Nutlin-3

Catalog No.S1061

For research use only.

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.

Nutlin-3 Chemical Structure

CAS No. 890090-75-2

Selleck's Nutlin-3 has been cited by 73 publications

Purity & Quality Control

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Biological Activity

Description Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.
Targets
Mdm2 [5]
(Cell-free assay)
180 nM
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SMMC-7721  NUPOU2VwTnWwY4Tpc44hSXO|YYm= MlzsNVAh|ryP Ml\KN|YhcA>? NFu5U5lFVVOR NYW4OZpz\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NFLX[3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
HuH-7 M4HRUGFxd3C2b4Ppd{BCe3OjeR?= Mnq0NlAh|ryP NYj5WoVLPDhiaB?= NIWzUoxFVVOR MW\pcoR2[2W|IHHwc5B1d3Orcx?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
SMMC-7721  MVTBdI9xfG:|aYOgRZN{[Xl? MWCyNEDPxE1? Mm[0OFghcA>? MnrXSG1UVw>? NIL6RYZqdmS3Y3XzJIFxd3C2b4Ppdy=> NVPSRo9uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPFY{OTJpPkK0Nlg3OzF{PD;hQi=>
HuH-7 MWHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXXTdpl1OS5{NT2yNEDPxE1? NEjpOoczPC92OD:3NkBp M2LKRmROW09? M2n2d4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 M1;lZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mki2N|EzLz5{NEK4OlMyOjxxYU6=
SMMC-7721  M2HrRmNmdGxiVnnhZoltcXS7IFHzd4F6 M{H4[lEvOjVvMkCg{txO NIfXOlEzPC92OD:3NkBp MoqzSG1UVw>? MonNbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NIDGPWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
RKO NH3kfpNHfW6ldHnvckBCe3OjeR?= NX:2b|dsOjBizszN MoPsNlQhcA>? MnvLbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= NH\I[Is9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
U2OS  MlTmSpVv[3Srb36gRZN{[Xl? MYeyNEDPxE1? NFTLbZMzPCCq MnXKbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NkCwO{c,OjR|Nk[wNFc9N2F-
RKO M3LORmZ2dmO2aX;uJGF{e2G7 NWnVemNjOjBizszN MlnvNlQhcA>? NEG2[W5qdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw NHHiTGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
U2OS  NUDK[VlmTnWwY4Tpc44hSXO|YYm= MYeyNEDPxE1? MYWyOEBp M1;5folv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? M4DTOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[2NFA4Lz5{NEO2OlAxPzxxYU6=
MOLM NULMXVFjTnWwY4Tpc44hSXO|YYm= M3vnfVExKM7:TR?= NYr0[WZPOjRiaB?= Mne2eZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w MoTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{O1OlIoRjJ2NEezOVYzRC:jPh?=
OCI NULJPFFvTnWwY4Tpc44hSXO|YYm= NUD5SY1KOTBizszN NIr0dm8zPCCq MU\1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? M2fEWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEezOVYzLz5{NES3N|U3OjxxYU6=
BeWo MYLBdI9xfG:|aYOgRZN{[Xl? M2DFblMxKML3TR?= NXexXJlPOjRiaB?= MUTpcoNz\WG|ZYOgZZBweHSxc3nz MorRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2OUixOVQoRjJ2NEm4NVU1RC:jPh?=
BeWo NXfHZVhJTnWwY4Tpc44hSXO|YYm= Mkf0N|AhyrWP MXKyOEBp NH3zbZFqdmO{ZXHz[ZMheDV|LDDN[I0zNCCyMkGgZY5lKFC3bXGgZZQhfGinIIDyc5RmcW5ibHX2[Yw> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR7OEG1OEc,OjR2OUixOVQ9N2F-
MOML13 NUOzeJBoTnWwY4Tpc44hSXO|YYm= NXrQPGlROTEQvF2= NFzE[ogzNzRiaB?= M1OwXYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NYDnR2tqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVk4PDlpPkK0OlU6PzR7PD;hQi=>
AML3 MnjSSpVv[3Srb36gRZN{[Xl? MUWxNO69VQ>? M2\ON|IwPCCq Mm\RbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= NWK1elh[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVk4PDlpPkK0OlU6PzR7PD;hQi=>
AML2 MYHGeY5kfGmxbjDBd5NigQ>? M17L[|Ex|ryP NIXkOGYzNzRiaB?= MV\pcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= MkLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
MOML13 NVrSU2tQSXCxcITvd4l{KEG|c3H5 NU\lZW9lOi9zMDFOwG0> NVTOSoU6OjRxNEigbC=> MW\pcoR2[2W|IHHwc5B1d3Orcx?= NHjhfno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
AML2 M17oemFxd3C2b4Ppd{BCe3OjeR?= NGrGU|MzNzFyIN88US=> M{\RblI1NzR6IHi= M1fvTYlv\HWlZYOgZZBweHSxc3nz NH7FV|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
U2OS  NIq3TIVHfW6ldHnvckBCe3OjeR?= MYKyNEDPxE1? NX\SNoIzOjRiaB?= NG\o[lNqdmO{ZXHz[ZMhfGinIH3SUmEhdGW4ZXzzJI9nyqCEQ1yyRVEtKEKFTGjMxsBidmSEQ1zX NUW1SFNWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OlczPTlpPkK0PFY4OjV7PD;hQi=>
