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 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXy1xsDPxE1? NH\xWYs1QMLiaB?= M1Tw[IJtd2OtczCyO{1QUENvaX7keYNm\CClZXzsJJBzd2yrZnXyZZRqd25iY3;tdIFz[WKuZTD0c{B1cGG2IH;mJIJie2GuIHzleoVtew>? NH31V3IzPjN3MEW2OS=>
NP69 MoPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\jR3pbUUN3ME2zNU43QcLzMj61OEDPxE1? NHf5b3IzPjJ3MkW3OS=>
NP460 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlq2TWM2OD1{Mj64OeKyOS5zODFOwG0> NXe2O5VxOjZ{NUK1O|U>
C666-1 NVTnOVdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTF7Lkm1xtE5Njl|IN88US=> MnPYNlYzPTJ3N{W=
C666-1 MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGXQPJgyOCEEtV2= MUS0PEBp MYrEUXNQ M17mR5NmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJJRp\SCleYTveI95cWNiZX\m[YN1KG:oIHPpd5Bt[XSrbh?= MWSyOlI2OjV5NR?=
C666-1  MWjGeY5kfGmxbjDBd5NigQ>? NFvWVpAyOCEEtV2= NI\0SnYzPCCq Mn\CSG1UVw>? NHjROY1i[3SrdnH0[ZMhfGinIIC1N{Bx[XSqd3H5MEB2eHKnZ4XsZZRqdmdicEWzMEBxOjFiYX7kJG1ldTJ? NXzzdY5oOjZ{NUK1O|U>
C666-1 NU\0WopJSXCxcITvd4l{KEG|c3H5 NHXlWnYyOCEEtV2= MX:0PE84OiCq MmLISG1UVw>? MXPz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzDjbZNxdGG2aX6tbY5lfWOnZDDhdI9xfG:|aYO= M3LOZlI3OjV{NUe1
A549 M4jOZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVy3ZZRLOjRiaB?= M3HGUGlEPTB;MUeuOlghyrFiND61NkDPxE1? NXTqOXdiOjZzMkWyN|A>
A549-NTC M3z3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfhNlQhcA>? NXTtRoRzUUN3ME2xPU41OiEEsTCxMlk3KM7:TR?= MXGyOlEzPTJ|MB?=
A549-920 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlS4NlQhcA>? M1fzSGlEPTB;M{OuPFUhyrFiND64OEDPxE1? NWSz[YZDOjZzMkWyN|A>
CRL-5908 NYHvW45tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mme2NlQhcA>? M1nTXWlEPTB;M{iuO|EhyrFiMj60N{DPxE1? M4HPW|I3OTJ3MkOw
L6 MlzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX6xNOKh|ryPwrC= NETXVXYzPC92OD:3NkBp MXvEUXNQ M1zSNolvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? M3K1N|I2QDdzN{m0
C2C12 NH\XVIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjWZpIyOMLizszNxsA> MXWyOE81QC95MjDo NEjCTY5FVVOR NF;5NYFqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? MnLWNlU5PzF5OUS=
MCF-7  MmLzSpVv[3Srb36gRZN{[Xl? MVGxNOKh|ryP MW\EUXNQ M4nwc4lvcGmkaYTzJIN6[2yrbjDENUBidmRiRHnj[ZLDqA>? NHTYZYQzPTdyMkewNy=>
DU4475  NGfNblFHfW6ldHnvckBCe3OjeR?= NW\RO2t3PS9zMD:yNEDPxE1? MVyyOOKhcA>? NYP4bZc5\G:5boLl[5Vt[XSnczDUc4NiNTFiZH;z[UBl\XCnbnTlcpRtgQ>? M2L0bFI2PTR5MUe0
SMMC-7721 MX7GeY5kfGmxbjDBd5NigQ>? MmnuNVAh|ryP NGfZcFE1QCCq MkDrSG1UVw>? Mnz1Z4F2e2W|IFTORUBFW0JiZHHtZYdm MWOyOVU1PDN4MR?=
