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 NF;jXnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoG0OeKh|ryP NX[3ZYhrPDkEoHi= MUTicI9kc3NiMketU2hENWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKGOxbYDhdoFjdGVidH:geIhifCCxZjDiZZNidCCuZY\lcJM> NGPDZowzPjN3MEW2OS=>
NP69 NUjZVWpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnSzTWM2OD1|MT62PeKyOi53NDFOwG0> NHzlO3gzPjJ3MkW3OS=>
NP460 MlW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DEPWlEPTB;MkKuPFXDuTFwMUig{txO M1HXTFI3OjV{NUe1
C666-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEThVGZKSzVyPUG5Mlk2yrF6LkmzJO69VQ>? NVTRdnU4OjZ{NUK1O|U>
C666-1 MXjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkPUNVAhyrWP NXvNXWNZPDhiaB?= MWrEUXNQ Ml7Xd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:geIhmKGO7dH;0c5hq[yCnZn\lZ5Qhd2ZiY3nzdIxifGmw MmLHNlYzPTJ3N{W=
C666-1  NFrP[YhHfW6ldHnvckBCe3OjeR?= NH:2OocyOCEEtV2= M2G5R|I1KGh? M{XQV2ROW09? M{\mOIFkfGm4YYTld{B1cGVicEWzJJBifGi5YYmsJJVxemWpdXzheIlv\yCyNUOsJJAzOSCjbnSgUYRuOg>? M{jmVlI3OjV{NUe1
C666-1 NGPOTVJCeG:ydH;zbZMhSXO|YYm= Mn7JNVAhyrWP NYP3[I9PPDhxN{KgbC=> NEHOWnhFVVOR MUHz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzDjbZNxdGG2aX6tbY5lfWOnZDDhdI9xfG:|aYO= MojINlYzPTJ3N{W=
A549 MoLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHxNlQhcA>? MVPJR|UxRTF5Lk[4JOKyKDRwNUKg{txO M4jTOVI3OTJ3MkOw
A549-NTC NV3Ie|A1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYryToFWOjRiaB?= MlO1TWM2OD1zOT60NkDDuSBzLkm2JO69VQ>? Ml3INlYyOjV{M{C=
A549-920 NFHET3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrycoxDOjRiaB?= MYrJR|UxRTN|Lki1JOKyKDRwOESg{txO MlmyNlYyOjV{M{C=
CRL-5908 Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HwV|I1KGh? M3;TS2lEPTB;M{iuO|EhyrFiMj60N{DPxE1? NFvIbnIzPjF{NUKzNC=>
L6 MlfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUX4TmhyOTEEoN88UeKh NVXVOWd3OjRxNEivO|IhcA>? M{P3emROW09? Mnv0bY5pcWKrdIOgZ4VtdHNicILvcIln\XKjdHnvckBidmRiZHnm[oVz\W62aXH0bY9v NG\ONHMzPTh5MUe5OC=>
C2C12 M{jyfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\nNVDDqM7:TdMg NFS5VGszPC92OD:3NkBp NGW4UJdFVVOR NYmydnNRcW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w M1vWNFI2QDdzN{m0
MCF-7  M2rER2Z2dmO2aX;uJGF{e2G7 MX:xNOKh|ryP NWm4eHVpTE2VTx?= NIDISVBqdmirYnn0d{BkgWOuaX6gSFEh[W6mIFTpZ4VzyqB? MUmyOVcxOjdyMx?=
DU4475  MmqwSpVv[3Srb36gRZN{[Xl? NED6Nlk2NzFyL{KwJO69VQ>? MYiyOOKhcA>? M{S0UIRwf26{ZXf1cIF1\XNiVH;jZU0yKGSxc3Wg[IVx\W6mZX70cJk> NX7Ib4RUOjV3NEexO|Q>
SMMC-7721 MWXGeY5kfGmxbjDBd5NigQ>? NFzUdokyOCEQvF2= M1Pnc|Q5KGh? MnHRSG1UVw>? MkP2Z4F2e2W|IFTORUBFW0JiZHHtZYdm M1HBTVI2PTR2M{[x
