Nutlin-3 化学構造
分子量: 581.5

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Quality Control & MSDS

製品説明

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    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 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYqybmF3PcLizszN MWC0POKhcA>? MnjCZoxw[2u|IEK3MW9JSy2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiClb33wZZJi[mynIITvJJRp[XRib3[gZoF{[WxibHX2[Yx{ M37BclI3OzVyNU[1
NP69 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTNzLk[5xtEzNjV2IN88US=> NULhXnhLOjZ{NUK1O|U>
NP460 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXO2SW92UUN3ME2yNk45PcLzMT6xPEDPxE1? MXOyOlI2OjV5NR?=
C666-1 NVzoW4VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\zfVg6UUN3ME2xPU46PcLzOD65N{DPxE1? NHzOXlYzPjJ3MkW3OS=>
C666-1 Ml7YR4VtdCCYaXHibYxqfHliQYPzZZk> NYPDS|BFOTBiwsXN M4\jOFQ5KGh? MWPEUXNQ MlT4d4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:geIhmKGO7dH;0c5hq[yCnZn\lZ5Qhd2ZiY3nzdIxifGmw NXL3XGNTOjZ{NUK1O|U>
C666-1  MYHGeY5kfGmxbjDBd5NigQ>? M2fie|ExKML3TR?= MVyyOEBp M2nkVGROW09? NITsU5Bi[3SrdnH0[ZMhfGinIIC1N{Bx[XSqd3H5MEB2eHKnZ4XsZZRqdmdicEWzMEBxOjFiYX7kJG1ldTJ? MonGNlYzPTJ3N{W=
C666-1 MYLBdI9xfG:|aYOgRZN{[Xl? MXGxNEDDvU1? NH\zW2E1QC95MjDo NHzm[3NFVVOR Mk[wd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:gZ4l{eGyjdHnuMYlv\HWlZXSgZZBweHSxc3nz NX\qdodkOjZ{NUK1O|U>
A549 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\HNlQhcA>? MkPzTWM2OD1zNz62PEDDuSB2LkWyJO69VQ>? M2nDRlI3OTJ3MkOw
A549-NTC M1zhZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLFN3NUOjRiaB?= MkfXTWM2OD1zOT60NkDDuSBzLkm2JO69VQ>? M4L3fVI3OTJ3MkOw
A549-920 NInab2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzMO4xLOjRiaB?= MX\JR|UxRTN|Lki1JOKyKDRwOESg{txO NHvETFYzPjF{NUKzNC=>
CRL-5908 M33M[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3Ze2xzOjRiaB?= M4XmdWlEPTB;M{iuO|EhyrFiMj60N{DPxE1? M3zDfFI3OTJ3MkOw
L6 NEfNepFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHsS5QyOMLizszNxsA> MofzNlQwPDhxN{KgbC=> NEfSOHZFVVOR MmX3bY5pcWKrdIOgZ4VtdHNicILvcIln\XKjdHnvckBidmRiZHnm[oVz\W62aXH0bY9v NF:2[4czPTh5MUe5OC=>
C2C12 M2XSZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDWNVDDqM7:TdMg NEP2S2YzPC92OD:3NkBp M37xNmROW09? MVvpcohq[mm2czDj[YxteyCycn;sbYZmemG2aX;uJIFv\CCmaX\m[ZJmdnSrYYTpc44> NWjGXHBPOjV6N{G3PVQ>
MCF-7  M4rZSmZ2dmO2aX;uJGF{e2G7 MW[xNOKh|ryP NFfNeXpFVVOR MnnQbY5pcWKrdIOgZ5lkdGmwIFSxJIFv\CCGaXPlduKh NXHG[oJYOjV5MEK3NFM>
DU4475  MkXkSpVv[3Srb36gRZN{[Xl? M4S5S|UwOTBxMkCg{txO NFzId5YzPMLiaB?= NUL4T|Ny\G:5boLl[5Vt[XSnczDUc4NiNTFiZH;z[UBl\XCnbnTlcpRtgQ>? NFzoU3czPTV2N{G3OC=>
SMMC-7721 M{D2T2Z2dmO2aX;uJGF{e2G7 MUWxNEDPxE1? NUCxRZNUPDhiaB?= M3rKe2ROW09? M3TZeINifXOnczDEUmEhTFOEIHThcYFo\Q>? MkW2NlU2PDR|NkG=
