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。

価格 在庫  
USD 138 あり
USD 214 あり
USD 233 あり
USD 466 あり
USD 1222 あり

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)

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 Mke5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7JdVljPcLizszN Mn\aOFjDqGh? NWjpOmVt[myxY3vzJFI4NU:KQz3pcoR2[2WmIHPlcIwheHKxbHnm[ZJifGmxbjDjc41x[XKjYnzlJJRwKHSqYYSgc4Yh[mG|YXygcIV3\Wy| M2mwOVI3OzVyNU[1
NP69 MkHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP2TWM2OD1|MT62PeKyOi53NDFOwG0> NGDTbY8zPjJ3MkW3OS=>
NP460 NXrJRmN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHOVXZKSzVyPUKyMlg2yrFzLkG4JO69VQ>? MmLvNlYzPTJ3N{W=
C666-1 MoPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TlTGlEPTB;MUmuPVXDuThwOUOg{txO MYOyOlI2OjV5NR?=
C666-1 MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Ml\HNVAhyrWP NU[xeVA6PDhiaB?= MYfEUXNQ M2jIZZNmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJJRp\SCleYTveI95cWNiZX\m[YN1KG:oIHPpd5Bt[XSrbh?= MUiyOlI2OjV5NR?=
C666-1  NXHsd2tFTnWwY4Tpc44hSXO|YYm= M2W3UlExKML3TR?= NWXjVoJOOjRiaB?= NVP3fYZLTE2VTx?= MXfhZ5RqfmG2ZYOgeIhmKHB3MzDwZZRpf2G7LDD1dJJm\3WuYYTpcocheDV|LDDwNlEh[W6mIF3kcVI> MVSyOlI2OjV5NR?=
C666-1 NGG4cItCeG:ydH;zbZMhSXO|YYm= NFPPR|kyOCEEtV2= NFzV[|I1QC95MjDo NHXO[HVFVVOR MXjz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzDjbZNxdGG2aX6tbY5lfWOnZDDhdI9xfG:|aYO= MkXUNlYzPTJ3N{W=
A549 M3KwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\QNlQhcA>? MWjJR|UxRTF5Lk[4JOKyKDRwNUKg{txO Ml;QNlYyOjV{M{C=
A549-NTC NV3MO5V5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjzcIpZOjRiaB?= M4\qSWlEPTB;MUmuOFIhyrFiMT65OkDPxE1? M3HOcVI3OTJ3MkOw
A549-920 NHjsSGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWD3Z5Y{OjRiaB?= M2L2cWlEPTB;M{OuPFUhyrFiND64OEDPxE1? NYDVTHRFOjZzMkWyN|A>
CRL-5908 Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor5NlQhcA>? Mn3QTWM2OD1|OD63NUDDuSB{LkSzJO69VQ>? M4\E[VI3OTJ3MkOw
L6 NIT0VFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPXbIoyOMLizszNxsA> NF7jTogzPC92OD:3NkBp M4LTdGROW09? NG\4T4ZqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? M4fOSVI2QDdzN{m0
C2C12 M3nLOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjIVHAyOMLizszNxsA> NEGzRnMzPC92OD:3NkBp MUHEUXNQ NIXFUIVqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? MkS0NlU5PzF5OUS=
MCF-7  MWHGeY5kfGmxbjDBd5NigQ>? NGDl[pcyOMLizszN NGnueGFFVVOR NFjmTFVqdmirYnn0d{BkgWOuaX6gSFEh[W6mIFTpZ4VzyqB? M2[3W|I2PzB{N{Cz
DU4475  NGLVU4JHfW6ldHnvckBCe3OjeR?= NIPmb242NzFyL{KwJO69VQ>? MkfxNlTDqGh? MonV[I94dnKnZ4XsZZRmeyCWb3PhMVEh\G:|ZTDk[ZBmdmSnboTsfS=> NG\WZ2QzPTV2N{G3OC=>
