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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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 M{DGVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7iOeKh|ryP NHe5SG01QMLiaB?= NHvRfoNjdG:la4OgNlcuV0iFLXnu[JVk\WRiY3XscEBxem:uaX\ldoF1cW:wIHPvcZBiemGkbHWgeI8hfGijdDDv[kBj[XOjbDDs[ZZmdHN? MlzmNlY{PTB3NkW=
NP69 M1PifWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXqTWM2OD1|MT62PeKyOi53NDFOwG0> Mn;5NlYzPTJ3N{W=
NP460 NFPscW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XDdmlEPTB;MkKuPFXDuTFwMUig{txO NU\aXGM3OjZ{NUK1O|U>
C666-1 NUDmTWZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTF7Lkm1xtE5Njl|IN88US=> Mm\NNlYzPTJ3N{W=
C666-1 MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWSxNEDDvU1? Mlm3OFghcA>? NH2wbZhFVVOR NHuxdYx{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{B1cGViY4n0c5RwgGmlIHXm[oVkfCCxZjDjbZNxdGG2aX6= NYrtUGtLOjZ{NUK1O|U>
C666-1  M2P1Z2Z2dmO2aX;uJGF{e2G7 MofDNVAhyrWP M3XxOlI1KGh? MV\EUXNQ NI[1TZdi[3SrdnH0[ZMhfGinIIC1N{Bx[XSqd3H5MEB2eHKnZ4XsZZRqdmdicEWzMEBxOjFiYX7kJG1ldTJ? M{e5VFI3OjV{NUe1
C666-1 M3\kU2Fxd3C2b4Ppd{BCe3OjeR?= MnnTNVAhyrWP MVy0PE84OiCq NWnzcXRrTE2VTx?= NH31OIh{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{BkcXOybHH0bY4ucW6mdXPl[EBieG:ydH;zbZM> NYHpV3BMOjZ{NUK1O|U>
A549 M3zqTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPnNoozPCCq NG\qZVFKSzVyPUG3MlY5KMLzIESuOVIh|ryP MWCyOlEzPTJ|MB?=
A549-NTC MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;5SG9SOjRiaB?= NFXKZmtKSzVyPUG5MlQzKMLzIEGuPVYh|ryP MlK5NlYyOjV{M{C=
A549-920 NVHhZZl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFWycGUzPCCq M1:5dWlEPTB;M{OuPFUhyrFiND64OEDPxE1? MkDMNlYyOjV{M{C=
CRL-5908 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nyOVI1KGh? NGXkOFNKSzVyPUO4MlcyKMLzIEKuOFMh|ryP NEXSUm0zPjF{NUKzNC=>
L6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zlNlExyqEQvF5CpC=> NVHPdYgyOjRxNEivO|IhcA>? MkXXSG1UVw>? NVSzSId2cW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w NEnWSowzPTh5MUe5OC=>
C2C12 MmrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[zPFExyqEQvF5CpC=> NEXxZm8zPC92OD:3NkBp MUnEUXNQ NXe5NnZmcW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w M2DDfVI2QDdzN{m0
MCF-7  NV\VdWdUTnWwY4Tpc44hSXO|YYm= MVexNOKh|ryP M4rUVWROW09? Mm\jbY5pcWKrdIOgZ5lkdGmwIFSxJIFv\CCGaXPlduKh Mnv5NlU4ODJ5MEO=
DU4475  NHGyZmlHfW6ldHnvckBCe3OjeR?= NIDLc2I2NzFyL{KwJO69VQ>? NIH4U5gzPMLiaB?= MYDkc5dvemWpdXzheIV{KFSxY3GtNUBld3OnIHTldIVv\GWwdHz5 MlqyNlU2PDdzN{S=
SMMC-7721 NX[1NmtwTnWwY4Tpc44hSXO|YYm= MmiyNVAh|ryP NF;UNWc1QCCq NXzRdVNvTE2VTx?= MWDjZZV{\XNiRF7BJGRUSiCmYX3h[4U> NIO1foQzPTV2NEO2NS=>
SMMC-7721 MXnGeY5kfGmxbjDBd5NigQ>? NYjOZ5FkOTBizszN NHu5fnY1QCCq M1LxOGROW09? NWjOOZBycW6mdXPld{B1cGViY3jyc41ifGmwLXLveY5lKHC{b4TlbY4hUU[LMU[geI8heGG{dHnhcIx6KGyxY3HsbZpmKGmwIITo[UBkgXSxcHzhd43DqA>? M3vBRlI2PTR2M{[x