SMMC-7721 NFXxPWZHfW6ldHnvckBCe3OjeR?= MVOxNEDPxE1? NU\xdYtSPDhiaB?= M3jsUmROW09? M3r6PYlv\HWlZYOgeIhmKGOqcn;tZZRqdi2kb4Xu[EBxem:2ZXnuJGlHUTF4IITvJJBienSrYXzsfUBtd2OjbHn6[UBqdiC2aHWgZ5l1d3CuYYPtxsA> NFn5fIgzPTV2NEO2NS=>
SMMC-7721 NWXnN|RpTnWwY4Tpc44hSXO|YYm= NFPvTnkyOCEQvF2= MVG0PEBp NYiwV4RDTE2VTx?= MkPibY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:owrDJSm5DOcLibWLORS=> MXeyOVU1PDN4MR?=
SMMC-7721 NU\0S4doTnWwY4Tpc44hSXO|YYm= NG\YNo8yOCEQvF2= NIDZPZE{PiCq M4DRW2ROW09? MmHvZ4F2e2W|IITo[UBm[3SxcHnjJIV5eHKnc4Ppc44hd2ZiSV\JNVY> MYGyOVU1PDN4MR?=
MCF-7 NWDlN5lTTnWwY4Tpc44hSXO|YYm= NYL6cYdFOTEEoN88US=> NYXhPZZDOC1{NDDo NVy5[nlucW6mdXPld{BxPTNiYX7kJJAzOS:FaYCx MnewNlU1QDJ|N{O=
OVCAR10 MWHGeY5kfGmxbjDBd5NigQ>? NYnFbHVbOTEEoN88US=> NFnVOGUzOWkEoB?= NX7CXpFTTE2VTx?= NYrhWW1LcW6lcnXhd4V{KHB3MzDwdo91\WmwIHzleoVtew>? MYCyOVQzPjV2OB?=
NCI-H23 NUm5WWdGTnWwY4Tpc44hSXO|YYm= M{jwPVExyqEQvF2= NVTwVplOOjGqwrC= MnK4SG1UVw>? MonPbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NILGbJEzPTR{NkW0PC=>
A2780 NXn1cVFnTnWwY4Tpc44hSXO|YYm= NFfJSHQyOMLizszN MkHvNlFpyqB? NYW5RnBQTE2VTx?= MXnpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz NFrRWlkzPTR{NkW0PC=>
NCI-H23 NVu0W5J7TnWwY4Tpc44hSXO|YYm= NIjnSYoyOMLizszN MXiyNYjDqA>? NFq0[5ZFVVOR NV\ncItn\GWlcnXhd4V{KHSqZTDGc5hOOSCuZY\lcJM> MXuyOVQzPjV2OB?=
A2780 MWfGeY5kfGmxbjDBd5NigQ>? MX6xNOKh|ryP M2jkRVIycMLi M{HUbGROW09? M13yR4Rm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz MYOyOVQzPjV2OB?=
HCT116  M1izRmZ2dmO2aX;uJGF{e2G7 NIP0ZnUyOCEEtV2= NFHUPXIzPCCq NWrHdXBC[2G3c3XzJIEheDV|LXTldIVv\GWwdDD0[ZRz[XCub3nkJGcyNWG{cnXzeEBqdiCmaYDsc4llKEiFVEGxOkBkdG:wZYOgSFMh[W6mIFS4 MYKyOVM5ODB3NR?=
MCF-10CA1a Ml\ISpVv[3Srb36gRZN{[Xl? MVixNOKh|ryP NIPNeYY1QCCq MULEUXNQ MVrpcohq[mm2czDiZZNidCCrbo\hd4lwdiCjbnSgdoVlfWOnZDDUS2Yu|rJ|LXnu[JVk\WRiaX72ZZNqd25idH:gZoF{[WxibHX2[Yx{ NYTPdm9LOjV{NUe3Nlk>
MCF-10A1  NI\JXWRHfW6ldHnvckBCe3OjeR?= NXXvU4JiOTEEoN88US=> NX62cpdzOjRxNEigbC=> MkHySG1UVw>? NXGxXnp1cW6qaXLpeJMhdWmpcnH0bY9vKG:oIH7vdo1idCCkcnXhd5Qh\XCrdHjlcIlidMLi M13CVFI2OjV5N{K5
MCF-10CA1a NYjueY86TnWwY4Tpc44hSXO|YYm= MnnMNVDDqM7:TR?= M3n2RVI1KGh? MlTVSG1UVw>? M{DkUIRm[3KnYYPld{B1cGViVFfGMe6zOy2rbnT1Z4VlKG2UTlGgcIV3\Wy|IH;mUW1ROi{EoF3NVFktKGGwZNMgbY51\We{aX9CpO6zyqB| NXHucHZ[OjV{NUe3Nlk>
MCF-10CA1a NFuz[3FHfW6ldHnvckBCe3OjeR?= MWSxNOKh|ryP NU\vT2lbOjRiaB?= MoXrSG1UVw>? MWDpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? M2\lZ|I2OjV5N{K5
SK-BR-7 NX\LV5lVTnWwY4Tpc44hSXO|YYm= MnzvNVDDqM7:TR?= NF\Td40zPCCq NVHTSYEyTE2VTx?= NYXo[HlWcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MnvHNlUzPTd5Mkm=
SUM102PT MkmySpVv[3Srb36gRZN{[Xl? MoezNVDDqM7:TR?= NVT1NHRnOjRiaB?= NEDzd|RFVVOR NF7Hbo1qdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= MX:yOVI2Pzd{OR?=