SMMC-7721 NHf6XIVHfW6ldHnvckBCe3OjeR?= NX[3fFNOOTBizszN NFTET281QCCq NHf4R5JFVVOR Ml63bY5lfWOnczD0bIUh[2i{b33heIlvNWKxdX7kJJBzd3SnaX6gTWZKOTZidH:gdIFzfGmjbHz5JIxw[2GuaYrlJIlvKHSqZTDjfZRweGyjc35CpC=> NVfH[YVROjV3NESzOlE>
SMMC-7721 MX3GeY5kfGmxbjDBd5NigQ>? NIGwNIgyOCEQvF2= NHe1OWE1QCCq M4rZS2ROW09? MVrpcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2cEoFnGUmIyyqCvUl7B M4LrN|I2PTR2M{[x
SMMC-7721 Ml7ISpVv[3Srb36gRZN{[Xl? M1zsPVExKM7:TR?= MkKwN|YhcA>? NGXKWoFFVVOR NWG3N5BD[2G3c3XzJJRp\SCnY4TvdIlkKGW6cILld5Nqd25ib3[gTWZKOTZ? MUmyOVU1PDN4MR?=
MCF-7 NVHVRZFmTnWwY4Tpc44hSXO|YYm= NHfHb3EyOMLizszN MYSwMVI1KGh? M1zxXIlv\HWlZYOgdFU{KGGwZDDwNlEwS2myMR?= MXeyOVQ5OjN5Mx?=
OVCAR10 NU[3dGJYTnWwY4Tpc44hSXO|YYm= MX2xNOKh|ryP Mm[1NlFpyqB? NHnkN4lFVVOR NGPFTIxqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ MlS0NlU1OjZ3NEi=
NCI-H23 MVPGeY5kfGmxbjDBd5NigQ>? MWKxNOKh|ryP MX6yNYjDqA>? M3HoXmROW09? MYXpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz M2S3NVI2PDJ4NUS4
A2780 NFnOU3BHfW6ldHnvckBCe3OjeR?= MmPTNVDDqM7:TR?= MY[yNYjDqA>? MkK3SG1UVw>? MorQbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> M33zS|I2PDJ4NUS4
NCI-H23 MlznSpVv[3Srb36gRZN{[Xl? NYLjVoJ{OTEEoN88US=> NWDpXok5OjGqwrC= M1LnSmROW09? M3XBWoRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz NULZNlh5OjV2Mk[1OFg>
A2780 NV7NbXE3TnWwY4Tpc44hSXO|YYm= M{jYS|ExyqEQvF2= NVr4TldYOjGqwrC= NIPVZXFFVVOR MWnk[YNz\WG|ZYOgeIhmKE[xeF2xJIxmfmWucx?= M3LpTVI2PDJ4NUS4
HCT116  M3H5bmZ2dmO2aX;uJGF{e2G7 Mk\ZNVAhyrWP M4nVR|I1KGh? Mn;tZ4F2e2W|IHGgdFU{NWSncHXu[IVvfCC2ZYTyZZBtd2mmIFexMYFzemW|dDDpckBlcXCub3nkJGhEXDFzNjDjcI9v\XNiREOgZY5lKER6 NYXtUpA{OjV|OECwOVU>
MCF-10CA1a NW\KPY02TnWwY4Tpc44hSXO|YYm= NFnZfFQyOMLizszN NUHveoNWPDhiaB?= MULEUXNQ NH\BRnZqdmirYnn0d{Bj[XOjbDDpcpZie2mxbjDhcoQhemWmdXPl[EBVT0ZvzsKzMYlv\HWlZXSgbY53[XOrb36geI8h[mG|YXygcIV3\Wy| M2e3OlI2OjV5N{K5
MCF-10A1  Mm\zSpVv[3Srb36gRZN{[Xl? NVjK[FVrOTEEoN88US=> MV:yOE81QCCq NHrjeWxFVVOR MWLpcohq[mm2czDtbYdz[XSrb36gc4Yhdm:{bXHsJIJz\WG|dDDldIl1cGWuaXHsxsA> MnHYNlUzPTd5Mkm=
MCF-10CA1a NUXhN2xQTnWwY4Tpc44hSXO|YYm= M2TzU|ExyqEQvF2= MV:yOEBp NHjDVZlFVVOR M{\nWoRm[3KnYYPld{B1cGViVFfGMe6zOy2rbnT1Z4VlKG2UTlGgcIV3\Wy|IH;mUW1ROi{EoF3NVFktKGGwZNMgbY51\We{aX9CpO6zyqB| NH7xZ40zPTJ3N{eyPS=>
MCF-10CA1a M2i5PGZ2dmO2aX;uJGF{e2G7 Moe3NVDDqM7:TR?= Ml3yNlQhcA>? M4jTUGROW09? MkLTbY5pcWKrdIOgJHRITi4QskOtbY5lfWOnZDDFVGhDOsLibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:w NH;VeHEzPTJ3N{eyPS=>
SK-BR-7 M{XNZmZ2dmO2aX;uJGF{e2G7 NIn0VVgyOMLizszN MWeyOEBp MXLEUXNQ NFjxPZdqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= NG\1bGszPTJ3N{eyPS=>
