Nutlin-3a

For research use only. Not for use in humans.

目录号:S8059 别名: (-)-Nutlin-3

Nutlin-3a Chemical Structure

CAS No. 675576-98-4

Nutlin-3a ((-)-Nutlin-3)是Nutlin-3的活性对映体,抑制p53/MDM2相互作用,无细胞试验中IC50为90 nM。Nutlin-3a 可诱导p53依赖的自噬和细胞凋亡。

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客户使用Selleck生产的Nutlin-3a发表文献45篇:

产品安全说明书

Mdm2抑制剂选择性比较

生物活性

产品描述 Nutlin-3a ((-)-Nutlin-3)是Nutlin-3的活性对映体,抑制p53/MDM2相互作用,无细胞试验中IC50为90 nM。Nutlin-3a 可诱导p53依赖的自噬和细胞凋亡。
特性 高度选择性的MDM2抑制剂与对MDMX低得多的效果。对含野生型p53的肿瘤最有效。
靶点
p53/MDM2 interaction [3]
(Cell-free assay)
90 nM
体外研究

Nutlin-3α从MDM2蛋白的结合口袋置换p53,由此将p53从抑制和蛋白酶体降解状态释放出来,从而导致诱导其下游靶点,细胞周期停滞和细胞凋亡。七天孵育10 μM nutlin-3a导致了NIH3T3细胞的生长抑制达90%以上。[1] Nutlin-3α稳定并激活p53基因,以剂量依赖性的方式诱导p21的表达。[1] Nutlin-3A有效地减少S期细胞至0.2-2%,并增加了G1-和G2/M期细胞。[1] 在40小时后,Nutlin-3a诱导约60% SJSA-1和MHM细胞的凋亡,而到60小时后,凋亡细胞分别达到85%和65%。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 M2P0VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L0dmlEPTB;MD62NVI{PyEQvF2= NVnXV405W0GQR1XS
H4 MkLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjyUmxIUUN3ME2wMlY3OjhizszN NUjWOoN6W0GQR1XS
PA-1 NGL4Rm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XlNmlEPTB;MD64O|A6PiEQvF2= MX;TRW5ITVJ?
NKM-1 M1Pxemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzVR|F4UUN3ME2xMlA1QTNzIN88US=> M2\qN3NCVkeHUh?=
NEC8 NEXxXZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFwMkG1O|Ih|ryP NETpc|RUSU6JRWK=
EoL-1-cell M4fm[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j3ZWlEPTB;MT6yOlcxOSEQvF2= MoGzV2FPT0WU
K5 M{HoZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFwNEKwO|Ih|ryP NWHlb2RRW0GQR1XS
QIMR-WIL M4fkNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILjSW1KSzVyPUGuOlA5PTRizszN MUTTRW5ITVJ?
MOLT-16 NHfxNY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmS3TWM2OD1zLke4OlA1KM7:TR?= M{e0eXNCVkeHUh?=
CHP-212 NYXZUnA4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfKZlRQUUN3ME2xMlgyOzZ7IN88US=> MX7TRW5ITVJ?
CTB-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULNPXREUUN3ME2yMlAzOjR4IN88US=> MnL3V2FPT0WU
MOLT-4 NGXqSFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjsWoVvUUN3ME2yMlMzQDV|IN88US=> MVzTRW5ITVJ?
A101D NXX2dZVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJwM{WwNUDPxE1? M4LlSHNCVkeHUh?=
DOHH-2 NXXiW4ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTJwNEKyO|kh|ryP MV7TRW5ITVJ?
ES4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLxTWM2OD1{LkSzNVU2KM7:TR?= M3XDe3NCVkeHUh?=
SW780 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV31[4lvUUN3ME2yMlUxQDh|IN88US=> MWfTRW5ITVJ?
VA-ES-BJ M1jLZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DITWlEPTB;Mj61OFEyKM7:TR?= M3zR[nNCVkeHUh?=
RPMI-8866 MmDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLZXJZKSzVyPUKuOVYzOTRizszN M1jqcnNCVkeHUh?=
ML-2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO5cWdKSzVyPUKuOVY2PzZizszN MkW3V2FPT0WU
MSTO-211H MonQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTJwNUe0OVEh|ryP M{DZcnNCVkeHUh?=
JVM-3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnjUZp7UUN3ME2yMlU6OzJ2IN88US=> MmnyV2FPT0WU
A3-KAW MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\Ke2lEPTB;Mj62NVgyQCEQvF2= NEDzclVUSU6JRWK=
DK-MG M{XYUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJwNkK0O|Eh|ryP NEHYNI5USU6JRWK=
LNCaP-Clone-FGC MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTJwNkSzNVgh|ryP NYOzSpBSW0GQR1XS
HT-144 NXztdGp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17hfmlEPTB;Mj62OFU4PyEQvF2= MXfTRW5ITVJ?
NB69 NIXwSnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13idGlEPTB;Mj62OVM{PCEQvF2= NIKwfXlUSU6JRWK=
A172 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjUb3dKSzVyPUKuOlc2QDhizszN MknLV2FPT0WU
RS4-11 M3L4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\lTWM2OD1{LkeyOFA4KM7:TR?= NF6xTlNUSU6JRWK=
DU-4475 MoW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEeySnlKSzVyPUKuO|k2ODJizszN MkTDV2FPT0WU
