Nutlin-3

Nutlin-3は一種の有効で、選択性的なMdm2 (自身とp53に対するRING finger-dependent ubiquitin protein ligase) 拮抗剤で、無細胞試験でIC50値が90 nMですが、p53欠陥細胞中のp73を安定させられます。

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電話番号: + 81 3-5632-9610mail@cosmobio.co.jp

Nutlin-3 化学構造
分子量: 581.5

高品質保証

カスタマーフィードバック(3)

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は一種の有効で、選択性的なMdm2 (自身とp53に対するRING finger-dependent ubiquitin protein ligase) 拮抗剤で、無細胞試験でIC50値が90 nMですが、p53欠陥細胞中のp73を安定させられます。
ターゲット

Mdm2

IC50

180 nM [5]

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 NEPadXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nwTlXDqM7:TR?= MUC0POKhcA>? NHnhZZpjdG:la4OgNlcuV0iFLXnu[JVk\WRiY3XscEBxem:uaX\ldoF1cW:wIHPvcZBiemGkbHWgeI8hfGijdDDv[kBj[XOjbDDs[ZZmdHN? NX\HbnFyOjZ|NUC1OlU>
NP69 M4D1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXz0[IdTUUN3ME2zNU43QcLzMj61OEDPxE1? Mm\KNlYzPTJ3N{W=
NP460 NF3se3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfLN|hKSzVyPUKyMlg2yrFzLkG4JO69VQ>? MUCyOlI2OjV5NR?=
C666-1 NVjjW45vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTF7Lkm1xtE5Njl|IN88US=> NGPtTJAzPjJ3MkW3OS=>
C666-1 MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkPqNVAhyrWP NFTxSHg1QCCq MmnWSG1UVw>? NY\DN5pse2Wwc3n0bZpmeyCFNk[2MVEh[2WubIOgeI8hfGinIHP5eI91d3irYzDl[oZm[3Rib3[gZ4l{eGyjdHnu MYSyOlI2OjV5NR?=
C666-1  M4fQfmZ2dmO2aX;uJGF{e2G7 NIP4O4IyOCEEtV2= NEDOXIQzPCCq NU\JSopUTE2VTx?= M{fVSIFkfGm4YYTld{B1cGVicEWzJJBifGi5YYmsJJVxemWpdXzheIlv\yCyNUOsJJAzOSCjbnSgUYRuOg>? MoPvNlYzPTJ3N{W=
C666-1 MnfaRZBweHSxc3nzJGF{e2G7 NF3ISI4yOCEEtV2= NEH0cGM1QC95MjDo NGPJenpFVVOR MoDPd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:gZ4l{eGyjdHnuMYlv\HWlZXSgZZBweHSxc3nz NEfYXpgzPjJ3MkW3OS=>
A549 Mlr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDONllqOjRiaB?= NXHNZlU1UUN3ME2xO{43QCEEsTC0MlUzKM7:TR?= NYr6[4xGOjZzMkWyN|A>
A549-NTC NXHVV41RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGL0dZczPCCq NGPvR2ZKSzVyPUG5MlQzKMLzIEGuPVYh|ryP MmfXNlYyOjV{M{C=
A549-920 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknGNlQhcA>? M4fjR2lEPTB;M{OuPFUhyrFiND64OEDPxE1? NELJNlkzPjF{NUKzNC=>
CRL-5908 MlH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqyOEBp MXzJR|UxRTN6LkexJOKyKDJwNEOg{txO NYi4WHZ{OjZzMkWyN|A>
L6 MmjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHneXhvOTEEoN88UeKh M3TIWFI1NzR6L{eyJIg> NFnOV2hFVVOR NIXXN|dqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? MljGNlU5PzF5OUS=
C2C12 NXf4eoV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2mzXlExyqEQvF5CpC=> MkD1NlQwPDhxN{KgbC=> M4rVXmROW09? M4HZRolvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? NWTWSHI6OjV6N{G3PVQ>