SMMC-7721 M1rxNGZ2dmO2aX;uJGF{e2G7 MkDJNVAh|ryP NYnyTIU3PDhiaB?= M324[GROW09? MoXhZ4F2e2W|IFTORUBFW0JiZHHtZYdm MYeyOVU1PDN4MR?=
SMMC-7721 NEjGOWlHfW6ldHnvckBCe3OjeR?= NFLWNHkyOCEQvF2= M1T0bFQ5KGh? MlHQSG1UVw>? NFrqe5pqdmS3Y3XzJJRp\SClaILvcYF1cW5vYn;1coQheHKxdHXpckBKTklzNjD0c{Bx[XK2aXHscJkhdG:lYXzpfoUhcW5idHjlJIN6fG:ybHHzceKh MmXXNlU2PDR|NkG=
SMMC-7721 NW\aT4JuTnWwY4Tpc44hSXO|YYm= Mkn1NVAh|ryP MnzKOFghcA>? NF3oPVNFVVOR MXjpcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2cEoFnGUmIyyqCvUl7B MVyyOVU1PDN4MR?=
SMMC-7721 NVTCVYJUTnWwY4Tpc44hSXO|YYm= M3npOVExKM7:TR?= MoDxN|YhcA>? MUXEUXNQ MYjjZZV{\XNidHjlJIVkfG:yaXOg[ZhxemW|c3nvckBw\iCLRlmxOi=> NVrDVIkxOjV3NESzOlE>
MCF-7 NULMOYlHTnWwY4Tpc44hSXO|YYm= MXexNOKh|ryP NWHpUohbOC1{NDDo NInoR3pqdmS3Y3XzJJA2OyCjbnSgdFIyN0OrcEG= MViyOVQ5OjN5Mx?=
OVCAR10 NX7HU4VqTnWwY4Tpc44hSXO|YYm= NInhUFUyOMLizszN NIHodXUzOWkEoB?= MXPEUXNQ NGTmPXVqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ MlzRNlU1OjZ3NEi=
NCI-H23 MXLGeY5kfGmxbjDBd5NigQ>? M2XzclExyqEQvF2= M{f6c|IycMLi MW\EUXNQ MUPpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz NIXwN2wzPTR{NkW0PC=>
A2780 MlPNSpVv[3Srb36gRZN{[Xl? MXOxNOKh|ryP M4[2VVIycMLi MkW5SG1UVw>? NFmxTWNqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ MmXINlU1OjZ3NEi=
NCI-H23 MkjXSpVv[3Srb36gRZN{[Xl? NHXUNXUyOMLizszN MXSyNYjDqA>? Mnu1SG1UVw>? M1rscIRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz MYKyOVQzPjV2OB?=
A2780 NVnpVVkyTnWwY4Tpc44hSXO|YYm= NYj1bZZ{OTEEoN88US=> MnvZNlFpyqB? NHfFO2pFVVOR NWHORYJY\GWlcnXhd4V{KHSqZTDGc5hOOSCuZY\lcJM> MUGyOVQzPjV2OB?=
HCT116  M{LsWmZ2dmO2aX;uJGF{e2G7 NUP0botROTBiwsXN MmO1NlQhcA>? NGWyVW5k[XW|ZYOgZUBxPTNvZHXw[Y5l\W62IITleJJieGyxaXSgS|Eu[XK{ZYP0JIlvKGSrcHzvbYQhUEOWMUG2JINtd26nczDEN{BidmRiREi= NVfPfmk3OjV|OECwOVU>
MCF-10CA1a NGriSGtHfW6ldHnvckBCe3OjeR?= Mne4NVDDqM7:TR?= NHLDV5Q1QCCq NH7qZo1FVVOR NX;YN5QycW6qaXLpeJMh[mG|YXygbY53[XOrb36gZY5lKHKnZIXj[YQhXEeILd8yN{1qdmS3Y3XkJIlvfmG|aX;uJJRwKGKjc3HsJIxmfmWucx?= M3i0dFI2OjV5N{K5
MCF-10A1  M1\Rb2Z2dmO2aX;uJGF{e2G7 M1vYOlExyqEQvF2= MoLYNlQwPDhiaB?= NE[zbIlFVVOR NXfyd2ZmcW6qaXLpeJMhdWmpcnH0bY9vKG:oIH7vdo1idCCkcnXhd5Qh\XCrdHjlcIlidMLi NGDDRXozPTJ3N{eyPS=>
MCF-10CA1a NU\6WGhvTnWwY4Tpc44hSXO|YYm= MVexNOKh|ryP NVL2cYlCOjRiaB?= MWTEUXNQ NEP0VXJl\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= MX[yOVI2Pzd{OR?=
MCF-10CA1a MmXVSpVv[3Srb36gRZN{[Xl? MnO3NVDDqM7:TR?= MVeyOEBp NVnEWG1JTE2VTx?= MUfpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? M1;FXFI2OjV5N{K5
SK-BR-7 MVPGeY5kfGmxbjDBd5NigQ>? M4HydFExyqEQvF2= MkHjNlQhcA>? MlvQSG1UVw>? MXzpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? NEXNbGMzPTJ3N{eyPS=>