SMMC-7721 Mk\1SpVv[3Srb36gRZN{[Xl? MofINVAh|ryP MVG0PEBp NIjvT5RFVVOR Mln5bY5lfWOnczD0bIUh[2i{b33heIlvNWKxdX7kJJBzd3SnaX6gTWZKOTZidH:gdIFzfGmjbHz5JIxw[2GuaYrlJIlvKHSqZTDjfZRweGyjc35CpC=> NYr0c5VYOjV3NESzOlE>
SMMC-7721 NIXPS2RHfW6ldHnvckBCe3OjeR?= MkPXNVAh|ryP NEDWXok1QCCq MYfEUXNQ NHfXVWFqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3dCpGlHVkJzwrDtVm5C M3PvSVI2PTR2M{[x
SMMC-7721 M{jNc2Z2dmO2aX;uJGF{e2G7 M{TqfVExKM7:TR?= NXq0XFJ6OzZiaB?= NHn1ZphFVVOR NGfJOWdk[XW|ZYOgeIhmKGWldH;wbYMh\XiycnXzd4lwdiCxZjDJSmkyPg>? NHvEVIYzPTV2NEO2NS=>
MCF-7 MVzGeY5kfGmxbjDBd5NigQ>? MknKNVDDqM7:TR?= M1nSPFAuOjRiaB?= NHW5S2VqdmS3Y3XzJJA2OyCjbnSgdFIyN0OrcEG= M2j5V|I2PDh{M{ez
OVCAR10 NUPZ[284TnWwY4Tpc44hSXO|YYm= NELlTYsyOMLizszN NUK5cG5XOjGqwrC= MlnPSG1UVw>? MlzqbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NWnHTlFUOjV2Mk[1OFg>
NCI-H23 MV3GeY5kfGmxbjDBd5NigQ>? NVGxXoZtOTEEoN88US=> NYi4UJBJOjGqwrC= MnHzSG1UVw>? Mn\qbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> MnzCNlU1OjZ3NEi=
A2780 NIDxe3NHfW6ldHnvckBCe3OjeR?= NEmwT4YyOMLizszN NELlO|gzOWkEoB?= NYTMXIxbTE2VTx?= Ml\IbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NYPY[npiOjV2Mk[1OFg>
NCI-H23 MkfnSpVv[3Srb36gRZN{[Xl? NIDUTZQyOMLizszN NVP0U4pqOjGqwrC= MoK2SG1UVw>? MYnk[YNz\WG|ZYOgeIhmKE[xeF2xJIxmfmWucx?= NYL6dIdDOjV2Mk[1OFg>
A2780 MmjmSpVv[3Srb36gRZN{[Xl? NYnxPGJtOTEEoN88US=> MVmyNYjDqA>? NE\XO|FFVVOR M1K2TIRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz NV7Vem5qOjV2Mk[1OFg>
HCT116  MVjGeY5kfGmxbjDBd5NigQ>? MXGxNEDDvU1? NEDqZWEzPCCq MVzjZZV{\XNiYTDwOVMu\GWyZX7k[Y51KHSndILhdIxwcWRiR{GtZZJz\XO2IHnuJIRqeGyxaXSgTGNVOTF4IHPsc45meyCGMzDhcoQhTDh? NX3tcIxNOjV|OECwOVU>
MCF-10CA1a MUfGeY5kfGmxbjDBd5NigQ>? MXyxNOKh|ryP Ml\1OFghcA>? MUfEUXNQ MUHpcohq[mm2czDiZZNidCCrbo\hd4lwdiCjbnSgdoVlfWOnZDDUS2Yu|rJ|LXnu[JVk\WRiaX72ZZNqd25idH:gZoF{[WxibHX2[Yx{ NW\qe4N[OjV{NUe3Nlk>
MCF-10A1  NYTPWFd1TnWwY4Tpc44hSXO|YYm= NYflZo9yOTEEoN88US=> M4HPbFI1NzR6IHi= NYLpTm9kTE2VTx?= NIPMSVRqdmirYnn0d{BucWe{YYTpc44hd2Zibn;ycYFtKGK{ZXHzeEBmeGm2aHXsbYFtyqB? M1TTNFI2OjV5N{K5
MCF-10CA1a MmP3SpVv[3Srb36gRZN{[Xl? MlW1NVDDqM7:TR?= M3zOdFI1KGh? MnTZSG1UVw>? NXnqOWlG\GWlcnXhd4V{KHSqZTDUS2Yu|rJ|LXnu[JVk\WRibWLORUBt\X[nbIOgc4ZOVVB{LNMgUW1RQSxiYX7kxsBqdnSnZ4LpcuKh|rMEoEO= NGTCWGczPTJ3N{eyPS=>
MCF-10CA1a MkXVSpVv[3Srb36gRZN{[Xl? MVWxNOKh|ryP Ml;SNlQhcA>? Mn24SG1UVw>? M37XXIlvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= NFXKTngzPTJ3N{eyPS=>
SK-BR-7 NYOyWGNtTnWwY4Tpc44hSXO|YYm= NGrkW5MyOMLizszN NVHRNXk5OjRiaB?= NETuOXhFVVOR M{npUYlvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= MlLXNlUzPTd5Mkm=
