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 NIS0UVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7RN2c2yqEQvF2= NHTvTnA1QMLiaB?= MWXicI9kc3NiMketU2hENWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKGOxbYDhdoFjdGVidH:geIhifCCxZjDiZZNidCCuZY\lcJM> NX;TZ41xOjZ|NUC1OlU>
NP69 M2CyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS4UHN[UUN3ME2zNU43QcLzMj61OEDPxE1? MW[yOlI2OjV5NR?=
NP460 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1POW2lEPTB;MkKuPFXDuTFwMUig{txO NXuxO3NJOjZ{NUK1O|U>
C666-1 M{TZN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml33TWM2OD1zOT65OeKyQC57MzFOwG0> M1OzdFI3OjV{NUe1
C666-1 NVft[XNOS2WubDDWbYFjcWyrdImgRZN{[Xl? NIP4[I4yOCEEtV2= MoL6OFghcA>? MV3EUXNQ MYfz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzD0bIUh[3m2b4TvfIlkKGWoZnXjeEBw\iClaYPwcIF1cW5? NUfPcWp[OjZ{NUK1O|U>
C666-1  NH7ScJdHfW6ldHnvckBCe3OjeR?= NYXqcVlFOTBiwsXN MXqyOEBp M1i0RWROW09? M2fhU4FkfGm4YYTld{B1cGVicEWzJJBifGi5YYmsJJVxemWpdXzheIlv\yCyNUOsJJAzOSCjbnSgUYRuOg>? MoC0NlYzPTJ3N{W=
C666-1 MWjBdI9xfG:|aYOgRZN{[Xl? NHrCbpYyOCEEtV2= M1i3cFQ5Nzd{IHi= MYPEUXNQ NUDWZnFXe2Wwc3n0bZpmeyCFNk[2MVEh[2WubIOgeI8h[2m|cHzheIlvNWmwZIXj[YQh[XCxcITvd4l{ MXOyOlI2OjV5NR?=
A549 NYPwXnlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NES2OWwzPCCq MUnJR|UxRTF5Lk[4JOKyKDRwNUKg{txO NVfYNVhGOjZzMkWyN|A>
A549-NTC NEH0SmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWyOEBp MmjrTWM2OD1zOT60NkDDuSBzLkm2JO69VQ>? NHP5dlIzPjF{NUKzNC=>
A549-920 M2\RXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TPe|I1KGh? M2f4bmlEPTB;M{OuPFUhyrFiND64OEDPxE1? NF76PHkzPjF{NUKzNC=>
CRL-5908 M1XBNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDQNlQhcA>? M3jGWWlEPTB;M{iuO|EhyrFiMj60N{DPxE1? MXuyOlEzPTJ|MB?=
L6 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHB[ZR5OTEEoN88UeKh NUfHTZNUOjRxNEivO|IhcA>? Moe0SG1UVw>? MUTpcohq[mm2czDj[YxteyCycn;sbYZmemG2aX;uJIFv\CCmaX\m[ZJmdnSrYYTpc44> NUP3OIpbOjV6N{G3PVQ>
C2C12 M4TzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCxNOKh|ryPwrC= NVXQb2ZIOjRxNEivO|IhcA>? MnnaSG1UVw>? NYCz[IlncW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w Mmr0NlU5PzF5OUS=
MCF-7  M{fmeGZ2dmO2aX;uJGF{e2G7 MUSxNOKh|ryP MWjEUXNQ MoLwbY5pcWKrdIOgZ5lkdGmwIFSxJIFv\CCGaXPlduKh NVPvWVZlOjV5MEK3NFM>
DU4475  NGj0ZmpHfW6ldHnvckBCe3OjeR?= MUm1M|ExNzJyIN88US=> MlLTNlTDqGh? M3uxNIRwf26{ZXf1cIF1\XNiVH;jZU0yKGSxc3Wg[IVx\W6mZX70cJk> MnXNNlU2PDdzN{S=
SMMC-7721 NVP2[oVoTnWwY4Tpc44hSXO|YYm= NITpOpgyOCEQvF2= Mom0OFghcA>? M3fNXmROW09? M{LtUYNifXOnczDEUmEhTFOEIHThcYFo\Q>? MWOyOVU1PDN4MR?=
SMMC-7721 M1LFUmZ2dmO2aX;uJGF{e2G7 M1L1WlExKM7:TR?= NVq5PJY3PDhiaB?= M{jj[WROW09? MXjpcoR2[2W|IITo[UBkcHKxbXH0bY4u[m:3bnSgdJJwfGWrbjDJSmkyPiC2bzDwZZJ1cWGubImgcI9k[WyrenWgbY4hfGinIHP5eI9xdGG|bdMg NXLZ[mx[OjV3NESzOlE>