SUM102PT MWrGeY5kfGmxbjDBd5NigQ>? NV3pSZl4OTEEoN88US=> MmmyNlQhcA>? MmX1SG1UVw>? M4PTWolvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= NFK2dY8zPTJ3N{eyPS=>
RAW 264.7 MofsSpVv[3Srb36gRZN{[Xl? NHvOfY4yOMLizszN MVGzNEBucW5? NXXsS2dMeHKndnXueJMhfGinIIC1N{Bz\WS3Y4Tpc44hcW5icnXzdI9ve2VidH:gUHBU NFvacmYzPTF5MkW0Oy=>
RAW 264.7 MV\GeY5kfGmxbjDBd5NigQ>? NUezUYl5OTEEoN88US=> NFLmR5Q{OCCvaX6= M3fLN5Jm\HWlZYOgeIhmKEySUz3heYdu\W62ZXSgeIhmKE6ILd86RkBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZYN1cX[rdIm= M2PsOFI2OTd{NUS3
RAW 264.7 NYi0eoRoTnWwY4Tpc44hSXO|YYm= MoLrNVDDqM7:TR?= NIrMeGo{OCCvaX6= MYXpcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= Mn7HNlUyPzJ3NEe=
MCF7  Ml;UR4VtdCCYaXHibYxqfHliQYPzZZk> NUfpUXpYOi53INM1US=> NIfLNIw2KGR? MXHEUXNQ M1jKSpNmdnOrdHn6[ZMhVUOINzD0c{BRSVKSIHnubIljcXSrb36= M3fE[VI2ODh3OUCy
MCF7  NUfDZYZ1TnWwY4Tpc44hSXO|YYm= MWGyMlUhyrWP NXu2SYFvPDhiaB?= Mkf2SG1UVw>? NEXl[Xpl\WO{ZXHz[ZMhfGinIHjvcY9td2exdYOgSHNDKHKncHHpdkBnemWzdXXuZ4lmew>? M3XzW|I2ODh3OUCy
ACHN NIrqfZdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MViwMlUuOTBizszN NWL1TlJSOC14IHS= NGLuRnJFVVOR M3LjN4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mlz1NlUxPjd5OEe=
Caki-2 M{\xW2NmdGxiVnnhZoltcXS7IFHzd4F6 MXGwMlUuOTBizszN MXiwMVYh\A>? MV3EUXNQ MmnGbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1vhS|I2ODZ5N{i3
A498 NFvLbJpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVPsUnE2OC53LUGwJO69VQ>? MWiwMVYh\A>? MXfEUXNQ MV7pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUSyOVA3Pzd6Nx?=
115 Mo\ZR4VtdCCYaXHibYxqfHliQYPzZZk> MoO3NE42NTFyIN88US=> Mly3NE03KGR? NHm2UWtFVVOR NUT4ZlJ4cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MlfoNlUxPjd5OEe=
117 NVvvUlZuS2WubDDWbYFjcWyrdImgRZN{[Xl? M1Oyc|AvPS1zMDFOwG0> NV\FSWdSOC14IHS= NXrnNnZ5TE2VTx?= MniybY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NW\Bc|B3OjVyNke3PFc>
ACHN M2rDbGZ2dmO2aX;uJGF{e2G7 NV[1W5ZYOC53L{GvOUDPxE1? NFjlbG81QCCq MlH4SG1UVw>? MYLs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MY[yOVA3Pzd6Nx?=
Caki-2 NH\mPZdHfW6ldHnvckBCe3OjeR?= NGDGSnUxNjVxMT:1JO69VQ>? NFfqSJU1QCCq NVLkRWRqTE2VTx?= MY\s[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NF3lZ3MzPTB4N{e4Oy=>
A498 Mn;xSpVv[3Srb36gRZN{[Xl? NE[yZ|kxNjVxMT:1JO69VQ>? MVq0PEBp NIXoc3hFVVOR MnXacIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? NHW2[ZAzPTB4N{e4Oy=>
115 MlPPSpVv[3Srb36gRZN{[Xl? NFvHR40xNjVxMT:1JO69VQ>? MnHaOFghcA>? M{DhfmROW09? NXfXUVBSdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NILqcIkzPTB4N{e4Oy=>
ACHN MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\R[3M2KM7:TR?= Mo\WOFghcA>? NV\QOmJlTE2VTx?= MVfpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MkGxNlUxPjd5OEe=