SUM102PT M2e1OWZ2dmO2aX;uJGF{e2G7 NH;lSJkyOMLizszN M13hVlI1KGh? NXXLOnJsTE2VTx?= NFK4R2FqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= M3TkblI2OjV5N{K5
RAW 264.7 MYrGeY5kfGmxbjDBd5NigQ>? M13pN|ExyqEQvF2= MYezNEBucW5? MoDKdJJmfmWwdIOgeIhmKHB3MzDy[YR2[3Srb36gbY4hemW|cH;ud4UhfG9iTGDT NYC5[pFlOjVzN{K1OFc>
RAW 264.7 M3zSTmZ2dmO2aX;uJGF{e2G7 MWCxNOKh|ryP MmTEN|AhdWmw MlzEdoVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= NFLDTpozPTF5MkW0Oy=>
RAW 264.7 M3PpNGZ2dmO2aX;uJGF{e2G7 NGLlXlUyOMLizszN NETtSoY{OCCvaX6= MWjpcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= NXjIRVdtOjVzN{K1OFc>
MCF7  NEH1cZBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFXvN|AzNjViwsXN NEi3fVE2KGR? NHqze2JFVVOR M3T0NJNmdnOrdHn6[ZMhVUOINzD0c{BRSVKSIHnubIljcXSrb36= M1u0VlI2ODh3OUCy
MCF7  M4niOGZ2dmO2aX;uJGF{e2G7 NHnvOZEzNjViwsXN MYe0PEBp MXPEUXNQ NEPxXWRl\WO{ZXHz[ZMhfGinIHjvcY9td2exdYOgSHNDKHKncHHpdkBnemWzdXXuZ4lmew>? NV6zb4N4OjVyOEW5NFI>
ACHN M4jiOmNmdGxiVnnhZoltcXS7IFHzd4F6 NGHtSVExNjVvMUCg{txO MoLCNE03KGR? NH7teHVFVVOR NHW0WnFqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NUjWdHhVOjVyNke3PFc>
Caki-2 NITBZ5VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWKwMlUuOTBizszN NUHxSop2OC14IHS= M{jxXWROW09? NU\PfIRlcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= Mn7ENlUxPjd5OEe=
A498 NY\CWXNRS2WubDDWbYFjcWyrdImgRZN{[Xl? NFHmVGgxNjVvMUCg{txO M4TNV|AuPiCm NXvIUW9ITE2VTx?= MV\pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NH;BNJIzPTB4N{e4Oy=>
115 NXfHeY1oS2WubDDWbYFjcWyrdImgRZN{[Xl? NFnkT4cxNjVvMUCg{txO MYCwMVYh\A>? NGTjXplFVVOR NV7RPFdUcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M2nPPFI2ODZ5N{i3
117 NUDFUZZlS2WubDDWbYFjcWyrdImgRZN{[Xl? NEPxcVIxNjVvMUCg{txO MXewMVYh\A>? MVLEUXNQ MULpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX7U[5l4OjVyNke3PFc>
ACHN MkTESpVv[3Srb36gRZN{[Xl? MU[wMlUwOS93IN88US=> NVXCZWV[PDhiaB?= NFHWdW5FVVOR MWLs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MmrPNlUxPjd5OEe=
Caki-2 Mke5SpVv[3Srb36gRZN{[Xl? NGHyVHcxNjVxMT:1JO69VQ>? NWrsXJpTPDhiaB?= NWTXeJBFTE2VTx?= MX7s[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MV2yOVA3Pzd6Nx?=
A498 NELNTpVHfW6ldHnvckBCe3OjeR?= MV6wMlUwOS93IN88US=> NXrMcGZbPDhiaB?= MljySG1UVw>? MljicIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? M{XjOFI2ODZ5N{i3
115 MmHJSpVv[3Srb36gRZN{[Xl? M3vGTlAvPS9zL{Wg{txO MofmOFghcA>? M{TKe2ROW09? MmPZcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? M2DOfFI2ODZ5N{i3
ACHN NGjETW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[1JO69VQ>? NGGyZog1QCCq MVjEUXNQ M4X2TIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NXPpbnllOjVyNke3PFc>