SMMC-7721 NUG0doVSTnWwY4Tpc44hSXO|YYm= NHz0fJAyOCEQvF2= MV60PEBp NFL4PJRFVVOR NVLuSlA1cW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mxsBKTk6EMdMgcXJPSQ>? NIjRT44zPTV2NEO2NS=>
SMMC-7721 MkTySpVv[3Srb36gRZN{[Xl? Ml:zNVAh|ryP NF7nV3E{PiCq NXHUUoZ{TE2VTx?= MWfjZZV{\XNidHjlJIVkfG:yaXOg[ZhxemW|c3nvckBw\iCLRlmxOi=> NFPE[WEzPTV2NEO2NS=>
MCF-7 MmHKSpVv[3Srb36gRZN{[Xl? NIjtOlEyOMLizszN MUSwMVI1KGh? M2D3XYlv\HWlZYOgdFU{KGGwZDDwNlEwS2myMR?= MWWyOVQ5OjN5Mx?=
OVCAR10 NGCwNFZHfW6ldHnvckBCe3OjeR?= NGXLdFgyOMLizszN MmqzNlFpyqB? MkLFSG1UVw>? M1L5XIlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> Mlm5NlU1OjZ3NEi=
NCI-H23 M3XSXWZ2dmO2aX;uJGF{e2G7 NUG2SVlROTEEoN88US=> MUeyNYjDqA>? MVTEUXNQ MnPDbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NGX0[FYzPTR{NkW0PC=>
A2780 Mn3mSpVv[3Srb36gRZN{[Xl? NHmx[VMyOMLizszN NEPkcVMzOWkEoB?= M2O0bmROW09? NIG2OldqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ MXiyOVQzPjV2OB?=
NCI-H23 M1TMRWZ2dmO2aX;uJGF{e2G7 NHiwU|QyOMLizszN MmXFNlFpyqB? NXn6S|d[TE2VTx?= MlrO[IVkemWjc3XzJJRp\SCIb4jNNUBt\X[nbIO= M4KzO|I2PDJ4NUS4
A2780 M{K5[mZ2dmO2aX;uJGF{e2G7 MmPFNVDDqM7:TR?= NXWzTo83OjGqwrC= NYTKVXB1TE2VTx?= MYHk[YNz\WG|ZYOgeIhmKE[xeF2xJIxmfmWucx?= Ml7mNlU1OjZ3NEi=
HCT116  MoP6SpVv[3Srb36gRZN{[Xl? NWHhUIZFOTBiwsXN MXGyOEBp M2DnT4NifXOnczDhJJA2Oy2mZYDlcoRmdnRidHX0doFxdG:rZDDHNU1ienKnc4SgbY4h\GmybH;p[EBJS1RzMU[gZ4xwdmW|IFSzJIFv\CCGOB?= MY[yOVM5ODB3NR?=
MCF-10CA1a NVnlNVNHTnWwY4Tpc44hSXO|YYm= NEXRcm0yOMLizszN NXP2b3R3PDhiaB?= MXvEUXNQ NETQRWhqdmirYnn0d{Bj[XOjbDDpcpZie2mxbjDhcoQhemWmdXPl[EBVT0ZvzsKzMYlv\HWlZXSgbY53[XOrb36geI8h[mG|YXygcIV3\Wy| NIOzdFYzPTJ3N{eyPS=>
MCF-10A1  M3frW2Z2dmO2aX;uJGF{e2G7 M2\E[lExyqEQvF2= MmTrNlQwPDhiaB?= M3rzc2ROW09? NFTUWmhqdmirYnn0d{BucWe{YYTpc44hd2Zibn;ycYFtKGK{ZXHzeEBmeGm2aHXsbYFtyqB? NEjSWZMzPTJ3N{eyPS=>
MCF-10CA1a MnXLSpVv[3Srb36gRZN{[Xl? NG\lO4IyOMLizszN NV;mVJE6OjRiaB?= MVfEUXNQ NFXQW45l\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= MoLONlUzPTd5Mkm=
MCF-10CA1a MVXGeY5kfGmxbjDBd5NigQ>? NUjEfJR3OTEEoN88US=> MlvYNlQhcA>? M1jVTWROW09? NFj2fIJqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= MVOyOVI2Pzd{OR?=
SK-BR-7 NX\zcpl7TnWwY4Tpc44hSXO|YYm= Mn\lNVDDqM7:TR?= NFfPV28zPCCq MkX0SG1UVw>? NULRe2RrcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MnPFNlUzPTd5Mkm=
SUM102PT NYLp[Yh3TnWwY4Tpc44hSXO|YYm= NEfxZ2UyOMLizszN MYSyOEBp MkjxSG1UVw>? NWrLZ2hKcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MYGyOVI2Pzd{OR?=
RAW 264.7 MkTSSpVv[3Srb36gRZN{[Xl? M{XHRlExyqEQvF2= NWS3cFZnOzBibXnu M1q2VZBz\X[nboTzJJRp\SCyNUOgdoVlfWO2aX;uJIlvKHKnc4DvcpNmKHSxIFzQVy=> NWnObWJGOjVzN{K1OFc>