RAW 264.7 MmflSpVv[3Srb36gRZN{[Xl? NVHDW|B3OTEEoN88US=> MoTxN|AhdWmw NVLGOnNEeHKndnXueJMhfGinIIC1N{Bz\WS3Y4Tpc44hcW5icnXzdI9ve2VidH:gUHBU NH;qWVMzPTF5MkW0Oy=>
RAW 264.7 MYnGeY5kfGmxbjDBd5NigQ>? M3zKPVExyqEQvF2= NYXOfohwOzBibXnu M4i0U5Jm\HWlZYOgeIhmKEySUz3heYdu\W62ZXSgeIhmKE6ILd86RkBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZYN1cX[rdIm= NILyOpozPTF5MkW0Oy=>
RAW 264.7 MmrmSpVv[3Srb36gRZN{[Xl? M37qbFExyqEQvF2= MUezNEBucW5? NXyzUWhjcW6qaXLpeJMhVFCVLXnu[JVk\WRiTl:gdJJw\HWldHnvcuKh MXeyOVE4OjV2Nx?=
MCF7  MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVmyMlUhyrWP MYS1JIQ> MkHNSG1UVw>? NYWyZlNMe2Wwc3n0bZpmeyCPQ1[3JJRwKFCDUmCgbY5pcWKrdHnvci=> MY[yOVA5PTlyMh?=
MCF7  M2O4WmZ2dmO2aX;uJGF{e2G7 M1XvSlIvPSEEtV2= Mnn1OFghcA>? Mm\WSG1UVw>? NVnxU2Rt\GWlcnXhd4V{KHSqZTDoc41wdG:pb4XzJGRUSiC{ZYDhbZIh\nKncYXlcoNq\XN? MnjpNlUxQDV7MEK=
ACHN MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{KyO|AvPS1zMDFOwG0> MWKwMVYh\A>? NEi2W|dFVVOR MoDKbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXKyOVA3Pzd6Nx?=
Caki-2 NIX4N3lE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWHzWmpmOC53LUGwJO69VQ>? MXmwMVYh\A>? NV\tbmJITE2VTx?= NWOxcIVxcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NYm1Z4pbOjVyNke3PFc>
A498 MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHu0UGExNjVvMUCg{txO M3fqOFAuPiCm Mn\TSG1UVw>? MnTzbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXTSb2hVOjVyNke3PFc>
115 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NV3kbHpIOC53LUGwJO69VQ>? NF7o[I8xNTZiZB?= NIXrNWNFVVOR MmTybY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M3XtVFI2ODZ5N{i3
117 MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnvhNE42NTFyIN88US=> MYWwMVYh\A>? NIr2NXNFVVOR NV7VW3lbcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MYKyOVA3Pzd6Nx?=
ACHN MnfySpVv[3Srb36gRZN{[Xl? NXHLcmg{OC53L{GvOUDPxE1? NV;VSHdjPDhiaB?= NGT1bWFFVVOR MknHcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? MlLONlUxPjd5OEe=
Caki-2 MV7GeY5kfGmxbjDBd5NigQ>? M{Hzd|AvPS9zL{Wg{txO Mmj0OFghcA>? MnHnSG1UVw>? MoS1cIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? M1m5dVI2ODZ5N{i3
A498 Mn7CSpVv[3Srb36gRZN{[Xl? MmroNE42NzFxNTFOwG0> NWfuU49RPDhiaB?= MVHEUXNQ M3mxTIxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz NH\2UmszPTB4N{e4Oy=>
115 NVfJdWdwTnWwY4Tpc44hSXO|YYm= MkTBNE42NzFxNTFOwG0> NEDvfGo1QCCq NWHUWJhJTE2VTx?= MXrs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MVOyOVA3Pzd6Nx?=
ACHN NVyyNY1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvR[WlpPSEQvF2= MUK0PEBp M2S1OmROW09? MXXpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MYiyOVA3Pzd6Nx?=