Caki-2 NHr1ZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7wT402KM7:TR?= MWO0PEBp M2CwfWROW09? NV[2TFIxcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NFTwXmgzPTB4N{e4Oy=>
A498 M2O4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[1JO69VQ>? NX3TRYxkPDhiaB?= NX;2SZpDTE2VTx?= NVfBfnRVcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NHjtNGQzPTB4N{e4Oy=>
115 NUTNb5kzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjEUJJqPSEQvF2= Ml\0OFghcA>? MnjpSG1UVw>? NX7HVZBtcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NUfncIRmOjVyNke3PFc>
ACHN MmLGSpVv[3Srb36gRZN{[Xl? Ml\zOUDPxE1? NGTUS4c1QCCq M1rKWmROW09? NX\TNXpTcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> MWmyOVA3Pzd6Nx?=
Caki-2 M{LtZ2Z2dmO2aX;uJGF{e2G7 M3LvOVUh|ryP NEfa[oc1QCCq MkGxSG1UVw>? M3fVfolv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= MnjjNlUxPjd5OEe=
A498 NVvlfZdXTnWwY4Tpc44hSXO|YYm= MXW1JO69VQ>? MkXOOFghcA>? MnTFSG1UVw>? NUnsXYlOcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> MX6yOVA3Pzd6Nx?=
115 M3LWUGZ2dmO2aX;uJGF{e2G7 NGHPOJU2KM7:TR?= MWm0PEBp NVzKSXJRTE2VTx?= MnLJbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NUm2[ndCOjVyNke3PFc>
MOLM-13 Mmq1SpVv[3Srb36gRZN{[Xl? NEDhUGY3yqEQvF2= MoCxNE05KGh? Mn;CSG1UVw>? MmO3bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZicEWzMEBOTE1{LDDwNlEh[W6mIHHj[ZR6dGG2ZXSgdFU{ MnL6NlQ5QDVyOEK=
MOLM-13 MnH4SpVv[3Srb36gRZN{[Xl? M3v0T|bDqM7:TR?= M3vmcFYhcA>? MlT4SG1UVw>? Mk\5[Y5p[W6lZYOgeIhmKGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFJDKGGwZDDo[YF1KHOqb3PrJJBzd3SnaX7zJGh{eDJ5IHHu[EBJe3B7MB?= MV2yOFg5PTB6Mh?=
HepG2 MoO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvhO|IhcA>? NEHlPIVFVVOR NUPqW4hsUUN3ME2zOU45PiEEsTCyMlkh|ryP NFfvU4EzPDh6NEiwPS=>
HepG2/As M4fIXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rLTFczKGh? MYDEUXNQ M1\ye2lEPTB;NkiuNVMhyrFiOT62JO69VQ>? NEDXT3QzPDh6NEiwPS=>
SMMC7721 NIH3UoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXrO|IhcA>? NV\SZmJyTE2VTx?= MnPZTWM2OD1|MT6yPEDDuSB2LkKg{txO NVHjcGlGOjR6OES4NFk>
SMMC7721/Ac M4j3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HRelczKGh? NVrtc3M3TE2VTx?= NHPlTJBKSzVyPUW1MlIyKMLzIEWuNFMh|ryP MnLlNlQ5QDR6MEm=
Huh-7 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Dmd|czKGh? NUH0W3p5TE2VTx?= M1vvN2lEPTB;M{OuPVYhyrFiMz65JO69VQ>? M3L3R|I1QDh2OEC5
Hep3B MmH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;PbVVpPzJiaB?= NYXsc4g2TE2VTx?= NULBZoZHUUN3ME2yNE4yQCEEsTCxMlg1KM7:TR?= NWqyWoxFOjR6OES4NFk>
