Nutlin-3a

Catalog No.S8059 Synonyms: (-)-Nutlin-3

For research use only.

Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.

Nutlin-3a Chemical Structure

CAS No. 675576-98-4

Selleck's Nutlin-3a has been cited by 59 publications

Purity & Quality Control

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Biological Activity

Description Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
Features Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.
Targets
p53-MDM2 interaction [3]
(Cell-free assay)
90 nM
In vitro

Nutlin-3a displaces p53 from the binding pocket of MDM2 and thereby releases p53 from inhibition and proteasomal degradation, leading to induction of its downstream targets, cell cycle arrest, and apoptosis. Seven days of incubation with 10 μM nutlin-3a led to >90% inhibition of NIH3T3 cells’ growth[1]. Nutlin-3a stabilizes and activates p53, and induces p21 expression in a dose-dependent manner[1]. Nutlin-3a effectively depletes the S-phase compartment to 0.2-2% and increases the G1- and G2/M-phase compartments[1]. Nutlin-3a induces apoptosis in ~60% of SJSA-1 and MHM cells after 40 h, which increased further after 60 h (85% and 65%, respectively) [1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 Ml:xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;LS|BKSzVyPUCuOlEzOzdizszN MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
H4 M4nVc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nrPGlEPTB;MD62OlI5KM7:TR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
PA-1 NUPZOlA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwOEewPVYh|ryP M1jWUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
NKM-1 NVTt[WNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\H[VlKSzVyPUGuNFQ6OzFizszN NVLhUJRHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
NEC8 M1zUdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFwMkG1O|Ih|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
EoL-1-cell M{HvVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnhe5pKSzVyPUGuNlY4ODFizszN M1f1[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
K5 MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\0[pVKSzVyPUGuOFIxPzJizszN NU\sdXZ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
QIMR-WIL M3\YSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjQWolEUUN3ME2xMlYxQDV2IN88US=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
MOLT-16 NUj1SVg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTFwN{i2NFQh|ryP NEO1cJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
CHP-212 NEnheIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PFWGlEPTB;MT64NVM3QSEQvF2= NFjD[mQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
CTB-1 M{jsVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTJwMEKyOFYh|ryP NEizcXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
MOLT-4 M13McWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:1emd2UUN3ME2yMlMzQDV|IN88US=> NGXld4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
A101D Ml;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\TTWM2OD1{LkO1NFEh|ryP M4rzUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
DOHH-2 NEPBRZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTJwNEKyO|kh|ryP Ml:4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
ES4 MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jzV2lEPTB;Mj60N|E2PSEQvF2= NE\3c2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
SW780 MlXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDOPY1lUUN3ME2yMlUxQDh|IN88US=> M2ruOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
VA-ES-BJ MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zHOGlEPTB;Mj61OFEyKM7:TR?= NVLvPWo2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
RPMI-8866 NH\xTmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[xSmlEPTB;Mj61OlIyPCEQvF2= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
ML-2 M1\pSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrMV5VKSzVyPUKuOVY2PzZizszN NGXhdJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
MSTO-211H MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j2OWlEPTB;Mj61O|Q2OSEQvF2= MmPCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
JVM-3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TZSGlEPTB;Mj61PVMzPCEQvF2= MmPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
A3-KAW M3X6TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDlbIdKSzVyPUKuOlE5OThizszN M1rxWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
DK-MG NWPZSoFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\KXlFKSzVyPUKuOlI1PzFizszN NHHQNIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
LNCaP-Clone-FGC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPNTppuUUN3ME2yMlY1OzF6IN88US=> NWnZeoVMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
HT-144 NHnuWGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJwNkS1O|ch|ryP NFvTe4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
NB69 NXjkZolbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJwNkWzN|Qh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
A172 MoflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfjZWlNUUN3ME2yMlY4PTh6IN88US=> MnLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
RS4-11 NU\JZ4hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jmOmlEPTB;Mj63NlQxPyEQvF2= NHXON4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