SMMC-7721 MXjGeY5kfGmxbjDBd5NigQ>? MUGxNEDPxE1? NV\NWFBEPDhiaB?= NVTxfWRsTE2VTx?= NVzDN5FPcW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mxsBKTk6EMdMgcXJPSQ>? NIP3dFUzPTV2NEO2NS=>
SMMC-7721 NUjyXJh1TnWwY4Tpc44hSXO|YYm= MW[xNEDPxE1? Ml20N|YhcA>? MUPEUXNQ M1P3XINifXOnczD0bIUh\WO2b4DpZ{BmgHC{ZYPzbY9vKG:oIFnGTVE3 MVOyOVU1PDN4MR?=
MCF-7 MVvGeY5kfGmxbjDBd5NigQ>? NXPWTGJvOTEEoN88US=> MXKwMVI1KGh? NFfER4VqdmS3Y3XzJJA2OyCjbnSgdFIyN0OrcEG= MWOyOVQ5OjN5Mx?=
OVCAR10 MUHGeY5kfGmxbjDBd5NigQ>? MoLwNVDDqM7:TR?= NYDocYVkOjGqwrC= Mm\FSG1UVw>? MYfpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz MlzxNlU1OjZ3NEi=
NCI-H23 NVXZV5p2TnWwY4Tpc44hSXO|YYm= M334Z|ExyqEQvF2= M1faPVIycMLi NV;yepB5TE2VTx?= NETK[5BqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ MVmyOVQzPjV2OB?=
A2780 MkW4SpVv[3Srb36gRZN{[Xl? NXLPZnhkOTEEoN88US=> NWi3cFQ6OjGqwrC= MVXEUXNQ M1XZSYlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> M1n4dVI2PDJ4NUS4
NCI-H23 M4jteWZ2dmO2aX;uJGF{e2G7 MYKxNOKh|ryP M4HUVFIycMLi NUXwUIpsTE2VTx?= NWrlPFNX\GWlcnXhd4V{KHSqZTDGc5hOOSCuZY\lcJM> MV2yOVQzPjV2OB?=
A2780 NGTZbYNHfW6ldHnvckBCe3OjeR?= NFnNcG4yOMLizszN NH7LbXczOWkEoB?= NWnxPHBiTE2VTx?= NWDu[o86\GWlcnXhd4V{KHSqZTDGc5hOOSCuZY\lcJM> MmHwNlU1OjZ3NEi=
HCT116  M1rjUGZ2dmO2aX;uJGF{e2G7 NETI[ZcyOCEEtV2= MYWyOEBp MonWZ4F2e2W|IHGgdFU{NWSncHXu[IVvfCC2ZYTyZZBtd2mmIFexMYFzemW|dDDpckBlcXCub3nkJGhEXDFzNjDjcI9v\XNiREOgZY5lKER6 M2jEb|I2OzhyMEW1
MCF-10CA1a M4jQeGZ2dmO2aX;uJGF{e2G7 NEX2VVMyOMLizszN M4rrTlQ5KGh? Mn7JSG1UVw>? MnHkbY5pcWKrdIOgZoF{[WxiaX72ZZNqd25iYX7kJJJm\HWlZXSgWGdHNc7{Mz3pcoR2[2WmIHnueoF{cW:wIITvJIJie2GuIHzleoVtew>? NX3Wc4NJOjV{NUe3Nlk>
MCF-10A1  MmKwSpVv[3Srb36gRZN{[Xl? NFjMSnQyOMLizszN MVeyOE81QCCq MYnEUXNQ M3HOUYlvcGmkaYTzJI1q\3KjdHnvckBw\iCwb4LtZYwh[nKnYYP0JIVxcXSqZXzpZYzDqA>? Mm\BNlUzPTd5Mkm=
MCF-10CA1a NVnOcnB1TnWwY4Tpc44hSXO|YYm= M1LhWVExyqEQvF2= MofqNlQhcA>? MWTEUXNQ NIrhbVFl\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= NG[yZY8zPTJ3N{eyPS=>
MCF-10CA1a MUnGeY5kfGmxbjDBd5NigQ>? MYqxNOKh|ryP NVL1fpQ6OjRiaB?= MmrMSG1UVw>? MYTpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? MlfhNlUzPTd5Mkm=
SK-BR-7 M3WzfmZ2dmO2aX;uJGF{e2G7 MmfKNVDDqM7:TR?= M1fmV|I1KGh? MlTnSG1UVw>? MlGwbY5pcWKrdIOgJHRITi4QskOtbY5lfWOnZDDFVGhDOsLibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:w M3nrdFI2OjV5N{K5
SUM102PT NHXsO4ZHfW6ldHnvckBCe3OjeR?= NGjJ[3EyOMLizszN MlPFNlQhcA>? NHXlTGFFVVOR NELSNXZqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= NInhRnAzPTJ3N{eyPS=>
RAW 264.7 NGnWUY9HfW6ldHnvckBCe3OjeR?= Mk\GNVDDqM7:TR?= MX2zNEBucW5? MorvdJJmfmWwdIOgeIhmKHB3MzDy[YR2[3Srb36gbY4hemW|cH;ud4UhfG9iTGDT NG\HZoYzPTF5MkW0Oy=>