MCF-7  NEfK[IZHfW6ldHnvckBCe3OjeR?= NHHKO20yOMLizszN MnXySG1UVw>? MUjpcohq[mm2czDjfYNtcW5iREGgZY5lKESrY3XyxsA> Mk\FNlU4ODJ5MEO=
DU4475  NHiwNWtHfW6ldHnvckBCe3OjeR?= M1\2RlUwOTBxMkCg{txO MoHuNlTDqGh? NW\LWo5C\G:5boLl[5Vt[XSnczDUc4NiNTFiZH;z[UBl\XCnbnTlcpRtgQ>? M2nGe|I2PTR5MUe0
SMMC-7721 NXrpblI6TnWwY4Tpc44hSXO|YYm= MoXnNVAh|ryP MoLLOFghcA>? NXzMR4lSTE2VTx?= M2D6NYNifXOnczDEUmEhTFOEIHThcYFo\Q>? MYOyOVU1PDN4MR?=
SMMC-7721 Mn3GSpVv[3Srb36gRZN{[Xl? M2DDVVExKM7:TR?= M4XoeFQ5KGh? MYnEUXNQ NEDKdldqdmS3Y3XzJJRp\SClaILvcYF1cW5vYn;1coQheHKxdHXpckBKTklzNjD0c{Bx[XK2aXHscJkhdG:lYXzpfoUhcW5idHjlJIN6fG:ybHHzceKh M2rSSFI2PTR2M{[x
SMMC-7721 NEP2SJZHfW6ldHnvckBCe3OjeR?= NXXlNG1VOTBizszN NXHp[2xxPDhiaB?= NWjSZnlSTE2VTx?= MWDpcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2cEoFnGUmIyyqCvUl7B MXmyOVU1PDN4MR?=
SMMC-7721 MlLwSpVv[3Srb36gRZN{[Xl? M1i1cFExKM7:TR?= Mme2N|YhcA>? MofISG1UVw>? MnrLZ4F2e2W|IITo[UBm[3SxcHnjJIV5eHKnc4Ppc44hd2ZiSV\JNVY> M3\mU|I2PTR2M{[x
MCF-7 MUHGeY5kfGmxbjDBd5NigQ>? M{LKb|ExyqEQvF2= MmTKNE0zPCCq MUPpcoR2[2W|IIC1N{BidmRicEKxM2NqeDF? NGDt[nczPTR6MkO3Ny=>
OVCAR10 M4TjVGZ2dmO2aX;uJGF{e2G7 NUnaWI8zOTEEoN88US=> NW\0Xm9xOjGqwrC= MYLEUXNQ NInaVW9qdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ MYOyOVQzPjV2OB?=
NCI-H23 NYj3W4dwTnWwY4Tpc44hSXO|YYm= M{LHcFExyqEQvF2= MWWyNYjDqA>? NFPWe5JFVVOR M3jhRYlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> MmfpNlU1OjZ3NEi=
A2780 MoS4SpVv[3Srb36gRZN{[Xl? NVrT[3JVOTEEoN88US=> NG\yZpIzOWkEoB?= MnTuSG1UVw>? MlfPbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> MkSwNlU1OjZ3NEi=
NCI-H23 NGDCVVBHfW6ldHnvckBCe3OjeR?= MoTaNVDDqM7:TR?= M1LCSFIycMLi M1Oxb2ROW09? NHjsSWpl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> MXuyOVQzPjV2OB?=
A2780 MUjGeY5kfGmxbjDBd5NigQ>? MUCxNOKh|ryP M1nK[|IycMLi NVr2S3E6TE2VTx?= NUX4TI9k\GWlcnXhd4V{KHSqZTDGc5hOOSCuZY\lcJM> MV:yOVQzPjV2OB?=
HCT116  MX;GeY5kfGmxbjDBd5NigQ>? NHThT4wyOCEEtV2= M4HQ[VI1KGh? M{\CcoNifXOnczDhJJA2Oy2mZYDlcoRmdnRidHX0doFxdG:rZDDHNU1ienKnc4SgbY4h\GmybH;p[EBJS1RzMU[gZ4xwdmW|IFSzJIFv\CCGOB?= M1vaRVI2OzhyMEW1
MCF-10CA1a NFfSSnpHfW6ldHnvckBCe3OjeR?= NW\Sd4dTOTEEoN88US=> M3fLfFQ5KGh? Mmr4SG1UVw>? MVPpcohq[mm2czDiZZNidCCrbo\hd4lwdiCjbnSgdoVlfWOnZDDUS2Yu|rJ|LXnu[JVk\WRiaX72ZZNqd25idH:gZoF{[WxibHX2[Yx{ NW\kS4c3OjV{NUe3Nlk>
MCF-10A1  M1mxWGZ2dmO2aX;uJGF{e2G7 M4nwUVExyqEQvF2= M{KzSFI1NzR6IHi= NIK3foFFVVOR NFj0[HRqdmirYnn0d{BucWe{YYTpc44hd2Zibn;ycYFtKGK{ZXHzeEBmeGm2aHXsbYFtyqB? NXvSVphCOjV{NUe3Nlk>
MCF-10CA1a MkTvSpVv[3Srb36gRZN{[Xl? Mkn0NVDDqM7:TR?= MmTVNlQhcA>? NUT0WFhNTE2VTx?= NHLWdItl\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= M4S5c|I2OjV5N{K5