RAW 264.7 NWfsepRwTnWwY4Tpc44hSXO|YYm= MWOxNOKh|ryP NVv3Z20yOzBibXnu MoLjdoVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= M1WzZlI2OTd{NUS3
RAW 264.7 NXjjepVXTnWwY4Tpc44hSXO|YYm= MofkNVDDqM7:TR?= MVKzNEBucW5? M13PNolvcGmkaYTzJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb39CpC=> M{HNTFI2OTd{NUS3
MCF7  NFvlWpVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MorNNk42KML3TR?= NIGzOoE2KGR? M4PCZWROW09? NH6zU|d{\W6|aYTpfoV{KE2FRkegeI8hWEGUUDDpcohq[mm2aX;u M3fyNFI2ODh3OUCy
MCF7  MmrNSpVv[3Srb36gRZN{[Xl? MXSyMlUhyrWP NVPPXIRRPDhiaB?= M2r4VWROW09? M2ewRYRm[3KnYYPld{B1cGViaH;tc4xw\2:3czDEV2IhemWyYXnyJIZz\XG3ZX7jbYV{ MUKyOVA5PTlyMh?=
ACHN NHrHOYJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1L2UVAvPS1zMDFOwG0> MXSwMVYh\A>? M33s[WROW09? NUCwdolPcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NGH6VnAzPTB4N{e4Oy=>
Caki-2 NH7KTHFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGPOfXkxNjVvMUCg{txO MlHyNE03KGR? M{jBdGROW09? NFjke2pqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MnfTNlUxPjd5OEe=
A498 M3zr[GNmdGxiVnnhZoltcXS7IFHzd4F6 NGHWSWQxNjVvMUCg{txO NHzaN5MxNTZiZB?= M2CxemROW09? MUXpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWeyOVA3Pzd6Nx?=
115 M4PqV2NmdGxiVnnhZoltcXS7IFHzd4F6 MkTzNE42NTFyIN88US=> NI\SRmUxNTZiZB?= Mn7KSG1UVw>? MWLpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYrl[2g2OjVyNke3PFc>
117 NITEWpBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2PLO|AvPS1zMDFOwG0> M{frTFAuPiCm MVvEUXNQ MUfpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXSyOVA3Pzd6Nx?=
ACHN MWDGeY5kfGmxbjDBd5NigQ>? MnTUNE42NzFxNTFOwG0> M3XsdlQ5KGh? NYnVOVV6TE2VTx?= NGDaN2ht\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NE\HXpkzPTB4N{e4Oy=>
Caki-2 MorNSpVv[3Srb36gRZN{[Xl? M2XxNVAvPS9zL{Wg{txO NHX0UJg1QCCq NIjkVlFFVVOR MXns[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NGLsWXgzPTB4N{e4Oy=>
A498 MoLBSpVv[3Srb36gRZN{[Xl? Mkn5NE42NzFxNTFOwG0> MoLLOFghcA>? MY\EUXNQ M{D5SYxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz NX3zcZVJOjVyNke3PFc>
115 MWHGeY5kfGmxbjDBd5NigQ>? MWGwMlUwOS93IN88US=> NGDMflc1QCCq MmXjSG1UVw>? NUDsfYU3dGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= MXuyOVA3Pzd6Nx?=
ACHN M4POU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLCOUDPxE1? NIHDXnE1QCCq M{fFZ2ROW09? NETlXlNqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> M3\WeVI2ODZ5N{i3
Caki-2 NVPLPGZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXZeGE2KM7:TR?= MkXWOFghcA>? NF7QSVJFVVOR NFjCbHdqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NG\YbFYzPTB4N{e4Oy=>
A498 M2nhOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGG1enk2KM7:TR?= M4noUFQ5KGh? NInxUWRFVVOR MYnpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NV30W|F7OjVyNke3PFc>