HepG2 MV7BdI9xfG:|aYOgRZN{[Xl? MmPabY5lfWOnczDhdI9xfG:|aYO= NVftZpp{OjR6OES4NFk>
SMMC7721 Mm\IRZBweHSxc3nzJGF{e2G7 NGTZNXZqdmS3Y3XzJIFxd3C2b4Ppdy=> MkDsNlQ5QDR6MEm=
Huh-7 MoDaRZBweHSxc3nzJGF{e2G7 NWHnTmdPcW6mdXPld{BieG:ydH;zbZM> MUOyOFg5PDhyOR?=
Hep3B MXXBdI9xfG:|aYOgRZN{[Xl? MoTObY5lfWOnczDhdI9xfG:|aYO= MmX5NlQ5QDR6MEm=
U2OS  MYLGeY5kfGmxbjDBd5NigQ>? MnXpNlAh|ryP MViyOEBp M{S1R4lv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= M17nTVI1QDZ5MkW5
AML2 NVLWRWhrSXCxcITvd4l{KEG|c3H5 MoLwNk8yOCEQvF2= M{fuVlI1NzR6IHi= MV;pcoR2[2W|IHHwc5B1d3Orcx?= NVnsSY1POjR4NUm3OFk>
MOML13 MUTBdI9xfG:|aYOgRZN{[Xl? MnS2Nk8yOCEQvF2= MY[yOE81QCCq NWjpclFXcW6mdXPld{BieG:ydH;zbZM> NX\mTnpSOjR4NUm3OFk>
AML2 NWP0bld7TnWwY4Tpc44hSXO|YYm= NEix[4QyOM7:TR?= NYDBRpFXOi92IHi= M1THfIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NHPGe|AzPDZ3OUe0PS=>
AML3 NGGxUJRHfW6ldHnvckBCe3OjeR?= MnXENVDPxE1? Mk\wNk81KGh? NX3YT|l[cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NEOzZY4zPDZ3OUe0PS=>
MOML13 MVjGeY5kfGmxbjDBd5NigQ>? MoDjNVDPxE1? NYTRV3BZOi92IHi= NYrkUJJNcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NVLo[mwzOjR4NUm3OFk>
BeWo M4[3d2Z2dmO2aX;uJGF{e2G7 M{n3VVMxKML3TR?= M3z5e|I1KGh? MWfpcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= M4Lx[FI1PDl6MUW0
BeWo NFzQSYZCeG:ydH;zbZMhSXO|YYm= NHva[ZU{OCEEtV2= M4jKXlI1KGh? MYTpcoNz\WG|ZYOgZZBweHSxc3nz NHL1NlIzPDR7OEG1OC=>
OCI M4Cy[GZ2dmO2aX;uJGF{e2G7 NYX0Oo5VOTBizszN NUXD[GFYOjRiaB?= M2rQfJVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= NYrwfFRtOjR2N{O1OlI>
MOLM MUfGeY5kfGmxbjDBd5NigQ>? MnvENVAh|ryP NGnrUnczPCCq MoKxeZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w NITYeGgzPDR5M{W2Ni=>
U2OS  NEm5S|NHfW6ldHnvckBCe3OjeR?= M37MPFIxKM7:TR?= NG\EZ5gzPCCq MVXpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv M2DPVVI1OzZ4MEC3
RKO MlTOSpVv[3Srb36gRZN{[Xl? NX[4So9MOjBizszN NYX6b|ROOjRiaB?= MorpbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? MoOxNlQ{PjZyMEe=
U2OS  M{DqTGZ2dmO2aX;uJGF{e2G7 MUGyNEDPxE1? M2Do[lI1KGh? NVvWNodNcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MmK0NlQ{PjZyMEe=
RKO NFvwT2xHfW6ldHnvckBCe3OjeR?= NFzaOlMzOCEQvF2= MmDsNlQhcA>? NXTwZnN4cW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MnvKNlQ{PjZyMEe=
SMMC-7721  NHr2eohE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGXDNVgyNjJ3LUKwJO69VQ>? NWDWc2hQOjRxNEivO|IhcA>? MXPEUXNQ MYHpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NVTndpB{OjR{OE[zNVI>
HuH-7 NGLPZpdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVexMlI2NTJyIN88US=> NELmXFYzPC92OD:3NkBp M3y0bmROW09? M{Xle4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MleyNlQzQDZ|MUK=
