Nutlin-3a

Catalog No.S8059

Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay.

Price Stock Quantity  
USD 197 In stock
USD 670 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Nutlin-3a Chemical Structure

Nutlin-3a Chemical Structure
Molecular Weight: 581.49

Validation & Quality Control

Quality Control & MSDS

Product Information

  • Compare Mdm2 Inhibitors
    Compare Mdm2 Products
  • Research Area

Product Description

Biological Activity

Description Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay.
Targets p53/MDM2 interaction [3]
(Cell-free assay)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MV-4-11NF[2b3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MoHJTWM2OD1yLk[xNlM4KM7:TR?=M3\x[nNCVkeHUh?=
H4MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3LoPWlEPTB;MD62OlI5KM7:TR?=NWPoZXo3W0GQR1XS
PA-1MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MV\JR|UxRTBwOEewPVYh|ryPMYLTRW5ITVJ?
NKM-1MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MWPJR|UxRTFwMES5N|Eh|ryPNFG5ZZZUSU6JRWK=
NEC8Mn7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlnHTWM2OD1zLkKxOVczKM7:TR?=M3i3fHNCVkeHUh?=
EoL-1-cellMlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWjwWJNHUUN3ME2xMlI3PzBzIN88US=>NF3vbHJUSU6JRWK=
K5MknJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2DPWGlEPTB;MT60NlA4OiEQvF2=Mn\NV2FPT0WU
QIMR-WILMUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NY\jcWRKUUN3ME2xMlYxQDV2IN88US=>MnnuV2FPT0WU
MOLT-16MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXTJR|UxRTFwN{i2NFQh|ryPNXzGPIFXW0GQR1XS
CHP-212NWKxeWh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NF3Fe3VKSzVyPUGuPFE{PjlizszNNVPUcHNZW0GQR1XS
CTB-1M1H4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUfJR|UxRTJwMEKyOFYh|ryPNXHVT3FNW0GQR1XS
MOLT-4MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1rZVmlEPTB;Mj6zNlg2OyEQvF2=MmfVV2FPT0WU
A101DMV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnPvTWM2OD1{LkO1NFEh|ryPMUjTRW5ITVJ?
DOHH-2M{Dyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEfyVpNKSzVyPUKuOFIzPzlizszNNXu0TYxKW0GQR1XS
ES4MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2G0NWlEPTB;Mj60N|E2PSEQvF2=MXfTRW5ITVJ?
SW780M1flSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXPJR|UxRTJwNUC4PFMh|ryPM2TjOHNCVkeHUh?=
VA-ES-BJMmjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYjmcm52UUN3ME2yMlU1OTFizszNMVvTRW5ITVJ?
RPMI-8866MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MkDiTWM2OD1{LkW2NlE1KM7:TR?=NGrYeHlUSU6JRWK=
ML-2NFvyZXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXzYNpVoUUN3ME2yMlU3PTd4IN88US=>Mk\lV2FPT0WU
MSTO-211HM4n0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVzJR|UxRTJwNUe0OVEh|ryPMnHQV2FPT0WU
JVM-3MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NXrRNW86UUN3ME2yMlU6OzJ2IN88US=>M3frPHNCVkeHUh?=
A3-KAWNILIdHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MYTJR|UxRTJwNkG4NVgh|ryPNYfCPVNsW0GQR1XS
DK-MGNH7v[4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1vBd2lEPTB;Mj62NlQ4OSEQvF2=NIriVY5USU6JRWK=
LNCaP-Clone-FGCM1m2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkjoTWM2OD1{Lk[0N|E5KM7:TR?=NIK0XWZUSU6JRWK=
HT-144MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NGH4WJNKSzVyPUKuOlQ2PzdizszNMonJV2FPT0WU
NB69Ml7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmHjTWM2OD1{Lk[1N|M1KM7:TR?=MUDTRW5ITVJ?
A172NInCOIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYfoUFRCUUN3ME2yMlY4PTh6IN88US=>MmCyV2FPT0WU
RS4-11NH;xdYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGLhNWhKSzVyPUKuO|I1ODdizszNNUPJdG4yW0GQR1XS
DU-4475M{PuXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NF\iZVVKSzVyPUKuO|k2ODJizszNM1HpTHNCVkeHUh?=
SJSA-1MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmDGTWM2OD1{LkiyOVU3KM7:TR?=NUXZTGlWW0GQR1XS
BV-173NH\VV2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NHK5VGhKSzVyPUKuPFQ1OzlizszNNGrFXFBUSU6JRWK=