Caki-2 NHrCdnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWi1JO69VQ>? NWnzSYN6PDhiaB?= M{\J[2ROW09? NXvJZXJjcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MWmyOVA3Pzd6Nx?=
A498 M1T5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37xe|Uh|ryP MVS0PEBp M3;SZWROW09? MWrpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MnvxNlUxPjd5OEe=
115 NWnmWVFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGW0bIc2KM7:TR?= M1\uflQ5KGh? NUDoTotZTE2VTx?= MojXbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg NFnVNIwzPTB4N{e4Oy=>
ACHN M{T1NWZ2dmO2aX;uJGF{e2G7 MXW1JO69VQ>? MYq0PEBp MWLEUXNQ M{\qRolv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= Ml:yNlUxPjd5OEe=
Caki-2 Mo[1SpVv[3Srb36gRZN{[Xl? MkSzOUDPxE1? NU\uU2k2PDhiaB?= MXjEUXNQ MWLpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NWKwc49qOjVyNke3PFc>
A498 Mk\VSpVv[3Srb36gRZN{[Xl? MlWyOUDPxE1? NYj2TnRpPDhiaB?= M2HNZWROW09? MnHSbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MUOyOVA3Pzd6Nx?=
115 NUDUTXBpTnWwY4Tpc44hSXO|YYm= Mor1OUDPxE1? Mo\tOFghcA>? M1LOdmROW09? MmfobY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MnvmNlUxPjd5OEe=
MOLM-13 M1;Rb2Z2dmO2aX;uJGF{e2G7 NWHiXVU6PsLizszN M{XjTVAuQCCq MnrUSG1UVw>? NUTubWtKcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gdFU{NCCPRF2yMEBxOjFiYX7kJIFk\XS7bHH0[YQheDV| NITzZ4ozPDh6NUC4Ni=>
MOLM-13 MXLGeY5kfGmxbjDBd5NigQ>? M1Ly[FbDqM7:TR?= NYDtZmJKPiCq MVPEUXNQ MmT0[Y5p[W6lZYOgeIhmKGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFJDKGGwZDDo[YF1KHOqb3PrJJBzd3SnaX7zJGh{eDJ5IHHu[EBJe3B7MB?= M2TLd|I1QDh3MEiy
HepG2 M3XTfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS3NkBp NHW3dmFFVVOR NIPhU3BKSzVyPUO1Mlg3KMLzIEKuPUDPxE1? M1TWcFI1QDh2OEC5
HepG2/As NFG3V|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXsR3c2PzJiaB?= NYfOTlA5TE2VTx?= NIXRO2dKSzVyPU[4MlE{KMLzIEmuOkDPxE1? Ml7kNlQ5QDR6MEm=
SMMC7721 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\sO|IhcA>? MmTUSG1UVw>? MkLZTWM2OD1|MT6yPEDDuSB2LkKg{txO NInKNJAzPDh6NEiwPS=>
SMMC7721/Ac NGXlN4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DrVlczKGh? MlXRSG1UVw>? NFPPWFRKSzVyPUW1MlIyKMLzIEWuNFMh|ryP M1faeVI1QDh2OEC5
Huh-7 M{LDZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFy3TGk4OiCq MUjEUXNQ MkLWTWM2OD1|Mz65OkDDuSB|Lkmg{txO NHXETYczPDh6NEiwPS=>
Hep3B MlznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYC3NkBp NWGwT3BbTE2VTx?= NFi2dWFKSzVyPUKwMlE5KMLzIEGuPFQh|ryP NFv0WGczPDh6NEiwPS=>
HepG2 NHXUTVRCeG:ydH;zbZMhSXO|YYm= MlmwbY5lfWOnczDhdI9xfG:|aYO= M3jtcVI1QDh2OEC5
SMMC7721 NGjYTGZCeG:ydH;zbZMhSXO|YYm= M{HxXolv\HWlZYOgZZBweHSxc3nz M2XUbFI1QDh2OEC5
