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 55 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 NYf2dWNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnuTWM2OD1yLk[xNlM4KM7:TR?= NYTXTXM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
H4 Mof2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwNk[yPEDPxE1? MkK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
PA-1 MlPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwOEewPVYh|ryP NHi3XJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
NKM-1 MlrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLjVINKSzVyPUGuNFQ6OzFizszN MoLBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
NEC8 M1nWWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXNZ|dKSzVyPUGuNlE2PzJizszN MkCzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
EoL-1-cell NVK2PIhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTFwMk[3NFEh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
K5 M4C2Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTFwNEKwO|Ih|ryP M1W4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
QIMR-WIL MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fVUGlEPTB;MT62NFg2PCEQvF2= NF7OOpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
MOLT-16 NHHWcHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTFwN{i2NFQh|ryP NFy4Z5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
CHP-212 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnYWI5NUUN3ME2xMlgyOzZ7IN88US=> MmewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
CTB-1 M364emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHybZZbUUN3ME2yMlAzOjR4IN88US=> MkTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
MOLT-4 Mn;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XKS2lEPTB;Mj6zNlg2OyEQvF2= NGTET5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
A101D NY[yTlNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTJwM{WwNUDPxE1? M16zVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
DOHH-2 NYrobYx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnmzTWM2OD1{LkSyNlc6KM7:TR?= NHPId4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
ES4 NFzCeXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGG0WHhKSzVyPUKuOFMyPTVizszN NEmw[Wk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
SW780 Mn7hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXDbHlKSzVyPUKuOVA5QDNizszN NXnTVXZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
VA-ES-BJ NUHvb2NGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjwNYJKSzVyPUKuOVQyOSEQvF2= NHPMVWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
RPMI-8866 NETTV3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETmWIxKSzVyPUKuOVYzOTRizszN NF;XcG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
ML-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJwNU[1O|Yh|ryP M17XVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
MSTO-211H M{PTWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJwNUe0OVEh|ryP M3\MNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
JVM-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvGTWM2OD1{LkW5N|I1KM7:TR?= NWTacYlYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
A3-KAW MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v1SGlEPTB;Mj62NVgyQCEQvF2= MoXOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
DK-MG M2\MT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTJwNkK0O|Eh|ryP M2HRUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
LNCaP-Clone-FGC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTLTGRqUUN3ME2yMlY1OzF6IN88US=> MmWyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
HT-144 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorUTWM2OD1{Lk[0OVc4KM7:TR?= NXP3VItlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
NB69 NH3oRVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrEXnRxUUN3ME2yMlY2OzN2IN88US=> NVWwWGRoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
A172 MmW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP3TWM2OD1{Lk[3OVg5KM7:TR?= NWLONGUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
RS4-11 NWXLU21YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJwN{K0NFch|ryP M1XFfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
DU-4475 NFTEToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HVPWlEPTB;Mj63PVUxOiEQvF2= NFH3Z2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
SJSA-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTiNFluUUN3ME2yMlgzPTV4IN88US=> M{\zdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
BV-173 NYLoOWxmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLIS5pwUUN3ME2yMlg1PDN7IN88US=> Ml\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
U-2-OS MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTJwOUGwO{DPxE1? NIH5RpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
CHP-134 MkfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;YNVJKSzVyPUKuPVM5QDJizszN MlPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
D-502MG NH;tWVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPkTWM2OD1{Lkm3NVU1KM7:TR?= NVraWHU2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
KS-1 NF3KSldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zzTWlEPTB;Mz6wNVYzOyEQvF2= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
A204 M3uw[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFO5e|dKSzVyPUOuNFU2QDhizszN NF35d|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
KGN MojCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELEdoJKSzVyPUOuNFg1QTZizszN NVK4VlZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
NCI-H292 Mo\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfX[IRoUUN3ME2zMlEzODJ6IN88US=> NWHmWW53RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
CAKI-1 NUGwT5BpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTvV41{UUN3ME2zMlEzPjl2IN88US=> M{DSTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
C2BBe1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTNwMUewNlYh|ryP M1zxclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
NB10 MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfuOJZKSzVyPUOuNlA6PjZizszN M1rscFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
MHH-NB-11 NU\6XHdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjPVVJKSzVyPUOuNlY5OjdizszN NX[4fGhRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
NCI-SNU-1 NVruc41KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTNwMke4OFMh|ryP M1facVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
HCT-116 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDYTWM2OD1|LkOwN|M2KM7:TR?= Mk\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
G-401 M4\w[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki3TWM2OD1|LkO2N|IzKM7:TR?= MmL1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
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MCF7 Mn7zRZBweHSxc3nzJIF{e2G7 M{\nUVUxKG6P M1TQW|I1KHSxIEeyJIhzew>? NFvWXmFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh[WOldX31cIF1cW:wIH;mJINie3Cjc3WtN{BkdGWjdnHn[UBxem:mdXP0JIF1KDVyIH7NJIFnfGW{IEK0JJRwKDd{IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{ NUDOV2puRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4NFI4OTZpPkKzPFAzPzF4PD;hQi=>
MCF7 NVXoR2hNS2WubDDjfYNt\SCjc4PhfS=> MV[zJJVO NXu4WXE3OjRidH:gO|IhcHK| NUX2fY5{S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS|EheGijc3WgZZQhOyC3TTDh[pRmeiB{NDD0c{A4OiCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDGRWNUKGGwYXz5d4l{ MkOxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MEK3NVYoRjJ|OECyO|E3RC:jPh?=
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
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: SJSA-1 xenograft
  • Dosages: 50, 100, 200 mg/kg twice daily
  • Administration: oral
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(171.97 mM)
Water Insoluble
Ethanol '100 mg/mL

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

* 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 581.49
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
If you have any other enquiries, please leave a message.

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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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