RAW 264.7 MUPGeY5kfGmxbjDBd5NigQ>? NFywW4kyOMLizszN Mn3SN|AhdWmw M{n5RpJm\HWlZYOgeIhmKEySUz3heYdu\W62ZXSgeIhmKE6ILd86RkBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZYN1cX[rdIm= NULuPWFmOjVzN{K1OFc>
RAW 264.7 M4fyVWZ2dmO2aX;uJGF{e2G7 NInHdJcyOMLizszN M2PGU|MxKG2rbh?= NX24NGxDcW6qaXLpeJMhVFCVLXnu[JVk\WRiTl:gdJJw\HWldHnvcuKh MlPuNlUyPzJ3NEe=
MCF7  MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWO2[ZByOi53INM1US=> MkD5OUBl NYLT[|RYTE2VTx?= NXzhOJRQe2Wwc3n0bZpmeyCPQ1[3JJRwKFCDUmCgbY5pcWKrdHnvci=> M3:wOVI2ODh3OUCy
MCF7  M3[4fGZ2dmO2aX;uJGF{e2G7 NV\E[IUxOi53INM1US=> MnXtOFghcA>? NHnveXJFVVOR NX7XfZA2\GWlcnXhd4V{KHSqZTDoc41wdG:pb4XzJGRUSiC{ZYDhbZIh\nKncYXlcoNq\XN? NFfPdmQzPTB6NUmwNi=>
ACHN NVLVO5pOS2WubDDWbYFjcWyrdImgRZN{[Xl? Mo[yNE42NTFyIN88US=> MXWwMVYh\A>? NWrMSnpbTE2VTx?= NVXRe5lzcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MXeyOVA3Pzd6Nx?=
Caki-2 NYj0TFlvS2WubDDWbYFjcWyrdImgRZN{[Xl? M4rzdFAvPS1zMDFOwG0> M4jWOVAuPiCm NUHibpZ6TE2VTx?= NF7MZ5pqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NH3wOY8zPTB4N{e4Oy=>
A498 M{LXc2NmdGxiVnnhZoltcXS7IFHzd4F6 M2TGdlAvPS1zMDFOwG0> NEXnNY8xNTZiZB?= MYnEUXNQ MYrpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{LUUVI2ODZ5N{i3
115 NF3pTlRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWPDfHRJOC53LUGwJO69VQ>? M3TpN|AuPiCm M1;JOmROW09? Moe4bY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MV[yOVA3Pzd6Nx?=
117 MlvuR4VtdCCYaXHibYxqfHliQYPzZZk> NGjGfJExNjVvMUCg{txO NFjJR4MxNTZiZB?= NF;nWWNFVVOR M{PzdYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mnq4NlUxPjd5OEe=
ACHN NUDCfmlDTnWwY4Tpc44hSXO|YYm= MnzUNE42NzFxNTFOwG0> M1vJPFQ5KGh? NH;jZ4NFVVOR M3OzWYxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz MnTKNlUxPjd5OEe=
Caki-2 NWDjZodDTnWwY4Tpc44hSXO|YYm= M3P1SFAvPS9zL{Wg{txO MX[0PEBp MmSySG1UVw>? NYPDSWFMdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NH72[nIzPTB4N{e4Oy=>
A498 NVe1ZndRTnWwY4Tpc44hSXO|YYm= MYGwMlUwOS93IN88US=> MUK0PEBp NGnjSJNFVVOR NGPrUWZt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NH7Fe2EzPTB4N{e4Oy=>
115 MVHGeY5kfGmxbjDBd5NigQ>? NUS3[VU4OC53L{GvOUDPxE1? MWS0PEBp MYPEUXNQ NFzEbXRt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NUDifFIyOjVyNke3PFc>
ACHN MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHs[JE2KM7:TR?= M2fHXlQ5KGh? NVzrW4hzTE2VTx?= NX3uTlhRcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MmPpNlUxPjd5OEe=
Caki-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWW1JO69VQ>? M1\GTlQ5KGh? MnzoSG1UVw>? MlX5bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg M{KwV|I2ODZ5N{i3
A498 M1rw[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO1JO69VQ>? M2XjOFQ5KGh? MmXvSG1UVw>? M2i2Solv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NGLRPGEzPTB4N{e4Oy=>
115 M4fGfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PjUFUh|ryP NWmyOYFjPDhiaB?= NVHifXg3TE2VTx?= MX\pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MnLyNlUxPjd5OEe=