U-2-OSMn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2HVPGlEPTB;Mj65NVA4KM7:TR?=M1LkUXNCVkeHUh?=
CHP-134NILndJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NUXp[2xQUUN3ME2yMlk{QDh{IN88US=>NHvvUGtUSU6JRWK=
D-502MGMUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXTZRZh{UUN3ME2yMlk4OTV2IN88US=>NVLlbXRoW0GQR1XS
KS-1NGno[JZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXTGbY95UUN3ME2zMlAyPjJ|IN88US=>MYjTRW5ITVJ?
A204MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3e0WGlEPTB;Mz6wOVU5QCEQvF2=NILkZo1USU6JRWK=
KGNNYfYTWdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NWH3Xm97UUN3ME2zMlA5PDl4IN88US=>NW\KXZhjW0GQR1XS
NCI-H292M2PVdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYLlOmxlUUN3ME2zMlEzODJ6IN88US=>MnrGV2FPT0WU
CAKI-1MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MVXJR|UxRTNwMUK2PVQh|ryPNFnH[4VUSU6JRWK=
C2BBe1MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MX\JR|UxRTNwMUewNlYh|ryPM1;NNnNCVkeHUh?=
NB10NXHhd5MyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NInxUGlKSzVyPUOuNlA6PjZizszNMoHzV2FPT0WU
MHH-NB-11M4frT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHzLVVNKSzVyPUOuNlY5OjdizszNMoXPV2FPT0WU
NCI-SNU-1M{DPZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnTSTWM2OD1|LkK3PFQ{KM7:TR?=NIfkV5pUSU6JRWK=
HCT-116M2nCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEPkTXhKSzVyPUOuN|A{OzVizszNNEfIUJdUSU6JRWK=
G-401NV\FWG9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MYPJR|UxRTNwM{[zNlIh|ryPM4\tcHNCVkeHUh?=
MN-60M2H5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYnJR|UxRTNwNESwPVIh|ryPNXjTZoJTW0GQR1XS
SW982Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHXqe2hKSzVyPUOuOVA5PDhizszNMYfTRW5ITVJ?
RKONFO4S2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVrsOo9VUUN3ME2zMlU{QTN4IN88US=>MWPTRW5ITVJ?
D-283MEDMYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NEO2fpVKSzVyPUOuOVc6QDZizszNMkTkV2FPT0WU
LB996-RCCMljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkLTTWM2OD1|Lk[yOVU5KM7:TR?=MkSxV2FPT0WU
A549Ml:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWLxR3o{UUN3ME2zMlY{PTV{IN88US=>MnjsV2FPT0WU
LB2241-RCCMV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MYHJR|UxRTNwNkW3NFgh|ryPMnzFV2FPT0WU
SK-HEP-1M3fXZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NV[0NFBRUUN3ME2zMlc1Ojl5IN88US=>NGP6cXNUSU6JRWK=
G-402MkHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1HSTWlEPTB;Mz64NFg{OiEQvF2=MYjTRW5ITVJ?
GOTOMnnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4TM[WlEPTB;Mz64OFM{OyEQvF2=MXPTRW5ITVJ?
LOXIMVIM4XXVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3;TdGlEPTB;Mz64OVY4PSEQvF2=M2PWb3NCVkeHUh?=
NH-12MmfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MX7JR|UxRTRwMEG5OVkh|ryPM2HhbnNCVkeHUh?=
CTV-1MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3npSmlEPTB;ND6wO|k4OyEQvF2=NET5V2lUSU6JRWK=
CP50-MEL-BNV3h[G5kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXz3WXFsUUN3ME20MlI1Ozl{IN88US=>MlqxV2FPT0WU
RH-18MmeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlrUTWM2OD12LkK3O|A3KM7:TR?=NIT3W5pUSU6JRWK=
NB17NVzvfVF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MonCTWM2OD12LkOxO|Y5KM7:TR?=M3jPOXNCVkeHUh?=
A375NXOwW29UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1rsfmlEPTB;ND6zN|UzPCEQvF2=NU\YRoFqW0GQR1XS
IST-MES1MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGD0NFFKSzVyPUSuOFE1OTFizszNM33VXnNCVkeHUh?=
MZ2-MELNYfXRYNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mn30TWM2OD12LkWwNVU2KM7:TR?=Mm\DV2FPT0WU
CAL-54NXLuU|M2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NYm2T2hnUUN3ME20MlU{ODF7IN88US=>NEXQV4dUSU6JRWK=
NCI-H28M{fsPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXHzb3huUUN3ME20MlYzPzF5IN88US=>MUXTRW5ITVJ?
D-247MGM1PpN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHz4V2VKSzVyPUSuO|UxPzJizszNMnTnV2FPT0WU
