3OjeR?= NVL0W|B5OjBizszN M33hOVI1KGh? MXLpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= NIHwXnkzPDN4NkCwOy=>
RKO MnXhSpVv[3Srb36gRZN{[Xl? NG\ERoMzOCEQvF2= NGLzVHczPCCq NGj6dVZqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> M1SxTVI1OzZ4MEC3
SMMC-7721  MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXmxMlI2NTJyIN88US=> NGLjVmozPC92OD:3NkBp NYHHVWhITE2VTx?= MorXbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MmfCNlQzQDZ|MUK=
HuH-7 MVPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4rkSlEvOjVvMkCg{txO NV;h[GFQOjRxNEivO|IhcA>? M{DKUmROW09? MXPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NXz2dZIxOjR{OE[zNVI>
SMMC-7721  MWDBdI9xfG:|aYOgRZN{[Xl? MX2yNEDPxE1? NWjpNpRFPDhiaB?= NHXpOVVFVVOR NEPJTnVqdmS3Y3XzJIFxd3C2b4Ppdy=> NWHpdXBMOjR{OE[zNVI>
HuH-7 NFnvRpZCeG:ydH;zbZMhSXO|YYm= NXG0NXhuOjBizszN MUW0PEBp M1HSR2ROW09? NEH1WXBqdmS3Y3XzJIFxd3C2b4Ppdy=> MV2yOFI5PjNzMh?=
SMMC-7721  NF73TIFHfW6ldHnvckBCe3OjeR?= M3HBV|ExKM7:TR?= M3HkXFM3KGh? NYHhPFhVTE2VTx?= M4TDU4Rwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ M2TEfVI1Ojh4M{Gy
HuH-7 NVvTfZhyTnWwY4Tpc44hSXO|YYm= NEfmNnMyOCEQvF2= NUXkeJhzOzZiaB?= MXrEUXNQ Ml\J[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> NEfH[JczPDJ6NkOxNi=>
AT2 M2LoNGZ2dmO2aX;uJGF{e2G7 MoL5OU8yOCEQvF2= M2W2PIxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li M4LCflI1OjRyMkCz
REH NVfEcJFJTnWwY4Tpc44hSXO|YYm= M3j3fVUwOTBizszN M{WwToxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li M{nFS|I1OjRyMkCz
UoCB6 MlPzSpVv[3Srb36gRZN{[Xl? NG[5cng2NzFyIN88US=> NYLvNo5ydGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= MnXLNlQzPDB{MEO=
AT2 NULPUFhDS2WubDDWbYFjcWyrdImgRZN{[Xl? M2Xz[VAuOjVizszN M2K5cYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? Ml20NlQzPDB{MEO=
REH NV70WYVnS2WubDDWbYFjcWyrdImgRZN{[Xl? M2W3S|AuOjVizszN NGjWV2lqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NX7RTm1OOjR{NECyNFM>
UoCB6 MkPTR4VtdCCYaXHibYxqfHliQYPzZZk> MYCwMVI2KM7:TR?= MWTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MUeyOFI1ODJyMx?=
A2780 M{f1dWZ2dmO2aX;uJGF{e2G7 NX7xOIduPS9zMD:yNEDPxE1? NUDsSI5xOjRiaB?= NUPzNnp5fXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= M{TsVFI1OTN4MUS3
H460 MUTGeY5kfGmxbjDBd5NigQ>? NWfJNZdmPS9zMD:yNEDPxE1? M{HVOFI1KGh? NX\mRWVbfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= M2e3b|I1OTN4MUS3
Lovo  NXvaWIhUTnWwY4Tpc44hSXO|YYm= MYi1M|ExNzJyIN88US=> MmHXNlQhcA>? NHzJU2N2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= NGLBfFIzPDF|NkG0Oy=>
A2780 NUPscGVxSXCxcITvd4l{KEG|c3H5 M2DLTFUwOTBxMkCg{txO NFv1W40zPCCq MkLn[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> M1XuPFI1OTN4MUS3
H460 MXvBdI9xfG:|aYOgRZN{[Xl? M3XjO|UwOTBxMkCg{txO NUjMSXFsOjRiaB?= Mlrl[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> NHjDe2IzPDF|NkG0Oy=>
Lovo  M1PjU2Fxd3C2b4Ppd{BCe3OjeR?= NF;wfGQ2NzFyL{KwJO69VQ>? NULoOYd5OjRiaB?= Mlvn[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> M1T2WVI1OTN4MUS3

... 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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