MCF-10CA1a NFfwS3dHfW6ldHnvckBCe3OjeR?= MYSxNOKh|ryP Mn:1NlQhcA>? NGjFdm9FVVOR NYfqbY13cW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u NEnkOXAzPTJ3N{eyPS=>
SK-BR-7 M2K3VGZ2dmO2aX;uJGF{e2G7 Mo\RNVDDqM7:TR?= MmDKNlQhcA>? NV7qU|ZSTE2VTx?= M33KZ4lvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= M33ucFI2OjV5N{K5
SUM102PT NGe3bHZHfW6ldHnvckBCe3OjeR?= NEDnZWgyOMLizszN Mmn2NlQhcA>? M4XWPGROW09? NVuwUlFjcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u NUKwXlc2OjV{NUe3Nlk>
RAW 264.7 NHnjfFlHfW6ldHnvckBCe3OjeR?= M4XJNVExyqEQvF2= M1i0dlMxKG2rbh?= NH;tOJRxemW4ZX70d{B1cGVicEWzJJJm\HWldHnvckBqdiC{ZYPwc45{\SC2bzDMVHM> NIe5Z|QzPTF5MkW0Oy=>
RAW 264.7 NXXnZlh5TnWwY4Tpc44hSXO|YYm= NILxNYcyOMLizszN NXLOXVlsOzBibXnu MoT0doVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= M2nu[FI2OTd{NUS3
RAW 264.7 M4DhT2Z2dmO2aX;uJGF{e2G7 Mn7DNVDDqM7:TR?= M2HTTFMxKG2rbh?= MVrpcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= MonpNlUyPzJ3NEe=
MCF7  NHXheI5E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3q5[VIvPSEEtV2= MX:1JIQ> M{npTWROW09? NWPDS3Bwe2Wwc3n0bZpmeyCPQ1[3JJRwKFCDUmCgbY5pcWKrdHnvci=> MnrNNlUxQDV7MEK=
MCF7  MWHGeY5kfGmxbjDBd5NigQ>? NH;ZN3EzNjViwsXN MXW0PEBp MVTEUXNQ MULk[YNz\WG|ZYOgeIhmKGixbX;sc4dwfXNiRGPCJJJmeGGrcjDmdoVyfWWwY3nldy=> M4GxUVI2ODh3OUCy
ACHN NXHwXHprS2WubDDWbYFjcWyrdImgRZN{[Xl? NX32emtyOC53LUGwJO69VQ>? M4\nVVAuPiCm M{XCRWROW09? MXPpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmiyNlUxPjd5OEe=
Caki-2 NXjMVII2S2WubDDWbYFjcWyrdImgRZN{[Xl? NGWxWHYxNjVvMUCg{txO MkTENE03KGR? NILCNmVFVVOR NYG1ZYJScW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NGXoXoIzPTB4N{e4Oy=>
A498 NIT4TmtE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHT0S4YxNjVvMUCg{txO MmLtNE03KGR? MkHWSG1UVw>? MXnpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnG3NlUxPjd5OEe=
115 MmTWR4VtdCCYaXHibYxqfHliQYPzZZk> NVXlemF5OC53LUGwJO69VQ>? M1LYNVAuPiCm MnTtSG1UVw>? NHrIb5VqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M4myXlI2ODZ5N{i3
117 M3;ONGNmdGxiVnnhZoltcXS7IFHzd4F6 NH25Z2UxNjVvMUCg{txO M1XI[|AuPiCm M4fhRWROW09? MmT4bY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4HrZlI2ODZ5N{i3
ACHN NGfXVHVHfW6ldHnvckBCe3OjeR?= NVv0cVNPOC53L{GvOUDPxE1? NWD4Xo9VPDhiaB?= NF7ZRWhFVVOR M{K5NIxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz NWTucHlsOjVyNke3PFc>
Caki-2 NUjLT3hkTnWwY4Tpc44hSXO|YYm= MVewMlUwOS93IN88US=> NHrL[nA1QCCq Mn;kSG1UVw>? MYPs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NWG1SJFwOjVyNke3PFc>
A498 NGH0[nVHfW6ldHnvckBCe3OjeR?= MV:wMlUwOS93IN88US=> M4nEUVQ5KGh? M3TMbmROW09? MkTZcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? MX:yOVA3Pzd6Nx?=
115 M{LJRWZ2dmO2aX;uJGF{e2G7 MWSwMlUwOS93IN88US=> M3zaTlQ5KGh? MXPEUXNQ MYfs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? M{fRd|I2ODZ5N{i3