NCI-H460M3HC[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnTGTWM2OD12LkmxNVI4KM7:TR?=MmDGV2FPT0WU
MCF7NFTMWoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXTJR|UxRTVwNESyOFQh|ryPNX\IcFFUW0GQR1XS
697M1ywUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NVPObnVHUUN3ME21MlQ1PTVizszNM{HFSnNCVkeHUh?=
ONS-76MmDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHTNW2VKSzVyPUWuOVcxODlizszNM1rSeHNCVkeHUh?=
C32MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXjJR|UxRTVwNkCwNlkh|ryPNGPNUFRUSU6JRWK=
OS-RC-2NVS2SZB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1PGUmlEPTB;NT63N|g5PyEQvF2=NFXGSXlUSU6JRWK=
MEL-HONVjBfJRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVLDXmR4UUN3ME21Mlg2PjZ5IN88US=>NXzzWoo1W0GQR1XS
LoVoNHm4TYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFvxdVBKSzVyPU[uNFE3OjRizszNMk\oV2FPT0WU
AGSM1nEVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2LvWWlEPTB;Nj6xOFgzQCEQvF2=NV6wZYJLW0GQR1XS
GI-ME-NNGPSdlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXGyT|ZrUUN3ME22MlIzPDJzIN88US=>MoXjV2FPT0WU
H-EMC-SSMnvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2jufmlEPTB;Nj6zPFYh|ryPM1;6RnNCVkeHUh?=
RVH-421NWPoXoxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MYnJR|UxRTZwNEK0Nlgh|ryPM2LncXNCVkeHUh?=
SW954M1Xi[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXyzZVNVUUN3ME22MlU2PTd{IN88US=>NUPXOZlZW0GQR1XS
NB5MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4D4PGlEPTB;Nj61OlE5OyEQvF2=NEnlNplUSU6JRWK=
NCI-H2122MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGPmSZdKSzVyPU[uOVg4QTNizszNMorDV2FPT0WU
AM-38NWr4WVlyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M133T2lEPTB;Nj63OVY{QSEQvF2=NFezc3BUSU6JRWK=
KNS-81-FDNVy4eXV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2XCeWlEPTB;Nj63OlQ6PCEQvF2=M1e1fXNCVkeHUh?=
LS-513NF\yRppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4H4eGlEPTB;Nj63PVAzPiEQvF2=NVTKNoV3W0GQR1XS
A427Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmqxTWM2OD14Lki3PFI6KM7:TR?=NIi2OJJUSU6JRWK=
WM-115NIqyS5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkPITWM2OD14LkmzNlMh|ryPNID6OIZUSU6JRWK=
COLO-829M3TUcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFjnWoVKSzVyPUeuNlQyQDhizszNNWnJbYpYW0GQR1XS
NCI-H1650MonWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MmfGTWM2OD15LkO5NlI5KM7:TR?=M3;wfXNCVkeHUh?=
NCI-H358M{DpO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NECzeoRKSzVyPUeuOFQ5PzlizszNNX2zXIxrW0GQR1XS
HT-1080M4jIOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M12xWGlEPTB;Nz60PFI2PCEQvF2=MmixV2FPT0WU
HCC2218M3XaWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXXJR|UxRTdwNkK5O{DPxE1?MVvTRW5ITVJ?
NCI-H661MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1O1dGlEPTB;Nz64O|A3QSEQvF2=MkHWV2FPT0WU
KM-H2MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUGxUFZkUUN3ME23Mlg5Pjl2IN88US=>NHXTblJUSU6JRWK=
RPMI-2650NH:yfpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NF\1W4VKSzVyPUeuPVQ1OTRizszNNInNVGlUSU6JRWK=
NCI-H226MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MVLJR|UxRThwMkGxNlIh|ryPNFWxW2NUSU6JRWK=
MKN45M1Pnd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYLJR|UxRThwMk[2NFIh|ryPNETUXmxUSU6JRWK=
D-392MGNFX3dlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NIL5dVNKSzVyPUiuOVI4OjJizszNM2jh[XNCVkeHUh?=
RCC10RGBMoTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkniTWM2OD16Lki2Olk2KM7:TR?=MYfTRW5ITVJ?
CAL-51NEjOTldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mm[1TWM2OD17LkGwNlUyKM7:TR?=MlfwV2FPT0WU
COLO-678M4XqOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnHCTWM2OD17LkOyPFEyKM7:TR?=MnLQV2FPT0WU
SK-MEL-24MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGLhd4xKSzVyPUmuOVU5PTZizszNMkL4V2FPT0WU
SK-MEL-30NWjLXolmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHHiW4pKSzVyPUmuPVQ1PzZizszNNH3SR|dUSU6JRWK=