SJSA-1 M3;aWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TNbGlEPTB;Mj64NlU2PiEQvF2= MlHRV2FPT0WU
BV-173 NV\0TItUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3YTWM2OD1{Lki0OFM6KM7:TR?= NVPOdnQ1W0GQR1XS
U-2-OS NEHncIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlj6TWM2OD1{LkmxNFch|ryP M1\UbHNCVkeHUh?=
CHP-134 MoHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG4XWFKSzVyPUKuPVM5QDJizszN NWXxWJoyW0GQR1XS
D-502MG MmT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJwOUexOVQh|ryP NECwOFNUSU6JRWK=
KS-1 NH7DW2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTNwMEG2NlMh|ryP MYLTRW5ITVJ?
A204 NF3nblZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTNwMEW1PFgh|ryP MXfTRW5ITVJ?
KGN MkHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTNwMEi0PVYh|ryP NGfwWm9USU6JRWK=
NCI-H292 NVnxVVk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7SVJVKSzVyPUOuNVIxOjhizszN MnPNV2FPT0WU
CAKI-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL6dIZZUUN3ME2zMlEzPjl2IN88US=> MWfTRW5ITVJ?
C2BBe1 M3HTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HUbWlEPTB;Mz6xO|AzPiEQvF2= M1rrSHNCVkeHUh?=
NB10 M1rBfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTNwMkC5OlYh|ryP NWTTSlBwW0GQR1XS
MHH-NB-11 M1;YW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnvWYFKSzVyPUOuNlY5OjdizszN MYHTRW5ITVJ?
NCI-SNU-1 NHzJOHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG4NmdoUUN3ME2zMlI4QDR|IN88US=> MmTlV2FPT0WU
HCT-116 M33remdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4CydWlEPTB;Mz6zNFM{PSEQvF2= NULpZpVZW0GQR1XS
G-401 M4fpSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HRc2lEPTB;Mz6zOlMzOiEQvF2= MWPTRW5ITVJ?
MN-60 NFjEd4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTNwNESwPVIh|ryP NF30UmRUSU6JRWK=
SW982 NGHHPJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGeyPZZKSzVyPUOuOVA5PDhizszN Mo[yV2FPT0WU
RKO M1G3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTNwNUO5N|Yh|ryP NHXMPYxUSU6JRWK=
D-283MED NE\pT3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDwTWM2OD1|LkW3PVg3KM7:TR?= MkL4V2FPT0WU
LB996-RCC NEnGTmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TUdWlEPTB;Mz62NlU2QCEQvF2= NHvHZ|RUSU6JRWK=
A549 NGOxUmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\vTWM2OD1|Lk[zOVUzKM7:TR?= Mor4V2FPT0WU
LB2241-RCC NFnxUm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITa[IdKSzVyPUOuOlU4ODhizszN Mom4V2FPT0WU
SK-HEP-1 M1nPVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLCOIRKSzVyPUOuO|QzQTdizszN NXi2VIlTW0GQR1XS
G-402 NX;QN2NwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fCcWlEPTB;Mz64NFg{OiEQvF2= MoPFV2FPT0WU
GOTO NIG5TmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVS3WoxvUUN3ME2zMlg1OzN|IN88US=> NYPiSHBNW0GQR1XS
LOXIMVI NXHWbHJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTnTWM2OD1|Lki1Olc2KM7:TR?= MoT6V2FPT0WU
NH-12 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MluwTWM2OD12LkCxPVU6KM7:TR?= NVPFb3N6W0GQR1XS
CTV-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\TTWM2OD12LkC3PVc{KM7:TR?= MlriV2FPT0WU
CP50-MEL-B NGLmbpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPPN2ZOUUN3ME20MlI1Ozl{IN88US=> M3jTO3NCVkeHUh?=
RH-18 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrHN2hZUUN3ME20MlI4PzB4IN88US=> M4jFd3NCVkeHUh?=
NB17 NH30dllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH6[3l1UUN3ME20MlMyPzZ6IN88US=> NEPNZ41USU6JRWK=
A375 M37yT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4D1NGlEPTB;ND6zN|UzPCEQvF2= NUXyPGc{W0GQR1XS
IST-MES1 NGLWTXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTRwNEG0NVEh|ryP MYXTRW5ITVJ?
MZ2-MEL MnrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnrOo9KSzVyPUSuOVAyPTVizszN MXHTRW5ITVJ?
CAL-54 MmHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ThfWlEPTB;ND61N|AyQSEQvF2= M2LPenNCVkeHUh?=
NCI-H28 Ml;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTRwNkK3NVch|ryP MlvNV2FPT0WU