ACHN M{TzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjVV3NLPSEQvF2= NGj1TIk1QCCq M3rCbGROW09? M3PYW4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NF3aPVkzPTB4N{e4Oy=>
Caki-2 M4W3Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXi1JO69VQ>? NHSxOYE1QCCq MV;EUXNQ M3HjbIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NFfFXFEzPTB4N{e4Oy=>
A498 NEPDd2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzmVmo2KM7:TR?= MUS0PEBp NUfxbGVZTE2VTx?= MoHGbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg NELIVIwzPTB4N{e4Oy=>
115 MlK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnKWpUxPSEQvF2= MnrvOFghcA>? NIrzO2xFVVOR M{G0dolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MlX2NlUxPjd5OEe=
ACHN NFvKeWdHfW6ldHnvckBCe3OjeR?= MVi1JO69VQ>? NVTBZW1UPDhiaB?= MW\EUXNQ M2PmTIlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= MWKyOVA3Pzd6Nx?=
Caki-2 MlfvSpVv[3Srb36gRZN{[Xl? MVO1JO69VQ>? MnnFOFghcA>? MYXEUXNQ M3T3UIlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= MXuyOVA3Pzd6Nx?=
A498 Ml73SpVv[3Srb36gRZN{[Xl? MXi1JO69VQ>? NYXHOIFMPDhiaB?= M4HobmROW09? MUDpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NGC1fGczPTB4N{e4Oy=>
115 MkHtSpVv[3Srb36gRZN{[Xl? NFq3OYQ2KM7:TR?= MWq0PEBp M334eGROW09? M4fD[4lv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= NH3jXnkzPTB4N{e4Oy=>
MOLM-13 MVXGeY5kfGmxbjDBd5NigQ>? NHLTbFk3yqEQvF2= Ml2yNE05KGh? MmLySG1UVw>? M17TdIlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIIC1N{whVUSPMjygdFIyKGGwZDDhZ4V1gWyjdHXkJJA2Ow>? NYj4V5dvOjR6OEWwPFI>
MOLM-13 MWLGeY5kfGmxbjDBd5NigQ>? M{C2fVbDqM7:TR?= M3fkelYhcA>? MV;EUXNQ MWflcohidmOnczD0bIUh[WOndInsZZRqd25ib3[gbIl{fG:wZTDINmIh[W6mIHjlZZQhe2ixY3ugdJJwfGWrboOgTJNxOjdiYX7kJGh{eDly MViyOFg5PTB6Mh?=
HepG2 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUG3NkBp M1\kNmROW09? Mm\ITWM2OD1|NT64OkDDuSB{Lkmg{txO NWT5dFVwOjR6OES4NFk>
HepG2/As NVnPT|JwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi3NkBp MoDLSG1UVw>? MX3JR|UxRTZ6LkGzJOKyKDlwNjFOwG0> NXjaeopqOjR6OES4NFk>
SMMC7721 M33FUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\VO|IhcA>? MoLhSG1UVw>? NFXKdnpKSzVyPUOxMlI5KMLzIESuNkDPxE1? NYjOenc5OjR6OES4NFk>
SMMC7721/Ac NVvsS5d1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPuZ5N3PzJiaB?= NFnNfHZFVVOR MlPHTWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? MYOyOFg5PDhyOR?=
Huh-7 NHTFPGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rHTlczKGh? NVfmeZo5TE2VTx?= MkfMTWM2OD1|Mz65OkDDuSB|Lkmg{txO M3PGZVI1QDh2OEC5
Hep3B MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XocFczKGh? NYLQXlV1TE2VTx?= NIL1[HpKSzVyPUKwMlE5KMLzIEGuPFQh|ryP NGLmem0zPDh6NEiwPS=>