MMAC-SFNF;rbYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MoLuTWM2OD1zMD6zPVYyKM7:TR?=NVXEW2h7W0GQR1XS
NTERA-S-cl-D1M3LJSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlrCTWM2OD1zMD62OVA5KM7:TR?=MYHTRW5ITVJ?
NB12MkfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MUHJR|UxRTFzLkWwN{DPxE1?MWHTRW5ITVJ?
UACC-257NXO1d25lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{\HOGlEPTB;MUGuPFY6PSEQvF2=NUTLNHFJW0GQR1XS
LAN-6MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MkTHTWM2OD1zMT65PVI5KM7:TR?=MWTTRW5ITVJ?
SW1573MmewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MnHvTWM2OD1zMj6zNFg3KM7:TR?=NETIUWFUSU6JRWK=
NMC-G1Ml;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NFXYdHFKSzVyPUGyMlQyPzVizszNNHvW[YRUSU6JRWK=
SHP-77MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MkfQTWM2OD1zMj61OVc1KM7:TR?=MX3TRW5ITVJ?
IGROV-1NEH3dHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NEnQSIZKSzVyPUGyMlY2PzNizszNNULSNmxUW0GQR1XS
22RV1MnS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NHLsdm1KSzVyPUGyMlgxPTlizszNMVvTRW5ITVJ?
SK-MEL-3M{[3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4jUfmlEPTB;MUOuN|k4OyEQvF2=NIjGcppUSU6JRWK=
NCI-H1563MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mn[2TWM2OD1zMz60NlAzKM7:TR?=MWHTRW5ITVJ?
IGR-1MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MoL4TWM2OD1zND6wN|Q4KM7:TR?=MYjTRW5ITVJ?
EW-3M{jXemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkHoTWM2OD1zND6xOlM6KM7:TR?=MmTBV2FPT0WU
JEG-3M3znU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUfJR|UxRTF2LkS5OVMh|ryPMn\yV2FPT0WU
ES3M4W1PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGX0UWdKSzVyPUG0MlY2PjJizszNNHLRNWdUSU6JRWK=
MDA-MB-175-VIINYjT[ZM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MW\JR|UxRTF2LkexNVEh|ryPNEmwO|NUSU6JRWK=
P30-OHKMV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NEG2d4JKSzVyPUG1MlA1QTZizszNM2\wZnNCVkeHUh?=
GP5dMUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mn3ETWM2OD1zNT6xOFY3KM7:TR?=MoTmV2FPT0WU
HMV-IINFSxTWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVvpc|k1UUN3ME2xOU4{OzN|IN88US=>NUiyfZZVW0GQR1XS
COLO-679MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWDiUXV3UUN3ME2xOU42ODFizszNM4iwd3NCVkeHUh?=
JARM1TxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlnmTWM2OD1zNT63NlA2KM7:TR?=MlvCV2FPT0WU
NCI-H1666NHvmNGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXn1PWJHUUN3ME2xOU46Ozl7IN88US=>NH7ifnhUSU6JRWK=
SW48NXHhS2d1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2PVfmlEPTB;MUWuPVUyPiEQvF2=MmTCV2FPT0WU
NCI-H720MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Ml\jTWM2OD1zNT65PVg6KM7:TR?=NVfHTI9CW0GQR1XS
HT-1197MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1TXd2lEPTB;MU[uNFM2OiEQvF2=MlvQV2FPT0WU
HL-60MlTGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYLzSFluUUN3ME2xOk4xOzh2IN88US=>M12zT3NCVkeHUh?=
BENNUe5XYFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVPJR|UxRTF4LkW2N|gh|ryPM3y4dnNCVkeHUh?=
HAL-01M2T1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFnyPIpKSzVyPUG2Mlg6ODlizszNMoHTV2FPT0WU
SW900Mle2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2PoOGlEPTB;MU[uPVE{OiEQvF2=NX3ZNYl[W0GQR1XS
SBC-1M3rsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUnJR|UxRTF5LkW0Nlkh|ryPMlXDV2FPT0WU
SH-4Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MVXJR|UxRTF5LkW4OFEh|ryPNYf2ZnBzW0GQR1XS
UACC-62NEfCN2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Ml:5TWM2OD1zNz63OlM4KM7:TR?=MkfOV2FPT0WU
BHT-101M{Hzdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVzJR|UxRTF7Lki3NFUh|ryPMWjTRW5ITVJ?
DBMlLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Ml64TWM2OD1{MT61OlQ6KM7:TR?=NICxZ5FUSU6JRWK=
SK-MEL-1MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NIr1V|JKSzVyPUKxMlU5PzJizszNM1v6T3NCVkeHUh?=
NCI-H747Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlHmTWM2OD1{Mj63N|c6KM7:TR?=NFfyRXpUSU6JRWK=