D-247MG M{jmR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\QcFlXUUN3ME20Mlc2ODd{IN88US=> M2[wO3NCVkeHUh?=
NCI-H460 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDVVZpZUUN3ME20MlkyOTJ5IN88US=> MWfTRW5ITVJ?
MCF7 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLGTWM2OD13LkS0NlQ1KM7:TR?= MlP3V2FPT0WU
697 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LvcmlEPTB;NT60OFU2KM7:TR?= MlvCV2FPT0WU
ONS-76 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoO1TWM2OD13LkW3NFA6KM7:TR?= NXvTT3VrW0GQR1XS
C32 NHq4UZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTVwNkCwNlkh|ryP MYHTRW5ITVJ?
OS-RC-2 NWO5Xm5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPEVYVOUUN3ME21Mlc{QDh5IN88US=> Ml25V2FPT0WU
MEL-HO MmHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTVwOEW2Olch|ryP MmLjV2FPT0WU
LoVo MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3PTWM2OD14LkCxOlI1KM7:TR?= NEfqboZUSU6JRWK=
AGS MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;wdYRKSzVyPU[uNVQ5OjhizszN NH[5V5hUSU6JRWK=
GI-ME-N MoSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPKTWM2OD14LkKyOFIyKM7:TR?= MVvTRW5ITVJ?
H-EMC-SS NXTST|E6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTZwM{i2JO69VQ>? M4fhdnNCVkeHUh?=
RVH-421 M1rmWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTZwNEK0Nlgh|ryP MkO0V2FPT0WU
SW954 M2\YPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P4c2lEPTB;Nj61OVU4OiEQvF2= MkjwV2FPT0WU
NB5 NF3qTZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGW5OnZKSzVyPU[uOVYyQDNizszN MWPTRW5ITVJ?
NCI-H2122 M4T6cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFH2R3ZKSzVyPU[uOVg4QTNizszN M2i2THNCVkeHUh?=
AM-38 MkS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFntN2dKSzVyPU[uO|U3OzlizszN NH\lRmhUSU6JRWK=
KNS-81-FD MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrUS3c6UUN3ME22Mlc3PDl2IN88US=> MmPWV2FPT0WU
LS-513 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\UTWM2OD14Lke5NFI3KM7:TR?= MVfTRW5ITVJ?
A427 NFjoOYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTZwOEe4Nlkh|ryP MYjTRW5ITVJ?
WM-115 MmTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnTNmtKSzVyPU[uPVMzOyEQvF2= NHX6XpVUSU6JRWK=
COLO-829 NYLHOYc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[zTWM2OD15LkK0NVg5KM7:TR?= MkK5V2FPT0WU
NCI-H1650 NX;mcIFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH24UVFKSzVyPUeuN|kzOjhizszN NYHDVXRUW0GQR1XS
NCI-H358 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTdwNES4O|kh|ryP M1PRNXNCVkeHUh?=
HT-1080 MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[2Z2lEPTB;Nz60PFI2PCEQvF2= Ml\sV2FPT0WU
HCC2218 M3GxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX21Tmd2UUN3ME23MlYzQTdizszN MYnTRW5ITVJ?
NCI-H661 NEewNndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLSTWM2OD15Lki3NFY6KM7:TR?= NIH4RYFUSU6JRWK=
KM-H2 NXS3cnpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzuTWM2OD15Lki4Olk1KM7:TR?= NInMd29USU6JRWK=
RPMI-2650 NYXyNnRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPKTWM2OD15Lkm0OFE1KM7:TR?= NFz6ZYJUSU6JRWK=
NCI-H226 NUfuSXdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVz5RVQzUUN3ME24MlIyOTJ{IN88US=> NH7XR3FUSU6JRWK=
MKN45 NEX5WXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPtOlNKSzVyPUiuNlY3ODJizszN MX7TRW5ITVJ?
D-392MG MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRThwNUK3NlIh|ryP MVjTRW5ITVJ?
RCC10RGB M1[xS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PiRmlEPTB;OD64OlY6PSEQvF2= NYrSbpl6W0GQR1XS
CAL-51 MoP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1z5T2lEPTB;OT6xNFI2OSEQvF2= MWDTRW5ITVJ?
COLO-678 M4nS[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHMfXFKSzVyPUmuN|I5OTFizszN M1HQ[nNCVkeHUh?=
SK-MEL-24 NXLiR4d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f3UGlEPTB;OT61OVg2PiEQvF2= NYKzS|llW0GQR1XS
SK-MEL-30 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;Mb4RjUUN3ME25Mlk1PDd4IN88US=> NWnSZoRGW0GQR1XS