Hep3B MXfBdI9xfG:|aYOgRZN{[Xl? M3vTZolv\HWlZYOgZZBweHSxc3nz MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Huh-7 NXfzXVh7SXCxcITvd4l{KEG|c3H5 NG\nbYFqdmS3Y3XzJIFxd3C2b4Ppdy=> NHfmXWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
SMMC7721 NWrX[2ViSXCxcITvd4l{KEG|c3H5 NX\i[ZB4cW6mdXPld{BieG:ydH;zbZM> MoT6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
HepG2 NYHxUVJySXCxcITvd4l{KEG|c3H5 NXvnSVQ1cW6mdXPld{BieG:ydH;zbZM> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Hep3B NWjudY9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr0O|IhcA>? MVTEUXNQ MXnJR|UxRTJyLkG4JOKyKDFwOESg{txO MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Huh-7 Mn3YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7QV5hxPzJiaB?= M1PmcWROW09? NYfZcmN5UUN3ME2zN{46PiEEsTCzMlkh|ryP MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
SMMC7721/Ac MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYe3NkBp M{\XTWROW09? MlvyTWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? MoK4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
SMMC7721 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDUO|IhcA>? NFHXO|dFVVOR Mk\3TWM2OD1|MT6yPEDDuSB2LkKg{txO NH3qPXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
HepG2/As MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LwUlczKGh? MnH6SG1UVw>? NU\3cowzUUN3ME22PE4yOyEEsTC5MlYh|ryP NFnDSHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
HepG2 M3TzS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWi3NkBp M3PKWWROW09? Mn[wTWM2OD1|NT64OkDDuSB{Lkmg{txO NX\qVG9IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
MOLM-13 NWnRPWJ[TnWwY4Tpc44hSXO|YYm= MUK2xsDPxE1? MoXJOkBp MYLEUXNQ NXzrfZJD\W6qYX7j[ZMhfGinIHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhUDKEIHHu[EBp\WG2IIPoc4NsKHC{b4TlbY5{KEi|cEK3JIFv\CCKc4C5NC=> Mk[3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OEWwPFIoRjJ2OEi1NFgzRC:jPh?=
MOLM-13 M1m2WGZ2dmO2aX;uJGF{e2G7 NIrPXpo3yqEQvF2= NFjZPG4xNThiaB?= M4DxTGROW09? Mmf6bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZicEWzMEBOTE1{LDDwNlEh[W6mIHHj[ZR6dGG2ZXSgdFU{ M2rNelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi1NFgzLz5{NEi4OVA5OjxxYU6=
115 NU\oflRMTnWwY4Tpc44hSXO|YYm= MmSyOUDPxE1? NV7HZnVwPDhiaB?= NF\hTHZFVVOR NXXKZndNcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> M{m4[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
A498 Ml;oSpVv[3Srb36gRZN{[Xl? M2LLeVUh|ryP MVW0PEBp M4DaT2ROW09? MWnpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi M4HodFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
Caki-2 NUfPeoJvTnWwY4Tpc44hSXO|YYm= M2f4cFUh|ryP MVO0PEBp MY\EUXNQ NXfnSZREcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> MlP4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
ACHN M1f4NGZ2dmO2aX;uJGF{e2G7 M3HnUVUh|ryP MorwOFghcA>? MVzEUXNQ NF\YSHpqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
115 MkmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYOwdoRrPSEQvF2= NELlPZM1QCCq MorJSG1UVw>? M1G5Z4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
A498 MmTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmq4OUDPxE1? NXrveXhGPDhiaB?= NEXnPZZFVVOR MWTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= Mn;wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
Caki-2 MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXXOUDPxE1? Ml\COFghcA>? M2W3cGROW09? Ml;SbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg M3LTbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
ACHN NWn4S|N1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHrfJBIPSEQvF2= M1\GeFQ5KGh? MmH4SG1UVw>? NWK5XVRjcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
115 MVTGeY5kfGmxbjDBd5NigQ>? NF;rSFQxNjVxMT:1JO69VQ>? Mn25OFghcA>? Mn7iSG1UVw>? M1nVV4xm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
A498 NUeyZpN5TnWwY4Tpc44hSXO|YYm= Mo\DNE42NzFxNTFOwG0> MnLiOFghcA>? NXHDcmlVTE2VTx?= MlvKcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? NVvnXJczRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
Caki-2 MXnGeY5kfGmxbjDBd5NigQ>? NHf6TlMxNjVxMT:1JO69VQ>? MnTyOFghcA>? NFzxSYVFVVOR NWfVRoFEdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= MkPZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
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UoCB6 M4r5[WZ2dmO2aX;uJGF{e2G7 NV;ZWIl{PS9zMDFOwG0> MYDs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? NI\IVWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK0NFIxOyd-MkSyOFAzODN:L3G+