Huh-7 NWfS[406SXCxcITvd4l{KEG|c3H5 M{T3O4lv\HWlZYOgZZBweHSxc3nz MVqyOFg5PDhyOR?=
Hep3B NITWWFBCeG:ydH;zbZMhSXO|YYm= M1:xS4lv\HWlZYOgZZBweHSxc3nz M3HuZVI1QDh2OEC5
U2OS  MXfGeY5kfGmxbjDBd5NigQ>? NXTxR3ZUOjBizszN NEnme5QzPCCq NHjqZ4NqdmO{ZXHz[ZMhfGinIH3SUmEhdGW4ZXzzJI9nyqCEQ1yyRVEtKEKFTGjMxsBidmSEQ1zX Mm\ENlQ5Pjd{NUm=
AML2 MoLTRZBweHSxc3nzJGF{e2G7 NFHufXAzNzFyIN88US=> MkjuNlQwPDhiaB?= MnzPbY5lfWOnczDhdI9xfG:|aYO= M{TF[lI1PjV7N{S5
MOML13 MU\BdI9xfG:|aYOgRZN{[Xl? Mmf2Nk8yOCEQvF2= M{DE[lI1NzR6IHi= MoP6bY5lfWOnczDhdI9xfG:|aYO= M2[yb|I1PjV7N{S5
AML2 NXfNSmczTnWwY4Tpc44hSXO|YYm= MmLkNVDPxE1? M3LVZ|IwPCCq NEfUeY5qdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> M{fGSFI1PjV7N{S5
AML3 M2TiZ2Z2dmO2aX;uJGF{e2G7 MoLZNVDPxE1? MUCyM|QhcA>? M3LPc4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NVPBXZNkOjR4NUm3OFk>
MOML13 MX;GeY5kfGmxbjDBd5NigQ>? MX6xNO69VQ>? MYWyM|QhcA>? NH7E[WpqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> MVSyOFY2QTd2OR?=
BeWo NVexRmprTnWwY4Tpc44hSXO|YYm= MmnIN|AhyrWP MYOyOEBp M4TadIlv[3KnYYPld{BxPTNuIF3kcVItKHB{MTDhcoQhWHWvYTDheEB1cGVicILveIVqdiCuZY\lcC=> M{jvT|I1PDl6MUW0
BeWo MmTJRZBweHSxc3nzJGF{e2G7 NXP2R2MzOzBiwsXN NVnoZmlZOjRiaB?= MX\pcoNz\WG|ZYOgZZBweHSxc3nz NX\VfpZkOjR2OUixOVQ>
OCI NUD6WlFETnWwY4Tpc44hSXO|YYm= NH2yXJkyOCEQvF2= M4r3OFI1KGh? MVz1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? MUWyOFQ4OzV4Mh?=
MOLM MnvvSpVv[3Srb36gRZN{[Xl? MormNVAh|ryP M1\lTVI1KGh? NUTvO2dOfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u M{fKU|I1PDd|NU[y
U2OS  MmjySpVv[3Srb36gRZN{[Xl? MWGyNEDPxE1? M4i4SVI1KGh? MnfBbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? NFfETZIzPDN4NkCwOy=>
RKO MX7GeY5kfGmxbjDBd5NigQ>? NFHpN|YzOCEQvF2= MormNlQhcA>? NYmyNY5ncW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= MVeyOFM3PjByNx?=
U2OS  M{G2eWZ2dmO2aX;uJGF{e2G7 MVyyNEDPxE1? MVOyOEBp Mn;PbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= MknlNlQ{PjZyMEe=
RKO Mn3ESpVv[3Srb36gRZN{[Xl? MlizNlAh|ryP NEfHdo0zPCCq NUnSZVFscW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> NIf4UYYzPDN4NkCwOy=>
SMMC-7721  MUPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWLqXIhKOS5{NT2yNEDPxE1? MkWyNlQwPDhxN{KgbC=> MUnEUXNQ M4jEdIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 M17ZVFI1Ojh4M{Gy
HuH-7 M2T3TmNmdGxiVnnhZoltcXS7IFHzd4F6 NHm0elUyNjJ3LUKwJO69VQ>? NVvIPYpsOjRxNEivO|IhcA>? NWH2NGo1TE2VTx?= M1vuXYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NFnoOXczPDJ6NkOxNi=>
SMMC-7721  M2HUSGFxd3C2b4Ppd{BCe3OjeR?= Mny0NlAh|ryP MmnpOFghcA>? M2ezdmROW09? NHj4WGhqdmS3Y3XzJIFxd3C2b4Ppdy=> M{LSe|I1Ojh4M{Gy