MMAC-SF NUi5b492T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jiXGlEPTB;MUCuN|k3OSEQvF2= NGLPS2lUSU6JRWK=
NTERA-S-cl-D1 NWq4VZpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFyLk[1NFgh|ryP MnHTV2FPT0WU
NB12 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTFzLkWwN{DPxE1? MX;TRW5ITVJ?
UACC-257 NEDkXotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILrNWZKSzVyPUGxMlg3QTVizszN NYrjTVZkW0GQR1XS
LAN-6 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTFzLkm5Nlgh|ryP MnfQV2FPT0WU
SW1573 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jLS2lEPTB;MUKuN|A5PiEQvF2= MWXTRW5ITVJ?
NMC-G1 NIj3VnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnX0TWM2OD1zMj60NVc2KM7:TR?= Mlj1V2FPT0WU
SHP-77 NWXPcoVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLmTWM2OD1zMj61OVc1KM7:TR?= NEjaemNUSU6JRWK=
IGROV-1 MnnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnqxTWM2OD1zMj62OVc{KM7:TR?= M33ud3NCVkeHUh?=
22RV1 NWXCTmNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zK[2lEPTB;MUKuPFA2QSEQvF2= MWDTRW5ITVJ?
SK-MEL-3 M3zCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn3U21KSzVyPUGzMlM6PzNizszN NY[0RWlWW0GQR1XS
NCI-H1563 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF|LkSyNFIh|ryP Mne3V2FPT0WU
IGR-1 NFnSfpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jsTGlEPTB;MUSuNFM1PyEQvF2= NXXXOpBLW0GQR1XS
EW-3 MnrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fWfmlEPTB;MUSuNVY{QSEQvF2= NUPocZlPW0GQR1XS
JEG-3 MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTF2LkS5OVMh|ryP NEHL[JBUSU6JRWK=
ES3 NYn5bJFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xye2lEPTB;MUSuOlU3OiEQvF2= M33xT3NCVkeHUh?=
MDA-MB-175-VII MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjaW2R7UUN3ME2xOE44OTFzIN88US=> M4LSSnNCVkeHUh?=
P30-OHK NHPKSoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnvZVlKSzVyPUG1MlA1QTZizszN NX\pZoo2W0GQR1XS
GP5d MkjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTF3LkG0OlYh|ryP NVvHdGxvW0GQR1XS
HMV-II MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTF3LkOzN|Mh|ryP MkfSV2FPT0WU
COLO-679 M37PbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTNTWM2OD1zNT61NFEh|ryP NVj1fXh7W0GQR1XS
JAR MmrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTF3LkeyNFUh|ryP MUDTRW5ITVJ?
NCI-H1666 MkHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XhRWlEPTB;MUWuPVM6QSEQvF2= NVPCW4h1W0GQR1XS
SW48 M4[2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3FOWNKSzVyPUG1Mlk2OTZizszN NXizO2NXW0GQR1XS
NCI-H720 NXjCWnp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPKN2VKSzVyPUG1Mlk6QDlizszN M{fQcnNCVkeHUh?=
HT-1197 NVPVVJVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfPd2prUUN3ME2xOk4xOzV{IN88US=> M3yxfXNCVkeHUh?=
HL-60 NYHDXnNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XnVGlEPTB;MU[uNFM5PCEQvF2= M2TFOXNCVkeHUh?=
BEN NHvPXFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;vVG9HUUN3ME2xOk42PjN6IN88US=> NUDTfIlqW0GQR1XS
HAL-01 M1nzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTJOHlFUUN3ME2xOk45QTB7IN88US=> M4mxbnNCVkeHUh?=
SW900 MlO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF4LkmxN|Ih|ryP MoO5V2FPT0WU
SBC-1 Ml36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XGVGlEPTB;MUeuOVQzQSEQvF2= MYDTRW5ITVJ?
SH-4 M3PxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHvTWM2OD1zNz61PFQyKM7:TR?= M1q2dXNCVkeHUh?=
UACC-62 MkjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoS0TWM2OD1zNz63OlM4KM7:TR?= NHjnZYZUSU6JRWK=
BHT-101 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HESWlEPTB;MUmuPFcxPSEQvF2= MmTHV2FPT0WU
DB Mn7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTJzLkW2OFkh|ryP MoPjV2FPT0WU
SK-MEL-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPrTWM2OD1{MT61PFczKM7:TR?= NFzzU|BUSU6JRWK=
NCI-H747 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPPTWM2OD1{Mj63N|c6KM7:TR?= M3K4ZXNCVkeHUh?=
SK-LU-1 NXfJOmVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlH3TWM2OD1{Mz6zOVI1KM7:TR?= M4O5ZnNCVkeHUh?=