SUM102PT NInvVlhHfW6ldHnvckBCe3OjeR?= NG\COlYyOMLizszN NGqzZ4YzPCCq NGXURm1FVVOR MluybY5pcWKrdIOgJHRITi4QskOtbY5lfWOnZDDFVGhDOsLibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:w M{jSeFI2OjV5N{K5
RAW 264.7 Mn;3SpVv[3Srb36gRZN{[Xl? MU[xNOKh|ryP M3mxZlMxKG2rbh?= Mk\adJJmfmWwdIOgeIhmKHB3MzDy[YR2[3Srb36gbY4hemW|cH;ud4UhfG9iTGDT NFXDTGgzPTF5MkW0Oy=>
RAW 264.7 M3;yb2Z2dmO2aX;uJGF{e2G7 M4riR|ExyqEQvF2= M3zPRlMxKG2rbh?= MWTy[YR2[2W|IITo[UBNWFNvYYXncYVvfGWmIITo[UBPTi4QulKgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHjeIl3cXS7 M{C5UVI2OTd{NUS3
RAW 264.7 M3nHeGZ2dmO2aX;uJGF{e2G7 MoXENVDDqM7:TR?= NYrBTW16OzBibXnu M1Tk[olvcGmkaYTzJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb39CpC=> M1nUSVI2OTd{NUS3
MCF7  M3jOc2NmdGxiVnnhZoltcXS7IFHzd4F6 M4S1Z|IvPSEEtV2= NVLYZYdYPSCm M{HFR2ROW09? NWLnVZFSe2Wwc3n0bZpmeyCPQ1[3JJRwKFCDUmCgbY5pcWKrdHnvci=> MmTyNlUxQDV7MEK=
MCF7  MoKwSpVv[3Srb36gRZN{[Xl? MlfyNk42KML3TR?= NFv4d2c1QCCq MXzEUXNQ MmTm[IVkemWjc3XzJJRp\SCqb33vcI9od3W|IFTTRkBz\XCjaYKg[pJmeXWnbnPp[ZM> NWexWGIzOjVyOEW5NFI>
ACHN MoXoR4VtdCCYaXHibYxqfHliQYPzZZk> NHftWlAxNjVvMUCg{txO NWj4NYlHOC14IHS= MnnsSG1UVw>? MljYbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXvQVnZQOjVyNke3PFc>
Caki-2 NFLjSlZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHjMO5cxNjVvMUCg{txO MV:wMVYh\A>? MU\EUXNQ NV;3ZXFvcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MmXVNlUxPjd5OEe=
A498 MlPYR4VtdCCYaXHibYxqfHliQYPzZZk> NYjz[Hg{OC53LUGwJO69VQ>? M2rZVlAuPiCm Mmi0SG1UVw>? MX;pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXiyOVA3Pzd6Nx?=
115 MoTuR4VtdCCYaXHibYxqfHliQYPzZZk> Mn75NE42NTFyIN88US=> NH\vdIIxNTZiZB?= NWH5Z4MyTE2VTx?= MXnpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NF7QOYozPTB4N{e4Oy=>
117 NEH3SI1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkDsNE42NTFyIN88US=> MUKwMVYh\A>? M3PkS2ROW09? MVjpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHnXOZUzPTB4N{e4Oy=>
ACHN NIfPeYpHfW6ldHnvckBCe3OjeR?= M1[4VlAvPS9zL{Wg{txO M4LCXFQ5KGh? M{TxZ2ROW09? MmrFcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? MVqyOVA3Pzd6Nx?=
Caki-2 M3nBd2Z2dmO2aX;uJGF{e2G7 MVKwMlUwOS93IN88US=> NXHBWYlMPDhiaB?= MVjEUXNQ MlezcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? Ml;CNlUxPjd5OEe=
A498 NHTzVo5HfW6ldHnvckBCe3OjeR?= Ml3NNE42NzFxNTFOwG0> M4TZVFQ5KGh? M{ThO2ROW09? NXv2XHZNdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NUjSfZR1OjVyNke3PFc>
115 MoDiSpVv[3Srb36gRZN{[Xl? NYfCbpVNOC53L{GvOUDPxE1? M2K3blQ5KGh? MWDEUXNQ NHrJXpBt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= M2LVOFI2ODZ5N{i3