SMMC-7721  NXi0ZW9RSXCxcITvd4l{KEG|c3H5 NHS4bZkzOCEQvF2= NG[0U2o1QCCq NWjPdmEzTE2VTx?= M37zT4lv\HWlZYOgZZBweHSxc3nz MmHHNlQzQDZ|MUK=
HuH-7 M1HtWmFxd3C2b4Ppd{BCe3OjeR?= M{XQUlIxKM7:TR?= MUK0PEBp Mkm2SG1UVw>? NGTkclNqdmS3Y3XzJIFxd3C2b4Ppdy=> NX\qNWRwOjR{OE[zNVI>
SMMC-7721  M3i4V2Z2dmO2aX;uJGF{e2G7 MlvtNVAh|ryP M1XFfVM3KGh? MVHEUXNQ Mkf4[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> M4XYdVI1Ojh4M{Gy
HuH-7 MUnGeY5kfGmxbjDBd5NigQ>? MX:xNEDPxE1? NUfKd4dMOzZiaB?= NV\UWm53TE2VTx?= NHW1WoRld3ewLYLl[5Vt[XSnczD0bIUheHKxdHXpckBmgHC{ZYPzbY9vKGyndnXsJI9nKHCqb4PwbI8uW2W{M{myMZA2Ow>? M2LldFI1Ojh4M{Gy
AT2 NEDOUIFHfW6ldHnvckBCe3OjeR?= MmO2OU8yOCEQvF2= M3L0WIxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li MYKyOFI1ODJyMx?=
REH MoLSSpVv[3Srb36gRZN{[Xl? NFjv[4o2NzFyIN88US=> M{PxToxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li NEDZTGozPDJ2MEKwNy=>
UoCB6 MXrGeY5kfGmxbjDBd5NigQ>? NFX3ZZY2NzFyIN88US=> NHK0VHZt\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= M4HJ[VI1OjRyMkCz
AT2 NUXCXY1wS2WubDDWbYFjcWyrdImgRZN{[Xl? NXXtO|dDOC1{NTFOwG0> M13xW4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? Mn\rNlQzPDB{MEO=
REH MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4HIeFAuOjVizszN NEDxcpNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MXiyOFI1ODJyMx?=
UoCB6 M2nnZmNmdGxiVnnhZoltcXS7IFHzd4F6 M1HVe|AuOjVizszN NFvKc3RqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MonRNlQzPDB{MEO=
A2780 M172emZ2dmO2aX;uJGF{e2G7 MmHCOU8yOC9{MDFOwG0> M2LxVFI1KGh? MYL1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? NF3iR2czPDF|NkG0Oy=>
H460 NUjncHRDTnWwY4Tpc44hSXO|YYm= NF;scmY2NzFyL{KwJO69VQ>? NX3UToM5OjRiaB?= M4LK[ZVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi M1uwXVI1OTN4MUS3
Lovo  MU\GeY5kfGmxbjDBd5NigQ>? M2HDXFUwOTBxMkCg{txO MnvhNlQhcA>? MWn1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? MlvZNlQyOzZzNEe=
A2780 NV3MV5VtSXCxcITvd4l{KEG|c3H5 MnHKOU8yOC9{MDFOwG0> Mnj4NlQhcA>? M{TlZYVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN M2jLS|I1OTN4MUS3
H460 NXjESZJkSXCxcITvd4l{KEG|c3H5 NH\ndVE2NzFyL{KwJO69VQ>? NXjBfVJrOjRiaB?= NYH4R4Ro\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? MVeyOFE{PjF2Nx?=
Lovo  MmfmRZBweHSxc3nzJGF{e2G7 NH3MXFk2NzFyL{KwJO69VQ>? M2X5OFI1KGh? MkPq[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MVGyOFE{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

    Z-VAD-FMKは細胞透過性、不可逆汎カスパーゼの阻害剤です。

    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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