KG-1 MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LocWlEPTB;MkOuOFk1PiEQvF2= MY\TRW5ITVJ?
LXF-289 NFr3d2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJ|LkexOEDPxE1? NYrsdollW0GQR1XS
HCC1954 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrGTWM2OD1{ND64PFQ1KM7:TR?= NXL5WJlWW0GQR1XS
Ramos-2G6-4C10 NFW2bIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXkTFNnUUN3ME2yOk41QThzIN88US=> MYXTRW5ITVJ?
DBTRG-05MG NWjm[G5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf3OGdKSzVyPUK2MlY1QDhizszN MX;TRW5ITVJ?
NCI-H2052 NE\GdGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPlPGpJUUN3ME2yO{42Pjh2IN88US=> MnnmV2FPT0WU
RMG-I M2TFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnyfJU1UUN3ME2yPU41OTN7IN88US=> M{Ph[nNCVkeHUh?=
H9 NWnpWmhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHBXoVKSzVyPUOxMlMxODhizszN NGTtU|BUSU6JRWK=
GR-ST NVjwOGp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTN{LkS0OVMh|ryP NVXITlZOW0GQR1XS
Mo-T NISxcldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorzTWM2OD1|Mj61NFQ3KM7:TR?= NHTsN|lUSU6JRWK=
SW1088 NWe0Oll[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jrWWlEPTB;M{KuPVgxOSEQvF2= MUnTRW5ITVJ?
LB2518-MEL M331VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HiTmlEPTB;M{OuNFc6PyEQvF2= NFPER|hUSU6JRWK=
NCI-H82 MnrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTN|LkG2OlEh|ryP NHj3XnRUSU6JRWK=
LAMA-84 NEfaTm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3tPJdKSzVyPUO0MlYxPzNizszN NHHTZYFUSU6JRWK=
KYSE-450 NYmxcmJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjWUZZKSzVyPUO0MlY4PzZizszN NWfpS3MxW0GQR1XS
LU-99A M4L1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPjSYlKSzVyPUO1MlAxODdizszN MV;TRW5ITVJ?
BE-13 NYP1TY1uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TnTmlEPTB;M{WuOlU1PSEQvF2= M2\qcHNCVkeHUh?=
GAK M3rVOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37hc2lEPTB;M{WuOlk2KM7:TR?= NHv4XYRUSU6JRWK=
NCI-H1573 NHPYdVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jWemlEPTB;M{WuPFgyQCEQvF2= MY\TRW5ITVJ?
AsPC-1 NY\YU3A4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGKzbYhKSzVyPUO2MlE2OjdizszN MknOV2FPT0WU
HDLM-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXMRpJLUUN3ME2zOk4{OTZizszN NInnfHVUSU6JRWK=
NCI-H441 NVO0[FJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jhc2lEPTB;M{euNFY6OSEQvF2= MYnTRW5ITVJ?
CAL-27 NEf5TmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXO2WlEzUUN3ME2zO{44OjNzIN88US=> NU\YVHpqW0GQR1XS
OVCAR-3 M1\4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXL[HVKSzVyPUO5MlMyQDFizszN NH7ncVhUSU6JRWK=
RPMI-8226 MoTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PC[mlEPTB;M{muOVk5KM7:TR?= NWDwU2RNW0GQR1XS
EFO-21 M3H3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTRyLkW4NVQh|ryP MXjTRW5ITVJ?
SNU-C2B M{PlW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTRzLkWwPFQh|ryP MX3TRW5ITVJ?
VM-CUB-1 M1jZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P6NGlEPTB;NEOuPFA{PyEQvF2= MV;TRW5ITVJ?
NCI-H2087 NEXa[ZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3W3VWlEPTB;NEWuNFI{OyEQvF2= NYG5d5EyW0GQR1XS
EW-16 NHf3bHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELydWJKSzVyPUS2MlMyOzdizszN M1ToNXNCVkeHUh?=
SK-N-AS MlnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPiTWM2OD12Nj63NVY4KM7:TR?= MUjTRW5ITVJ?
COR-L105 NYO5RpRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4S2e2lEPTB;NE[uPFg2PyEQvF2= MkD1V2FPT0WU
DEL NUK2N4ltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYf3OFNCUUN3ME20PE4xPDJ7IN88US=> MoTHV2FPT0WU
JVM-2 NGXyOWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\lfmtJUUN3ME20PE4xPTV6IN88US=> NF3IXYdUSU6JRWK=
KARPAS-45 NFH1fFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHXd5RKSzVyPUS5MlQ2OzhizszN MoHUV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53 / MDM2 / p21 / Bax / Bak / Noxa / cleaved caspase / pro-caspase; 