DU-4475 NITtcXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDUTWM2OD1{Lke5OVAzKM7:TR?= MnvFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
SJSA-1 MnT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3H2TGlEPTB;Mj64NlU2PiEQvF2= NFe3bIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
BV-173 Ml7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTJwOES0N|kh|ryP M3vq[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
U-2-OS NYPGVGpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rF[2lEPTB;Mj65NVA4KM7:TR?= M2jkNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
CHP-134 NVS3[o06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJwOUO4PFIh|ryP MojUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
D-502MG NHfabZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nnUGlEPTB;Mj65O|E2PCEQvF2= NVPDcFQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
KS-1 MnLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDBTWM2OD1|LkCxOlI{KM7:TR?= NGS3W|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
A204 M3Pi[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjlOoo1UUN3ME2zMlA2PTh6IN88US=> NVHtdIVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
KGN MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInKVoZKSzVyPUOuNFg1QTZizszN M3;SelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
NCI-H292 NYC3W2JnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPHTWVjUUN3ME2zMlEzODJ6IN88US=> NF;wfWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
CAKI-1 MorHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTsTWM2OD1|LkGyOlk1KM7:TR?= MmrzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
C2BBe1 MoLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTNwMUewNlYh|ryP NHPN[mg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
NB10 Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfMTWM2OD1|LkKwPVY3KM7:TR?= M3GzOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
MHH-NB-11 NFzkenJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mni5TWM2OD1|LkK2PFI4KM7:TR?= NH3OSZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
NCI-SNU-1 M4nFdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTNwMke4OFMh|ryP M{nyRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
HCT-116 Ml7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfrNnlKSzVyPUOuN|A{OzVizszN NH7mN209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
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MCF7 MX;BdI9xfG:|aYOgZZN{[Xl? MnzJN{B2VQ>? NYTDTIZEOjRidH:gO|IhcHK| NFnERolKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5icEKxJIV5eHKnc4Ppc44hdGW4ZXygZZQhOyC3TTDh[pRmeiB{NDD0c{A4OiCqcoOgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzhyMkexOkc,OjN6MEK3NVY9N2F-
MCF7 M3T6UGFxd3C2b4Ppd{Bie3OjeR?= NXnLN5RpOyC3TR?= NFfvR2UzPCC2bzC3NkBpenN? NWq2OJR2UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIFLjcE15WyCneIDy[ZN{cW:wIHzleoVtKGG2IEOgeW0h[W[2ZYKgNlQhfG9iN{KgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdiYX7hcJl{cXN? MmDoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MEK3NVYoRjJ|OECyO|E3RC:jPh?=
MCF7 MYfBdI9xfG:|aYOgZZN{[Xl? M4\vb|UxKG6P M2\rZVI1KHSxIEeyJIhzew>? M2DsPGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25ib3[gZ4F{eGG|ZT2zJINt\WG4YXflJJBzd2S3Y4SgZZQhPTBibl2gZYZ1\XJiMkSgeI8hPzJiaILzJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> MkDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MEK3NVYoRjJ|OECyO|E3RC:jPh?=
MCF7 M{PH[mNmdGxiY4njcIUh[XO|YYm= MVSzJJVO NWTNT2F3OjRidH:gO|IhcHK| NF3UPJdE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMD;HNUBxcGG|ZTDheEA{KHWPIHHmeIVzKDJ2IITvJFczKGi{czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nMYJie2WmIF\BR3Mh[W6jbInzbZM> NGm1[G09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iwNlcyPid-MkO4NFI4OTZ:L3G+
Assay
Methods Test Index PMID
Western blot p53 / MDM2 / p21 / Bax / Bak / Noxa / cleaved caspase / pro-caspase ; BMI-1 ; p53-Ser15 / p53-Ser37 / p53-Lys382 / MDM2 / CDC2 / PLK1 / HSC70 16014563 26887044 23666059
Immunofluorescence p-p21 / β-actin ; P53 ; Ac-p300 31083332 21394100 30240745
Growth inhibition assay Cell viability 26248031
In vivo Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage [1]. Nutlin-3 is a selective activator of the p53 pathway in vivo and highly efficacious against SJSA-1 osteosarcoma tumors[1]. Tumors with wild-type p53 and mdm2 gene amplification will respond best to therapy with Nutlin-3a.

Protocol (from reference)

Kinase Assay:[3]
  • Biacore studies:

    Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for 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 mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel

Cell Research:[2]
  • Cell lines: OSA, T778, RMS13, U2OS, SaOS-2
  • Concentrations: ~5 μM
  • Incubation Time: 120 h
  • Method: SRB
Animal Research:[1]
  • Animal Models: SJSA-1 xenograft
  • Dosages: 50, 100, 200 mg/kg twice daily
  • Administration: oral

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 581.49
Formula

C30H30Cl2N4O4

CAS No. 675576-98-4
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:
What is the difference between S1061 (Nutlin-3) and S8059 (Nutlin-3a)?

Answer:
S1061 is a racemic mixture of Nutlin3a and Nutlin3b. s8059 is the active enantiomer of Nutlin3.

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