ACHN NVjPdopIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUC1JO69VQ>? M2j2OFQ5KGh? M4S3[GROW09? MUfpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NF\V[GszPTB4N{e4Oy=>
Caki-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnxNIM2KM7:TR?= MYO0PEBp M2fCVWROW09? M4PrSIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> M1fxUlI2ODZ5N{i3
A498 M1H3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLWTXUzPSEQvF2= MX20PEBp NHm2fFJFVVOR NX:1NZdRcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MXWyOVA3Pzd6Nx?=
115 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW3RlY2KM7:TR?= NHPVS3k1QCCq M1HzWWROW09? M2LMfIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> M3qyTlI2ODZ5N{i3
ACHN M1rkfmZ2dmO2aX;uJGF{e2G7 NHu2R5k2KM7:TR?= NHjFXWo1QCCq NGrucG5FVVOR MWXpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NXn0dVlZOjVyNke3PFc>
Caki-2 MlzXSpVv[3Srb36gRZN{[Xl? MY[1JO69VQ>? M4\jU|Q5KGh? M3r2PWROW09? M1\ydolv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= MoP5NlUxPjd5OEe=
A498 MkDqSpVv[3Srb36gRZN{[Xl? MVG1JO69VQ>? NXPvTpJjPDhiaB?= NX3jRnN{TE2VTx?= NVy0[GNEcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> M3;qOlI2ODZ5N{i3
115 NV22R44yTnWwY4Tpc44hSXO|YYm= NIrycnA2KM7:TR?= MmTvOFghcA>? MYHEUXNQ MXPpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NFezVm0zPTB4N{e4Oy=>
MOLM-13 NWXNWlVDTnWwY4Tpc44hSXO|YYm= MWe2xsDPxE1? M1ixSFAuQCCq M1fNdmROW09? MXrpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyNUOsJG1FVTJuIICyNUBidmRiYXPleJlt[XSnZDDwOVM> M4rTXVI1QDh3MEiy
MOLM-13 NEC3dWVHfW6ldHnvckBCe3OjeR?= MnzrOuKh|ryP MoTmOkBp NWTleWc2TE2VTx?= NGi3Z3lmdmijbnPld{B1cGViYXPleJlt[XSrb36gc4YhcGm|dH;u[UBJOkJiYX7kJIhm[XRic3jvZ4sheHKxdHXpcpMhUHOyMkegZY5lKEi|cEmw NV3ic21{OjR6OEWwPFI>
HepG2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfMZXo4OiCq M{n0bWROW09? MYLJR|UxRTN3Lki2JOKyKDJwOTFOwG0> M3[wTVI1QDh2OEC5
HepG2/As NXPsR4tGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TBW|czKGh? NIro[4VFVVOR NU\r[W95UUN3ME22PE4yOyEEsTC5MlYh|ryP NIfRdVkzPDh6NEiwPS=>
SMMC7721 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILVRm44OiCq NVWxUVVmTE2VTx?= M2nU[GlEPTB;M{GuNlghyrFiND6yJO69VQ>? NIHIclUzPDh6NEiwPS=>
SMMC7721/Ac Mom2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInJNnY4OiCq Mn\DSG1UVw>? NVPoU4J3UUN3ME21OU4zOSEEsTC1MlA{KM7:TR?= MXqyOFg5PDhyOR?=
Huh-7 NETTUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[3NkBp MlTISG1UVw>? MX\JR|UxRTN|Lkm2JOKyKDNwOTFOwG0> NF;jZZYzPDh6NEiwPS=>