Caki-2 M2n1Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37JXlUh|ryP MXG0PEBp MXHEUXNQ NULGWVVvcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NVPW[HlSOjVyNke3PFc>
A498 M325UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjoWoc2KM7:TR?= MW[0PEBp Ml7xSG1UVw>? M1rqVYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MmnhNlUxPjd5OEe=
115 NY\5epdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;LVFQ2KM7:TR?= NV7MTGIzPDhiaB?= M{XCemROW09? M2LMN4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> M3vJXVI2ODZ5N{i3
ACHN NIf2eIVHfW6ldHnvckBCe3OjeR?= NXK0NZZ1PSEQvF2= NIPaZXY1QCCq Mln0SG1UVw>? Mlu3bY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= M2O3XlI2ODZ5N{i3
Caki-2 NXnNRW1QTnWwY4Tpc44hSXO|YYm= M{LwT|Uh|ryP NYG0VJY4PDhiaB?= MW\EUXNQ NYm5dG5ycW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> NGPncoozPTB4N{e4Oy=>
A498 MnexSpVv[3Srb36gRZN{[Xl? MoLWOUDPxE1? NXLxUopLPDhiaB?= NUnWR2VCTE2VTx?= MXPpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MonRNlUxPjd5OEe=
115 M1jpWWZ2dmO2aX;uJGF{e2G7 NEi5bGc2KM7:TR?= MYS0PEBp MmCzSG1UVw>? NEPmXZJqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg M3PxT|I2ODZ5N{i3
MOLM-13 MXjGeY5kfGmxbjDBd5NigQ>? NXzjc254PsLizszN NF;yN5AxNThiaB?= MlPhSG1UVw>? NGDoTFNqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjDwOVMtKE2GTUKsJJAzOSCjbnSgZYNmfHmuYYTl[EBxPTN? MXiyOFg5PTB6Mh?=
MOLM-13 Mo\jSpVv[3Srb36gRZN{[Xl? MVi2xsDPxE1? NWDzWWVUPiCq NX\sTGdpTE2VTx?= M133SIVvcGGwY3XzJJRp\SCjY3X0fYxifGmxbjDv[kBpcXO2b37lJGgzSiCjbnSgbIVifCC|aH;jb{Bxem:2ZXnud{BJe3B{NzDhcoQhUHOyOUC= NXe2RWZLOjR6OEWwPFI>
HepG2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MormO|IhcA>? NFfGfZpFVVOR NWTY[5RIUUN3ME2zOU45PiEEsTCyMlkh|ryP NXrWZXZjOjR6OES4NFk>
HepG2/As MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nCe|czKGh? M3TufWROW09? MonETWM2OD14OD6xN{DDuSB7Lk[g{txO NF3ZeVAzPDh6NEiwPS=>
SMMC7721 NVrnV4pCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:5O|IhcA>? Mn62SG1UVw>? NYXwPG9YUUN3ME2zNU4zQCEEsTC0MlIh|ryP MVeyOFg5PDhyOR?=
SMMC7721/Ac MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzIO|IhcA>? NIHVZYxFVVOR MV;JR|UxRTV3LkKxJOKyKDVwMEOg{txO Ml\INlQ5QDR6MEm=
Huh-7 NIS5UJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUi3NkBp MYHEUXNQ NIXuWGlKSzVyPUOzMlk3KMLzIEOuPUDPxE1? MnTRNlQ5QDR6MEm=
Hep3B M4\Lbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYOxR|FTPzJiaB?= NX3tSIMyTE2VTx?= NFX3[oFKSzVyPUKwMlE5KMLzIEGuPFQh|ryP M3eyVlI1QDh2OEC5
HepG2 NVzGXotZSXCxcITvd4l{KEG|c3H5 M3;Edolv\HWlZYOgZZBweHSxc3nz MmrENlQ5QDR6MEm=
SMMC7721 NF\FN5RCeG:ydH;zbZMhSXO|YYm= NHfLUHNqdmS3Y3XzJIFxd3C2b4Ppdy=> NHvkbm4zPDh6NEiwPS=>
Huh-7 M1qxXWFxd3C2b4Ppd{BCe3OjeR?= M4K5U4lv\HWlZYOgZZBweHSxc3nz NEPNWmMzPDh6NEiwPS=>
Hep3B NVzS[nhJSXCxcITvd4l{KEG|c3H5 Mn;xbY5lfWOnczDhdI9xfG:|aYO= M1;uflI1QDh2OEC5