ACHN MVTGeY5kfGmxbjDBd5NigQ>? M1m3bVUh|ryP MnvPOFghcA>? MWTEUXNQ MkXzbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NI\wTYQzPTB4N{e4Oy=>
Caki-2 NHTzcG5HfW6ldHnvckBCe3OjeR?= NHrQUGY2KM7:TR?= NYHqNI5rPDhiaB?= Mlm2SG1UVw>? NHrmTYNqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg M2\5UVI2ODZ5N{i3
A498 NISzVJBHfW6ldHnvckBCe3OjeR?= M{PJVFUh|ryP NH3tOZM1QCCq NXfnSo1pTE2VTx?= MWDpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MnO0NlUxPjd5OEe=
115 NGTSVIJHfW6ldHnvckBCe3OjeR?= M3\u[lUh|ryP MofNOFghcA>? NVjodZhDTE2VTx?= Mn7KbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MXqyOVA3Pzd6Nx?=
MOLM-13 NH74UYxHfW6ldHnvckBCe3OjeR?= MVG2xsDPxE1? MlL0NE05KGh? NW\NV2lSTE2VTx?= NIrubYZqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjDwOVMtKE2GTUKsJJAzOSCjbnSgZYNmfHmuYYTl[EBxPTN? MojMNlQ5QDVyOEK=
MOLM-13 M3zDZmZ2dmO2aX;uJGF{e2G7 MnHDOuKh|ryP M{LrflYhcA>? MkezSG1UVw>? NGL0[5BmdmijbnPld{B1cGViYXPleJlt[XSrb36gc4YhcGm|dH;u[UBJOkJiYX7kJIhm[XRic3jvZ4sheHKxdHXpcpMhUHOyMkegZY5lKEi|cEmw NGKyclczPDh6NUC4Ni=>
HepG2 NYq4UWJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDVdJdQPzJiaB?= M1jkRWROW09? NXvJSJhHUUN3ME2zOU45PiEEsTCyMlkh|ryP NHPmdZEzPDh6NEiwPS=>
HepG2/As M4r6TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnP2O|IhcA>? NXrkNFZFTE2VTx?= MUDJR|UxRTZ6LkGzJOKyKDlwNjFOwG0> NEHtW3QzPDh6NEiwPS=>
SMMC7721 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjLO|IhcA>? M4rVe2ROW09? NUexdZE{UUN3ME2zNU4zQCEEsTC0MlIh|ryP MmnKNlQ5QDR6MEm=
SMMC7721/Ac NVy0eZpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV23NkBp NVLCXohFTE2VTx?= MkXzTWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? MnzZNlQ5QDR6MEm=
Huh-7 M1jkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPhcWs4OiCq NGTRUpBFVVOR MkH3TWM2OD1|Mz65OkDDuSB|Lkmg{txO MWOyOFg5PDhyOR?=
Hep3B NEjLTJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYntUJFJPzJiaB?= MmDvSG1UVw>? MljjTWM2OD1{MD6xPEDDuSBzLki0JO69VQ>? NUiydJNUOjR6OES4NFk>
HepG2 MWTBdI9xfG:|aYOgRZN{[Xl? M162S4lv\HWlZYOgZZBweHSxc3nz MX2yOFg5PDhyOR?=
SMMC7721 MoPSRZBweHSxc3nzJGF{e2G7 NIn3XIlqdmS3Y3XzJIFxd3C2b4Ppdy=> M{CwXFI1QDh2OEC5
Huh-7 MlXERZBweHSxc3nzJGF{e2G7 NYnx[Jc2cW6mdXPld{BieG:ydH;zbZM> NFjRVXAzPDh6NEiwPS=>
Hep3B M3vFdWFxd3C2b4Ppd{BCe3OjeR?= Ml\SbY5lfWOnczDhdI9xfG:|aYO= MlSxNlQ5QDR6MEm=
U2OS  MX7GeY5kfGmxbjDBd5NigQ>? MUOyNEDPxE1? M37zWVI1KGh? M{iyV4lv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= MYmyOFg3PzJ3OR?=
AML2 MmjERZBweHSxc3nzJGF{e2G7 NX6wOY45Oi9zMDFOwG0> M1\kUFI1NzR6IHi= NF7yZYxqdmS3Y3XzJIFxd3C2b4Ppdy=> Mnz6NlQ3PTl5NEm=
MOML13 NX;lOYZMSXCxcITvd4l{KEG|c3H5 NGLtXXMzNzFyIN88US=> NGnJcYEzPC92ODDo NIjYNnFqdmS3Y3XzJIFxd3C2b4Ppdy=> MYSyOFY2QTd2OR?=
AML2 NX60[pNoTnWwY4Tpc44hSXO|YYm= NXK3bJlGOTEQvF2= NXzuOm1sOi92IHi= NHLSb3RqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> M4LUPFI1PjV7N{S5