Hep3B NHTSTXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2O5N|czKGh? M2\3SmROW09? NXj2ZnY4UUN3ME2yNE4yQCEEsTCxMlg1KM7:TR?= NWmzUJZROjR6OES4NFk>
HepG2 M4jXT2Fxd3C2b4Ppd{BCe3OjeR?= M2O4c4lv\HWlZYOgZZBweHSxc3nz MUOyOFg5PDhyOR?=
SMMC7721 MnGzRZBweHSxc3nzJGF{e2G7 NF7S[WVqdmS3Y3XzJIFxd3C2b4Ppdy=> NVr5cVZkOjR6OES4NFk>
Huh-7 NVTobFA5SXCxcITvd4l{KEG|c3H5 MXTpcoR2[2W|IHHwc5B1d3Orcx?= MUiyOFg5PDhyOR?=
Hep3B MVzBdI9xfG:|aYOgRZN{[Xl? NHrEeHJqdmS3Y3XzJIFxd3C2b4Ppdy=> M{DUfFI1QDh2OEC5
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AML2 Mn;ORZBweHSxc3nzJGF{e2G7 NF33SHYzNzFyIN88US=> NHjQeXgzPC92ODDo NVjiW4lVcW6mdXPld{BieG:ydH;zbZM> NED4ZnAzPDZ3OUe0PS=>
MOML13 NUnCe3RzSXCxcITvd4l{KEG|c3H5 MXOyM|ExKM7:TR?= Mn\ZNlQwPDhiaB?= MlHtbY5lfWOnczDhdI9xfG:|aYO= MUmyOFY2QTd2OR?=
AML2 NXX1Z4ZyTnWwY4Tpc44hSXO|YYm= M1PkfVEx|ryP NWPlbmY2Oi92IHi= MXnpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= M4XGVFI1PjV7N{S5
AML3 MUfGeY5kfGmxbjDBd5NigQ>? MnnJNVDPxE1? NXLFN2tDOi92IHi= MUjpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= NFjLd4MzPDZ3OUe0PS=>
MOML13 NVG3RXZiTnWwY4Tpc44hSXO|YYm= MVixNO69VQ>? NX7reZd3Oi92IHi= NFq0cG9qdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> Ml;WNlQ3PTl5NEm=
BeWo M2\2emZ2dmO2aX;uJGF{e2G7 M1rwV|MxKML3TR?= M1zaelI1KGh? NETJb4JqdmO{ZXHz[ZMheDV|LDDN[I0zNCCyMkGgZY5lKFC3bXGgZZQhfGinIIDyc5RmcW5ibHX2[Yw> MlzKNlQ1QThzNUS=
BeWo NIDsXo5CeG:ydH;zbZMhSXO|YYm= NXPQbGpZOzBiwsXN MmXMNlQhcA>? NV61dmZNcW6lcnXhd4V{KGGyb4D0c5Nqew>? M{TFVFI1PDl6MUW0
OCI MlPySpVv[3Srb36gRZN{[Xl? NVPvbIFjOTBizszN NGLKOm0zPCCq Mn7qeZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w MWmyOFQ4OzV4Mh?=
MOLM M3:zcWZ2dmO2aX;uJGF{e2G7 MlHVNVAh|ryP MXOyOEBp M17qSJVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= NHTZSFAzPDR5M{W2Ni=>
U2OS  MmnRSpVv[3Srb36gRZN{[Xl? MoPxNlAh|ryP M2HOSFI1KGh? NXSwb|g1cW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= M3HWSVI1OzZ4MEC3
RKO MUTGeY5kfGmxbjDBd5NigQ>? NVvmdIE6OjBizszN M{HXdFI1KGh? NWPubYxtcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= MV:yOFM3PjByNx?=
U2OS  M4Xqe2Z2dmO2aX;uJGF{e2G7 NWrpfFllOjBizszN M3nUeVI1KGh? NETSZ5NqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> NETqfmkzPDN4NkCwOy=>
RKO NGD5SY9HfW6ldHnvckBCe3OjeR?= MmnoNlAh|ryP NGfnNIYzPCCq NX7LcYJJcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> M{Hx[FI1OzZ4MEC3
SMMC-7721  MnnoR4VtdCCYaXHibYxqfHliQYPzZZk> NYjmcY9qOS5{NT2yNEDPxE1? MYiyOE81QC95MjDo Mo\uSG1UVw>? NXrZXollcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MlfwNlQzQDZ|MUK=