SK-LU-1M3rp[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M{XQSGlEPTB;MkOuN|UzPCEQvF2=NEDa[WVUSU6JRWK=
KG-1NYPwfZl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHPifVNKSzVyPUKzMlQ6PDZizszNNEm0THRUSU6JRWK=
LXF-289NFG0SlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3H2TmlEPTB;MkOuO|E1KM7:TR?=MUnTRW5ITVJ?
HCC1954NHL4dmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1nrSWlEPTB;MkSuPFg1PCEQvF2=MYrTRW5ITVJ?
Ramos-2G6-4C10MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MnfMTWM2OD1{Nj60PVgyKM7:TR?=NUnXWmZrW0GQR1XS
DBTRG-05MGNY\hcZN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M{LyWmlEPTB;Mk[uOlQ5QCEQvF2=M1vMZXNCVkeHUh?=
NCI-H2052NXrVUGh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXPvb4pwUUN3ME2yO{42Pjh2IN88US=>NV:wXnJLW0GQR1XS
RMG-IMlHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkO5TWM2OD1{OT60NVM6KM7:TR?=Ml3hV2FPT0WU
H9MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NYn5T4ROUUN3ME2zNU4{ODB6IN88US=>NGDTdVlUSU6JRWK=
GR-STM2HiZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3;ocmlEPTB;M{KuOFQ2OyEQvF2=MVLTRW5ITVJ?
Mo-TNYrBOlFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MV3JR|UxRTN{LkWwOFYh|ryPNHvibFlUSU6JRWK=
SW1088MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MYLJR|UxRTN{Lkm4NFEh|ryPM3XnWXNCVkeHUh?=
LB2518-MELMWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUT4cWxqUUN3ME2zN{4xPzl5IN88US=>MWfTRW5ITVJ?
NCI-H82M{jOWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXnwc5F2UUN3ME2zN{4yPjZzIN88US=>NWLOelk3W0GQR1XS
LAMA-84MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2f0PWlEPTB;M{SuOlA4OyEQvF2=MlT0V2FPT0WU
KYSE-450M3Lz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXjJR|UxRTN2Lk[3O|Yh|ryPNHK0eWNUSU6JRWK=
LU-99ANH\2WnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1mweWlEPTB;M{WuNFAxPyEQvF2=M{LNbXNCVkeHUh?=
BE-13MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NHTxXXFKSzVyPUO1MlY2PDVizszNNYO5WZF6W0GQR1XS
GAKMmHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkPPTWM2OD1|NT62PVUh|ryPNEDiR5NUSU6JRWK=
NCI-H1573Mlv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUWyUmhnUUN3ME2zOU45QDF6IN88US=>NEXTcHhUSU6JRWK=
AsPC-1NHizSm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXG0NotjUUN3ME2zOk4yPTJ5IN88US=>M37qdnNCVkeHUh?=
HDLM-2NXHy[nNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NEnseVBKSzVyPUO2MlMyPiEQvF2=M1\RSHNCVkeHUh?=
NCI-H441NFrXfXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1XOUWlEPTB;M{euNFY6OSEQvF2=NI\ye3VUSU6JRWK=
CAL-27MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{n0PGlEPTB;M{euO|I{OSEQvF2=NGH1bYlUSU6JRWK=
OVCAR-3MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXLCfphZUUN3ME2zPU4{OThzIN88US=>NHqxO2NUSU6JRWK=
RPMI-8226MnrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NVmxUo9qUUN3ME2zPU42QThizszNMoP4V2FPT0WU
EFO-21NY\nRZdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MX\JR|UxRTRyLkW4NVQh|ryPM1\5RXNCVkeHUh?=
SNU-C2BMX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NI\KdI5KSzVyPUSxMlUxQDRizszNM3vnNnNCVkeHUh?=
VM-CUB-1MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{e1NWlEPTB;NEOuPFA{PyEQvF2=MkPHV2FPT0WU
NCI-H2087NYnrOnRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1z0VWlEPTB;NEWuNFI{OyEQvF2=NFzFW2hUSU6JRWK=
EW-16NUewTVExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NYrGPG9TUUN3ME20Ok4{OTN5IN88US=>MnfSV2FPT0WU
SK-N-ASNH23XpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MV7JR|UxRTR4LkexOlch|ryPNFnDT3VUSU6JRWK=
COR-L105NF62XpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NEnXR3RKSzVyPUS2Mlg5PTdizszNMUfTRW5ITVJ?
DELNHXmbGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkDNTWM2OD12OD6wOFI6KM7:TR?=NV[5Sm1nW0GQR1XS
JVM-2MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MX\JR|UxRTR6LkC1OVgh|ryPM3joZnNCVkeHUh?=
KARPAS-45M4TsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2HEbGlEPTB;NEmuOFU{QCEQvF2=MlXhV2FPT0WU