HepG2 NUHMR2tpSXCxcITvd4l{KEG|c3H5 NXHzTIpbcW6mdXPld{BieG:ydH;zbZM> MYmyOFg5PDhyOR?=
SMMC7721 NWjMNpNrSXCxcITvd4l{KEG|c3H5 M3PnTIlv\HWlZYOgZZBweHSxc3nz NXH4[4Q6OjR6OES4NFk>
Huh-7 NYHqXINuSXCxcITvd4l{KEG|c3H5 MWHpcoR2[2W|IHHwc5B1d3Orcx?= NInteWEzPDh6NEiwPS=>
Hep3B NH60[|RCeG:ydH;zbZMhSXO|YYm= MWPpcoR2[2W|IHHwc5B1d3Orcx?= NVPH[mY4OjR6OES4NFk>
U2OS  NWrZZo85TnWwY4Tpc44hSXO|YYm= NELkc5MzOCEQvF2= MXGyOEBp M2XUSIlv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= NHPQb5EzPDh4N{K1PS=>
AML2 MnXxRZBweHSxc3nzJGF{e2G7 NGrv[GgzNzFyIN88US=> NFf4SJIzPC92ODDo NHnBdpdqdmS3Y3XzJIFxd3C2b4Ppdy=> Ml:xNlQ3PTl5NEm=
MOML13 NFjrc2lCeG:ydH;zbZMhSXO|YYm= MonaNk8yOCEQvF2= MWOyOE81QCCq MWHpcoR2[2W|IHHwc5B1d3Orcx?= M3nadVI1PjV7N{S5
AML2 NUnH[W9yTnWwY4Tpc44hSXO|YYm= MknSNVDPxE1? NV;zXnMzOi92IHi= NXrYUXFScW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NIjWOW8zPDZ3OUe0PS=>
AML3 NGjQfIZHfW6ldHnvckBCe3OjeR?= NX3LRWdiOTEQvF2= M4LZ[FIwPCCq MmPxbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= MlHoNlQ3PTl5NEm=
MOML13 MW\GeY5kfGmxbjDBd5NigQ>? NWrCPGtlOTEQvF2= NH;Je5QzNzRiaB?= NVLxeWIxcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MmnWNlQ3PTl5NEm=
BeWo MkHLSpVv[3Srb36gRZN{[Xl? NGfGeoo{OCEEtV2= M1XzdFI1KGh? NEHzRZhqdmO{ZXHz[ZMheDV|LDDN[I0zNCCyMkGgZY5lKFC3bXGgZZQhfGinIIDyc5RmcW5ibHX2[Yw> NHzjUJYzPDR7OEG1OC=>
BeWo NY[1PXpNSXCxcITvd4l{KEG|c3H5 NE\RXWQ{OCEEtV2= NHjlVWkzPCCq NXHOOoxIcW6lcnXhd4V{KGGyb4D0c5Nqew>? M2\Ub|I1PDl6MUW0
OCI NVXERmV6TnWwY4Tpc44hSXO|YYm= NEXq[3QyOCEQvF2= NWPBVXV3OjRiaB?= MW\1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? M2XOc|I1PDd|NU[y
MOLM NFPKWWdHfW6ldHnvckBCe3OjeR?= NXz6S3F[OTBizszN NF;4WWEzPCCq M3XKPZVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= Mn7TNlQ1PzN3NkK=
U2OS  NF7OTGNHfW6ldHnvckBCe3OjeR?= NWK3dFZ1OjBizszN MYmyOEBp MlPBbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? NIP1N4czPDN4NkCwOy=>
RKO NYW2WWdJTnWwY4Tpc44hSXO|YYm= NG\JOWMzOCEQvF2= NUXnN2o1OjRiaB?= M3fBTYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? MXKyOFM3PjByNx?=
U2OS  NUDoelk3TnWwY4Tpc44hSXO|YYm= M1jFclIxKM7:TR?= MWGyOEBp NGLiVGNqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> NVm4[lhrOjR|Nk[wNFc>
RKO MWDGeY5kfGmxbjDBd5NigQ>? M4PGflIxKM7:TR?= NGHvR5czPCCq NGj0WY9qdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> MYqyOFM3PjByNx?=
SMMC-7721  MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NX35Z2J3OS5{NT2yNEDPxE1? MofFNlQwPDhxN{KgbC=> NIPEPWVFVVOR NXTocIR5cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MYeyOFI5PjNzMh?=
HuH-7 M1HPRmNmdGxiVnnhZoltcXS7IFHzd4F6 NXjWd45POS5{NT2yNEDPxE1? MkW5NlQwPDhxN{KgbC=> M3y4SGROW09? NG\6ZVNqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MWSyOFI5PjNzMh?=