HuH-7 MmXpRZBweHSxc3nzJGF{e2G7 MWiyNEDPxE1? M4XxTlQ5KGh? M1L6V2ROW09? NV7mS4pncW6mdXPld{BieG:ydH;zbZM> NH\lV5ozPDJ6NkOxNi=>
SMMC-7721  Ml76SpVv[3Srb36gRZN{[Xl? NYLpNJhDOTBizszN MV:zOkBp MnHQSG1UVw>? M2rEUYRwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ MV:yOFI5PjNzMh?=
HuH-7 MoC5SpVv[3Srb36gRZN{[Xl? M{D6N|ExKM7:TR?= NX3ycHBmOzZiaB?= NHPsOoFFVVOR NIDINJVld3ewLYLl[5Vt[XSnczD0bIUheHKxdHXpckBmgHC{ZYPzbY9vKGyndnXsJI9nKHCqb4PwbI8uW2W{M{myMZA2Ow>? MnqyNlQzQDZ|MUK=
AT2 MnXDSpVv[3Srb36gRZN{[Xl? NYK5c4R1PS9zMDFOwG0> NVHxWHJpdGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NU\oU3pDOjR{NECyNFM>
REH M3TZb2Z2dmO2aX;uJGF{e2G7 NXrpR4V6PS9zMDFOwG0> MXTs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? MlS5NlQzPDB{MEO=
UoCB6 NX;idpJUTnWwY4Tpc44hSXO|YYm= NU\uVWFMPS9zMDFOwG0> MX3s[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? MX:yOFI1ODJyMx?=
AT2 MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnXpNE0zPSEQvF2= MXfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MWGyOFI1ODJyMx?=
REH MnrwR4VtdCCYaXHibYxqfHliQYPzZZk> M1T5TFAuOjVizszN MYTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NIrUSmwzPDJ2MEKwNy=>
UoCB6 MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MlzaNE0zPSEQvF2= NX70WXJMcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= Mo\nNlQzPDB{MEO=
A2780 Mn7iSpVv[3Srb36gRZN{[Xl? NIf0Xm02NzFyL{KwJO69VQ>? NEHYT3ozPCCq MXz1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? MViyOFE{PjF2Nx?=
H460 NWroNIxmTnWwY4Tpc44hSXO|YYm= NVXxeWFQPS9zMD:yNEDPxE1? MXuyOEBp MmjGeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? M4PuUlI1OTN4MUS3
Lovo  Mk\pSpVv[3Srb36gRZN{[Xl? NHzUeno2NzFyL{KwJO69VQ>? MXuyOEBp MmrJeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? M1XGSlI1OTN4MUS3
A2780 NGi5O21CeG:ydH;zbZMhSXO|YYm= NF7tVJY2NzFyL{KwJO69VQ>? NEfMR4gzPCCq MnfE[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> M3;qVFI1OTN4MUS3
H460 MnjvRZBweHSxc3nzJGF{e2G7 MmHOOU8yOC9{MDFOwG0> NIDwVIEzPCCq MUXlcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> MYOyOFE{PjF2Nx?=
Lovo  NGXwNnNCeG:ydH;zbZMhSXO|YYm= NF3rZZk2NzFyL{KwJO69VQ>? NGLQeFMzPCCq NYHENoZL\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? MXKyOFE{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 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

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。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related Mdm2 阻害剤

  • Idasanutlin (RG-7388)

    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。

最近チェックしたアイテム

Tags: Nutlin-3を買う | Nutlin-3供給者 | Nutlin-3を購入する | Nutlin-3費用 | Nutlin-3生産者 | オーダーNutlin-3 | Nutlin-3代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