... Click to View More Cell Line Experimental Data

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.
Features Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.

Protocol(Only for 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 Assay: [2]

Cell lines OSA, T778, RMS13, U2OS, SaOS-2
Concentrations ~5 μM
Incubation Time 120 h
Method SRB

Animal Study: [1]

Animal Models SJSA-1 xenograft
Formulation 1% Klucel, 0.1% Tween 80
Dosages 50, 100, 200 mg/kg twice daily
Administration oral

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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

References

[1] Tovar C, et al. Proc Natl Acad Sci U S A, 2006, 103(6), 1888-1893.

[2] Ohnstad HO, et al. BMC Cancer, 2011, 11(211), 1-11.

view more

Chemical Information

Molecular Weight (MW) 581.49
Formula

C30H30Cl2N4O4

CAS No. 675576-98-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms (-)-Nutlin-3
Solubility (25°C) * In vitro DMSO 100 mg/mL (171.97 mM)
Ethanol 100 mg/mL (171.97 mM)
Water <1 mg/mL (<1 mM)
In vivo 2% DMSO+1% hydroxyethyl cellulose+0.2% Tween 80 15 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.
Chemical Name 2-Piperazinone, 4-[[(4S,5R)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-

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.

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

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

* Indicates a Required Field

Related Mdm2 Products

  • Idasanutlin (RG-7388)

    Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM.

  • 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.

  • Nutlin-3

    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.

  • NSC 207895

    NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

  • 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 is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.

    Features:A key compound for apoptosis studies.

  • ABT-263 (Navitoclax)

    ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.

  • Venetoclax (ABT-199, GDC-0199)

    Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.

    Features:Re-engineered version of ABT-263 (Navitoclax).

Recently Viewed Items

Tags: buy Nutlin-3a | Nutlin-3a supplier | purchase Nutlin-3a | Nutlin-3a cost | Nutlin-3a manufacturer | order Nutlin-3a | Nutlin-3a distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us