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BeWo NIfDdnFCeG:ydH;zbZMhSXO|YYm= MYmzNEDDvU1? NH;5cHgzPCCq MYfpcoNz\WG|ZYOgZZBweHSxc3nz NVPzVmFzOjR2OUixOVQ>
OCI NUH6[JJYTnWwY4Tpc44hSXO|YYm= M3noRlExKM7:TR?= NXn2cmtxOjRiaB?= NHfwfmx2eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= M{PwOlI1PDd|NU[y
MOLM MWjGeY5kfGmxbjDBd5NigQ>? MWqxNEDPxE1? NYnhNG4zOjRiaB?= MYj1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? M1jOcFI1PDd|NU[y
U2OS  M{i3V2Z2dmO2aX;uJGF{e2G7 NGjMcZczOCEQvF2= MmriNlQhcA>? MX\pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv NHvQNHkzPDN4NkCwOy=>
RKO NFLCW5hHfW6ldHnvckBCe3OjeR?= M4i1[lIxKM7:TR?= MnPZNlQhcA>? MmjKbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? NXSx[JFwOjR|Nk[wNFc>
U2OS  M1W5e2Z2dmO2aX;uJGF{e2G7 MWeyNEDPxE1? NFTVe5gzPCCq NWmzW|JWcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MVmyOFM3PjByNx?=
RKO M2HETmZ2dmO2aX;uJGF{e2G7 MnT1NlAh|ryP NX7YbVlIOjRiaB?= NHvh[WNqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> M3q5W|I1OzZ4MEC3
SMMC-7721  NWTxfIJbS2WubDDWbYFjcWyrdImgRZN{[Xl? NWTlcZF1OS5{NT2yNEDPxE1? NIrFflEzPC92OD:3NkBp NHfIfpRFVVOR NU\SWZp2cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> Mlu1NlQzQDZ|MUK=
HuH-7 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEHieHAyNjJ3LUKwJO69VQ>? Mki2NlQwPDhxN{KgbC=> MXPEUXNQ NGrpNnJqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MXyyOFI5PjNzMh?=
SMMC-7721  NGjn[5lCeG:ydH;zbZMhSXO|YYm= NGjaeJAzOCEQvF2= NYi0V5FEPDhiaB?= NHq5U3hFVVOR MULpcoR2[2W|IHHwc5B1d3Orcx?= MlPPNlQzQDZ|MUK=
HuH-7 MULBdI9xfG:|aYOgRZN{[Xl? NWfGcWFXOjBizszN MX60PEBp M33jdWROW09? MlP4bY5lfWOnczDhdI9xfG:|aYO= MnnWNlQzQDZ|MUK=
SMMC-7721  NVvz[2pTTnWwY4Tpc44hSXO|YYm= NVqzenUyOTBizszN M{PnclM3KGh? M1LJS2ROW09? NXHSSGtN\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? MVKyOFI5PjNzMh?=
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AT2 NGDDTVBHfW6ldHnvckBCe3OjeR?= MoXhOU8yOCEQvF2= NFHDcY1t\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= NYDMclhJOjR{NECyNFM>
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UoCB6 M3PHOGZ2dmO2aX;uJGF{e2G7 MmPiOU8yOCEQvF2= Mn3JcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? M1;0PFI1OjRyMkCz
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Lovo  NXzVZXJGTnWwY4Tpc44hSXO|YYm= MYW1M|ExNzJyIN88US=> MlTWNlQhcA>? M37nSZVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NUDnboo5OjRzM{[xOFc>
A2780 NIfrOolCeG:ydH;zbZMhSXO|YYm= NEi2XYw2NzFyL{KwJO69VQ>? MlKyNlQhcA>? Ml\0[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> NGTSdnYzPDF|NkG0Oy=>
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... 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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