115 NFr5WIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIqxfYk2KM7:TR?= M124R|Q5KGh? NGrxNVNFVVOR MUHpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= M{nCPVI2ODZ5N{i3
ACHN M{DPfmZ2dmO2aX;uJGF{e2G7 NHnaXmM2KM7:TR?= MnPPOFghcA>? M4PQOmROW09? NGXOT3VqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MoHGNlUxPjd5OEe=
Caki-2 NXjuN4tQTnWwY4Tpc44hSXO|YYm= NEXlWo42KM7:TR?= NFzxPYw1QCCq M2PvR2ROW09? M3nyR4lv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= NITFc20zPTB4N{e4Oy=>
A498 M3rUR2Z2dmO2aX;uJGF{e2G7 M4m5[lUh|ryP MkHnOFghcA>? MoHVSG1UVw>? NVP5To06cW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> M1\rclI2ODZ5N{i3
115 NEHCfJBHfW6ldHnvckBCe3OjeR?= M3XNTVUh|ryP M4X1UlQ5KGh? MoPtSG1UVw>? NFLnSo9qdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg M1vl[lI2ODZ5N{i3
MOLM-13 MUHGeY5kfGmxbjDBd5NigQ>? M4LaWlbDqM7:TR?= MX:wMVghcA>? M2OyNWROW09? M1P6Nolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIIC1N{whVUSPMjygdFIyKGGwZDDhZ4V1gWyjdHXkJJA2Ow>? NW\LO2V7OjR6OEWwPFI>
MOLM-13 NHOwUY9HfW6ldHnvckBCe3OjeR?= MnnhOuKh|ryP NY[1N25bPiCq MXPEUXNQ NF;WXo1mdmijbnPld{B1cGViYXPleJlt[XSrb36gc4YhcGm|dH;u[UBJOkJiYX7kJIhm[XRic3jvZ4sheHKxdHXpcpMhUHOyMkegZY5lKEi|cEmw NYjhfVB7OjR6OEWwPFI>
HepG2 MlrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3L2cFczKGh? NUi2b3J3TE2VTx?= NFewT2JKSzVyPUO1Mlg3KMLzIEKuPUDPxE1? MkTCNlQ5QDR6MEm=
HepG2/As MnHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnQO|IhcA>? NVPiXW1UTE2VTx?= MWfJR|UxRTZ6LkGzJOKyKDlwNjFOwG0> MkLwNlQ5QDR6MEm=
SMMC7721 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fMSlczKGh? M{f0bWROW09? MkX3TWM2OD1|MT6yPEDDuSB2LkKg{txO MlnyNlQ5QDR6MEm=
SMMC7721/Ac MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVriXGw2PzJiaB?= NHfScFlFVVOR MU\JR|UxRTV3LkKxJOKyKDVwMEOg{txO NHvOfogzPDh6NEiwPS=>
Huh-7 M2iwdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjGO|IhcA>? NXTWenNHTE2VTx?= MnTiTWM2OD1|Mz65OkDDuSB|Lkmg{txO MXSyOFg5PDhyOR?=
Hep3B MortS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDOS3U4OiCq M3ftVmROW09? M{T5W2lEPTB;MkCuNVghyrFiMT64OEDPxE1? NVL1[Fk5OjR6OES4NFk>
HepG2 M2rGdWFxd3C2b4Ppd{BCe3OjeR?= MnfTbY5lfWOnczDhdI9xfG:|aYO= MXuyOFg5PDhyOR?=
SMMC7721 NUXOOI93SXCxcITvd4l{KEG|c3H5 MUjpcoR2[2W|IHHwc5B1d3Orcx?= NYDMdYdMOjR6OES4NFk>
Huh-7 MVjBdI9xfG:|aYOgRZN{[Xl? MX3pcoR2[2W|IHHwc5B1d3Orcx?= NEe3OYIzPDh6NEiwPS=>
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MOLM M2WxUWZ2dmO2aX;uJGF{e2G7 M4TiXVExKM7:TR?= NXvsdIxlOjRiaB?= M2PtV5VxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= NGLXfW8zPDR5M{W2Ni=>
U2OS  NWq0T2piTnWwY4Tpc44hSXO|YYm= Ml;jNlAh|ryP M4XRcVI1KGh? M{LCSYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? MmDSNlQ{PjZyMEe=
RKO MYTGeY5kfGmxbjDBd5NigQ>? NXTsZ4xpOjBizszN MkXPNlQhcA>? MU\pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv NFzkc4MzPDN4NkCwOy=>