SMMC-7721  NHPUVVlCeG:ydH;zbZMhSXO|YYm= NGKwWlczOCEQvF2= M3rCelQ5KGh? M{fUeWROW09? NVXrVZlxcW6mdXPld{BieG:ydH;zbZM> NHnZWY4zPDJ6NkOxNi=>
HuH-7 NGTzfJBCeG:ydH;zbZMhSXO|YYm= NVvzPYNCOjBizszN Mn3TOFghcA>? NWHUbVdITE2VTx?= NXS0WZcxcW6mdXPld{BieG:ydH;zbZM> M4\3NVI1Ojh4M{Gy
SMMC-7721  NGLsc4RHfW6ldHnvckBCe3OjeR?= MoflNVAh|ryP MYKzOkBp NF7JWW5FVVOR MUHkc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> NYjtVGRsOjR{OE[zNVI>
HuH-7 M{mzb2Z2dmO2aX;uJGF{e2G7 M135N|ExKM7:TR?= M2H1UlM3KGh? MmfHSG1UVw>? M2DYeYRwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ NYSzOXJlOjR{OE[zNVI>
AT2 MVfGeY5kfGmxbjDBd5NigQ>? MYC1M|ExKM7:TR?= NHzxSFRt\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= M2rnN|I1OjRyMkCz
REH M2jUe2Z2dmO2aX;uJGF{e2G7 M4TFXFUwOTBizszN M3rXWIxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li Mn3vNlQzPDB{MEO=
UoCB6 NEO1N|JHfW6ldHnvckBCe3OjeR?= NE[zU202NzFyIN88US=> NGjwTVBt\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= NYD1UYhxOjR{NECyNFM>
AT2 NIDqdpRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn;6NE0zPSEQvF2= MVrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NHnDWYgzPDJ2MEKwNy=>
REH MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2fyTFAuOjVizszN MUfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MYeyOFI1ODJyMx?=
UoCB6 MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkPUNE0zPSEQvF2= MUPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MYmyOFI1ODJyMx?=
A2780 MW\GeY5kfGmxbjDBd5NigQ>? NWS4VYp5PS9zMD:yNEDPxE1? MmDRNlQhcA>? NUPwOG9mfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= NUjyRVR6OjRzM{[xOFc>
H460 M{jnUmZ2dmO2aX;uJGF{e2G7 M1Hyd|UwOTBxMkCg{txO NFqwdXMzPCCq MojjeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? MYeyOFE{PjF2Nx?=
Lovo  NE\ye5NHfW6ldHnvckBCe3OjeR?= Mn[0OU8yOC9{MDFOwG0> NUe2[5VZOjRiaB?= NWmyUG81fXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= MWqyOFE{PjF2Nx?=
A2780 NWnEb5lzSXCxcITvd4l{KEG|c3H5 M{S1fVUwOTBxMkCg{txO NU[4fpY6OjRiaB?= M{TmfoVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN MV6yOFE{PjF2Nx?=
H460 MoK0RZBweHSxc3nzJGF{e2G7 M37qN|UwOTBxMkCg{txO NIfw[2ozPCCq NFXsSpNmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? NFPRSGszPDF|NkG0Oy=>
Lovo  NH;QXoVCeG:ydH;zbZMhSXO|YYm= MoPUOU8yOC9{MDFOwG0> NEHKOJgzPCCq M2i3TYVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN NH7NbHgzPDF|NkG0Oy=>

... 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

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  • Nutlin-3b

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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