HuH-7 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGXuOoUyNjJ3LUKwJO69VQ>? NGm4[G8zPC92OD:3NkBp M3;yUmROW09? MXXpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MXuyOFI5PjNzMh?=
SMMC-7721  M3jDTWFxd3C2b4Ppd{BCe3OjeR?= MkfNNlAh|ryP NYjvb2VpPDhiaB?= NV2zUmhMTE2VTx?= M3nBR4lv\HWlZYOgZZBweHSxc3nz MXyyOFI5PjNzMh?=
HuH-7 MV\BdI9xfG:|aYOgRZN{[Xl? MViyNEDPxE1? Mn3SOFghcA>? MXTEUXNQ Mn;sbY5lfWOnczDhdI9xfG:|aYO= MWqyOFI5PjNzMh?=
SMMC-7721  M4WxOWZ2dmO2aX;uJGF{e2G7 M2XOb|ExKM7:TR?= NVfXSYlDOzZiaB?= NV;1NWJ2TE2VTx?= M3raUIRwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ NGTNSIUzPDJ6NkOxNi=>
HuH-7 MnLUSpVv[3Srb36gRZN{[Xl? MYGxNEDPxE1? M3myO|M3KGh? NVHGfHlUTE2VTx?= Mn76[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> M3\wO|I1Ojh4M{Gy
AT2 MXrGeY5kfGmxbjDBd5NigQ>? MVu1M|ExKM7:TR?= M4m0Uoxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li Mm[4NlQzPDB{MEO=
REH NX\1VnZFTnWwY4Tpc44hSXO|YYm= NF;jWWU2NzFyIN88US=> NG\UXmpt\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= MW[yOFI1ODJyMx?=
UoCB6 M3q3dWZ2dmO2aX;uJGF{e2G7 NG\Ye3k2NzFyIN88US=> MlewcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? NEO4W4QzPDJ2MEKwNy=>
AT2 M3Oze2NmdGxiVnnhZoltcXS7IFHzd4F6 NV;pZ2NTOC1{NTFOwG0> NFjEdYdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 Ml3YNlQzPDB{MEO=
REH NGDT[WlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NInvWJUxNTJ3IN88US=> M{HsVYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MYqyOFI1ODJyMx?=
UoCB6 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV:wMVI2KM7:TR?= NIDlSopqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NIrlWogzPDJ2MEKwNy=>
A2780 MmToSpVv[3Srb36gRZN{[Xl? M{i3[lUwOTBxMkCg{txO NUGyNXpOOjRiaB?= MonzeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? Mo\HNlQyOzZzNEe=
H460 NEDBeYFHfW6ldHnvckBCe3OjeR?= MmHBOU8yOC9{MDFOwG0> MWSyOEBp NXzRSWxJfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= M4nXNlI1OTN4MUS3
Lovo  MmT6SpVv[3Srb36gRZN{[Xl? NX74PIVsPS9zMD:yNEDPxE1? MkLzNlQhcA>? NEPMXVB2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= MYOyOFE{PjF2Nx?=
A2780 NW\DPVJvSXCxcITvd4l{KEG|c3H5 NUfnZphnPS9zMD:yNEDPxE1? NWXvfHdVOjRiaB?= NGjzepVmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? MUGyOFE{PjF2Nx?=
H460 M2jO[GFxd3C2b4Ppd{BCe3OjeR?= MorIOU8yOC9{MDFOwG0> M2n3N|I1KGh? M1z3e4VvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN M37URlI1OTN4MUS3
Lovo  NFzGTmtCeG:ydH;zbZMhSXO|YYm= M1i0RlUwOTBxMkCg{txO MYGyOEBp NVnPS4pC\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? NUXXS|JqOjRzM{[xOFc>

... 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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