AML3 NVXxeZpkTnWwY4Tpc44hSXO|YYm= MoDqNVDPxE1? MYiyM|QhcA>? NWPIZWpLcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NVz0WphROjR4NUm3OFk>
MOML13 MoTKSpVv[3Srb36gRZN{[Xl? Mn\4NVDPxE1? NFXQOHczNzRiaB?= MW\pcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= NUf6RWNqOjR4NUm3OFk>
BeWo MlexSpVv[3Srb36gRZN{[Xl? MVmzNEDDvU1? M2riflI1KGh? NYXzb2RocW6lcnXhd4V{KHB3MzygUYRuOixicEKxJIFv\CCSdX3hJIF1KHSqZTDwdo91\WmwIHzleoVt MlHyNlQ1QThzNUS=
BeWo NHO3cpBCeG:ydH;zbZMhSXO|YYm= NEfQVFQ{OCEEtV2= MXuyOEBp NVW2dlVncW6lcnXhd4V{KGGyb4D0c5Nqew>? M3HPdlI1PDl6MUW0
OCI MUTGeY5kfGmxbjDBd5NigQ>? NVrtV291OTBizszN NF2zWVAzPCCq NInEUpp2eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= MX6yOFQ4OzV4Mh?=
MOLM MmXtSpVv[3Srb36gRZN{[Xl? MXWxNEDPxE1? Ml7lNlQhcA>? MkHXeZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w M{XBeFI1PDd|NU[y
U2OS  MX7GeY5kfGmxbjDBd5NigQ>? M1HVVVIxKM7:TR?= NFv4bIIzPCCq Mnv5bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? Ml35NlQ{PjZyMEe=
RKO Ml\ySpVv[3Srb36gRZN{[Xl? MoPFNlAh|ryP MViyOEBp MUTpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv NIj6bnkzPDN4NkCwOy=>
U2OS  NVHi[oNuTnWwY4Tpc44hSXO|YYm= M2\TcFIxKM7:TR?= M{\XR|I1KGh? MUHpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= NYjZOVVlOjR|Nk[wNFc>
RKO NHzIPHFHfW6ldHnvckBCe3OjeR?= NXPROXhiOjBizszN MXSyOEBp NXfEbVJZcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> M2[0ZVI1OzZ4MEC3
SMMC-7721  NIW2cIpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M13FSlEvOjVvMkCg{txO MmDZNlQwPDhxN{KgbC=> MYTEUXNQ MUHpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NXK4VmVkOjR{OE[zNVI>
HuH-7 Mn:5R4VtdCCYaXHibYxqfHliQYPzZZk> NEPa[XIyNjJ3LUKwJO69VQ>? M3TJVVI1NzR6L{eyJIg> MkTlSG1UVw>? MnLlbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NVjVSW9iOjR{OE[zNVI>
SMMC-7721  MVfBdI9xfG:|aYOgRZN{[Xl? MV:yNEDPxE1? MWS0PEBp Mo\tSG1UVw>? MXTpcoR2[2W|IHHwc5B1d3Orcx?= MV[yOFI5PjNzMh?=
HuH-7 NEPBVGRCeG:ydH;zbZMhSXO|YYm= NXyw[FVDOjBizszN NFewbYU1QCCq M1KxVmROW09? MV\pcoR2[2W|IHHwc5B1d3Orcx?= NU\TcZdMOjR{OE[zNVI>
SMMC-7721  Ml;XSpVv[3Srb36gRZN{[Xl? MoL6NVAh|ryP NIO3[oY{PiCq NETZOFVFVVOR NVTJS5Ex\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? MofGNlQzQDZ|MUK=
HuH-7 NWeyNogyTnWwY4Tpc44hSXO|YYm= MYqxNEDPxE1? Mm[wN|YhcA>? NETtcHlFVVOR NVf5SJZu\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? MkDiNlQzQDZ|MUK=
AT2 NI\oblZHfW6ldHnvckBCe3OjeR?= NIjYcYE2NzFyIN88US=> MUjs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? NXvOeWtpOjR{NECyNFM>
REH NUTDTItETnWwY4Tpc44hSXO|YYm= M2TrUVUwOTBizszN MV;s[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? MYOyOFI1ODJyMx?=
UoCB6 M{\yWGZ2dmO2aX;uJGF{e2G7 M163RlUwOTBizszN NV\CZ2J3dGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NELQcWUzPDJ2MEKwNy=>