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REH M2KwRWNmdGxiVnnhZoltcXS7IFHzd4F6 NEnEcoMxNTJ3IN88US=> NFP6bYdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 Mn3oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NECyNFMoRjJ2MkSwNlA{RC:jPh?=
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A2780 NEDOd5pHfW6ldHnvckBCe3OjeR?= MlXOOU8yOC9{MDFOwG0> MViyOEBp M2LIb5VxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NHTNdZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGzOlE1Pyd-MkSxN|YyPDd:L3G+
H460 NF\3RW1HfW6ldHnvckBCe3OjeR?= MVi1M|ExNzJyIN88US=> NHPjXXozPCCq NU\U[YRpfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= NXHTfINNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxN|YyPDdpPkK0NVM3OTR5PD;hQi=>
Lovo  NUDBVI5uTnWwY4Tpc44hSXO|YYm= Mk\aOU8yOC9{MDFOwG0> NEnsUpIzPCCq NEHvWHR2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= Ml24QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzM{[xOFcoRjJ2MUO2NVQ4RC:jPh?=
A2780 M{[wemFxd3C2b4Ppd{BCe3OjeR?= Moi0OU8yOC9{MDFOwG0> MWKyOEBp M3;lb4VvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF|NkG0O{c,OjRzM{[xOFc9N2F-
H460 M{LFfWFxd3C2b4Ppd{BCe3OjeR?= NF[0d2w2NzFyL{KwJO69VQ>? NH7me5ozPCCq MkXF[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF|NkG0O{c,OjRzM{[xOFc9N2F-
Lovo  MUPBdI9xfG:|aYOgRZN{[Xl? Mo\3OU8yOC9{MDFOwG0> NFHsV4szPCCq M2LGNYVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN MoCzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzM{[xOFcoRjJ2MUO2NVQ4RC:jPh?=
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U343MG Ml;5RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MWq0PEBpenN? MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV|NEPNS{Bk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBxPTNiYX\0[ZIhPDhiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDF{Lk[g{txONg>? M33QXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEWwO|gzLz5{N{C1NFc5OjxxYU6=
SW620 NY[1WXh{S3m2b4TvfIlkcXS7IHHzd4F6 NFTRSVY4OiCqcoO= MonuR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3c3OjBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOzhizszNMi=> NEfRWJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5EcEWPQly8M4E,
A549 NXvXOHpwS3m2b4TvfIlkcXS7IHHzd4F6 NGjxWY04OiCqcoO= MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTCwMlQyKM7:TT6= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7DbGVOSkx:L3G+
SJSA1 NVHPd2VsS3m2b4TvfIlkcXS7IHHzd4F6 MWW3NkBpenN? MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTnNCOSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNU45OSEQvF2u MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7DbGVOSkx:L3G+
HCT116 MYPDfZRwfG:6aXPpeJkh[XO|YYm= NGfFZVU4OiCqcoO= MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFQvPjNizszNMi=> M2\CeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQmNpTU2ETEyvZV4>
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Assay
Methods Test Index PMID
Western blot MDM2 / p53 / ALKBH2 / p21 / PUMA ; RRM1 / RRM2 / p53R2 / p21 / p53 / pS6 / S6 23258843 28507282
Immunofluorescence Lamin A / Lamin C / p16 / H3K9me3 ; Merlin / cyclin D1 / p53 / MDM2 ; p53 30728349 30274821 24286312
Growth inhibition assay Cell viability 29286113
In vivo 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]

Protocol (from reference)

Kinase Assay:

[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

Cell Research:

[1]

  • Cell lines: HCT116, RKO, SJSA-1, SW480, and MDA-MB-435
  • Concentrations: Dissolved in DMSO, final concentrations ~ 30 μM
  • Incubation Time: 8, 24, and 48 hours
  • Method:

    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.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: Athymic female nude mice (Nu/Nu-nuBR) injected subcutaneously with SJSA-1 cells
  • Dosages: 200 mg/kg
  • Administration: Orally, twice a day
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(171.96 mM)
Ethanol 30 mg/mL
(51.59 mM)
Water 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.

Chemical Information

Molecular Weight 581.5
Formula

C30H30Cl2N4O4

CAS No. 890090-75-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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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.

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