U2OS  NH7oU2ZHfW6ldHnvckBCe3OjeR?= NX;m[|dzOjBizszN M2nDVFI1KGh? M4nQRolv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u Mly5NlQ{PjZyMEe=
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SMMC-7721  MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{CzV|EvOjVvMkCg{txO M{P5U|I1NzR6L{eyJIg> NWrrWFlxTE2VTx?= MWfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MYiyOFI5PjNzMh?=
HuH-7 MWjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVLXOYZQOS5{NT2yNEDPxE1? MmDzNlQwPDhxN{KgbC=> NGXMd4RFVVOR NIfkbIZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M4LDcVI1Ojh4M{Gy
SMMC-7721  NYHGN2I3SXCxcITvd4l{KEG|c3H5 M4\TdVIxKM7:TR?= NGXMfnQ1QCCq NX63VnlHTE2VTx?= MWHpcoR2[2W|IHHwc5B1d3Orcx?= NGrRNogzPDJ6NkOxNi=>
HuH-7 MkHCRZBweHSxc3nzJGF{e2G7 MmrJNlAh|ryP M1zy[FQ5KGh? M{XRRWROW09? MlnHbY5lfWOnczDhdI9xfG:|aYO= MVeyOFI5PjNzMh?=
SMMC-7721  NVTFTZlxTnWwY4Tpc44hSXO|YYm= M4fv[|ExKM7:TR?= NGXRWHc{PiCq M4nOV2ROW09? Mm[2[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> Mn3aNlQzQDZ|MUK=
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REH NGW5O|FHfW6ldHnvckBCe3OjeR?= M1nkNVUwOTBizszN NGDOcG1t\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= MoTINlQzPDB{MEO=
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AT2 NELEOohE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFq0bo8xNTJ3IN88US=> NYjoblE5cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MUCyOFI1ODJyMx?=
REH NI[2VG9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{DaXlAuOjVizszN M2[1XolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{HqTFI1OjRyMkCz
UoCB6 MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVrFSo12OC1{NTFOwG0> MnW4bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MUSyOFI1ODJyMx?=
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H460 MoXnSpVv[3Srb36gRZN{[Xl? MVO1M|ExNzJyIN88US=> NWjrUlhkOjRiaB?= MkK5eZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? M1H2V|I1OTN4MUS3
Lovo  NWj1dHV5TnWwY4Tpc44hSXO|YYm= MUW1M|ExNzJyIN88US=> Mo\nNlQhcA>? NHvpZVJ2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= M4Szb|I1OTN4MUS3
A2780 NXG2cZhFSXCxcITvd4l{KEG|c3H5 NF;BVnM2NzFyL{KwJO69VQ>? NW\kOGduOjRiaB?= NXrEcoNH\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? M330ZlI1OTN4MUS3
H460 MUTBdI9xfG:|aYOgRZN{[Xl? M3HHV|UwOTBxMkCg{txO NVrlNYplOjRiaB?= Ml7v[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> NGrBWIIzPDF|NkG0Oy=>
Lovo  MnfxRZBweHSxc3nzJGF{e2G7 NVnvWHNJPS9zMD:yNEDPxE1? M3\mN|I1KGh? NF25SpVmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? M13Q[lI1OTN4MUS3

... 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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