AT2 NFjvNYJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUXIXZE3OC1{NTFOwG0> NUHUeYxrcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MVuyOFI1ODJyMx?=
REH M3\sOGNmdGxiVnnhZoltcXS7IFHzd4F6 MViwMVI2KM7:TR?= MlrabY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NXm3eZNwOjR{NECyNFM>
UoCB6 M2nJR2NmdGxiVnnhZoltcXS7IFHzd4F6 NWTjRldqOC1{NTFOwG0> MYLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFfVOo4zPDJ2MEKwNy=>
A2780 MnvWSpVv[3Srb36gRZN{[Xl? Mm\GOU8yOC9{MDFOwG0> NYfWTIZmOjRiaB?= NGjORVR2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= MlPpNlQyOzZzNEe=
H460 NWjxWHI{TnWwY4Tpc44hSXO|YYm= Ml;2OU8yOC9{MDFOwG0> NYjOblRtOjRiaB?= NI\3T|B2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= NHTsfmwzPDF|NkG0Oy=>
Lovo  M3vC[WZ2dmO2aX;uJGF{e2G7 NVWwRoZCPS9zMD:yNEDPxE1? NUjNNIJ2OjRiaB?= M4ryepVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NXvZW2RvOjRzM{[xOFc>
A2780 M{\4SGFxd3C2b4Ppd{BCe3OjeR?= NGq4W5k2NzFyL{KwJO69VQ>? NGLPb4QzPCCq Mn\F[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MWiyOFE{PjF2Nx?=
H460 NX76O5BwSXCxcITvd4l{KEG|c3H5 MXe1M|ExNzJyIN88US=> NIjMVnUzPCCq MV;lcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> MmXENlQyOzZzNEe=
Lovo  MVzBdI9xfG:|aYOgRZN{[Xl? MUK1M|ExNzJyIN88US=> M3XGOlI1KGh? NYTjbnYy\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? MXWyOFE{PjF2Nx?=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (171.96 mM)
Ethanol 30 mg/mL (51.59 mM)
Water <1 mg/mL
* <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

文献中の引用 (9)

Frequently Asked Questions

  • Question 1
    Is this a racemic mixture of Nutlin-3a and Nutlin-3b or just the Nutlin-3a enantiomer?

    Answer: It is a racemate.

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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* 必須

Related Mdm2 阻害剤

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    Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor.

  • MI-773 (SAR405838)

    MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

  • A-1210477

    A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.

  • NSC 207895

    NSC 207895が、リポーター・ベースの薬ふるい分けを通してのMDMX抑制器として発見されます。MDMXは、p53とMDM2(E3リガーゼ)を管理します。

  • Nutlin-3a

    Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM.

    Features:Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.

  • Nutlin-3b

    Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

  • YH239-EE

    YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

  • Z-VAD-FMK

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    Features:A key compound for apoptosis studies.

  • ABT-263 (Navitoclax)

    ABT-263(Navitoclax)は、 Bcl-xLBcl-2Bcl-w の強力な阻害剤で、Kiがそれぞれ ≤ 0.5 nM、≤1 nM 、≤ 1 nMです。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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