PubMed: 16014563     


Expression of apoptosis- and cell-cycle–associated proteins in OCI-AML-3 cells, which were treated with 5 μM Nutlin-3a for the indicated times. Nutlin-3a induced increased protein expression of p53, MDM2, and p21 in OCI-AML-3 cells in a time-dependent fashion. Nutlin-3a induced Noxa, a BH3-only member of the Bcl-2 family, followed by caspase activation. β-actin was used to confirm equal loading of proteins. Arrowheads indicate cleared caspases.

BMI-1; 

PubMed: 26887044     


Western blot analysis of BMI-1 and actin was performed in BV-173, SUP-B15, NALM-6, NALM-19 and REH cell lines after 24 hours treatment with increasing concentrations of Nutlin-3a (1 μM, 2 μM, 5 μM) and with DMSO control. 

p53-Ser15 / p53-Ser37 / p53-Lys382 / MDM2 / CDC2 / PLK1 / HSC70; 

PubMed: 23666059     


Expression of the indicated proteins in whole-cell lysates of cells treated for 96 h with 50 μM resveratrol (R), 5 μM nutlin-3a (N), or co-treated with both substances (RN).

16014563 26887044 23666059
Immunofluorescence
p-p21 / β-actin; 

PubMed: 31083332     


Cells were treated with fluoride (5 mM) with/without Nutlin-3a for 24 h. p-p21 (green), nucleus (DAPI; blue) and β-actin (red) expression were detected by immunocytochemistry. Nutlin-3a addition augmented p-p21 expression compared to NaF treatment alone.

P53; 

PubMed: 21394100     


At 12 h following treatment with nutlin-3a, DoHH2 and MCA cells had increased levels of p53 visualized by immunofluorescence. p53 localization was predominantly nuclear. The 4',6-diamidino-2-phenylindole was used as counterstain of the nuclei.

Ac-p300; 

PubMed: 30240745     


HepG2 cells were treated with 5 μM Nutlin-3a for 24 hr, and the levels of Ac-p300 and p53 were assessed by co-immunofluorescence. Fluorescence intensity of Ac-p300 in control cells versus Nutlin-3a-treated cells have been quantified (represented as mean ± SD, unpaired two-tailed Student's t test, n = 50 of three independent experiments). Scale bar, 10 μm.

31083332 21394100 30240745
Growth inhibition assay
Cell viability; 

PubMed: 26248031     


All 15 cell lines were plated in 96-well plates. After 24h, media was exchanged and cells were treated with incremental concentrations of Nutlin-3a (1 μM, 5 μM, 10 μM, 25 μM, 50 μM, and 70 μM). After 72h of Nutlin-3a treatment, cell viability was measured by WST assay and compared to untreated control.

26248031
体内研究 Nutlin-3α以剂量依赖性方式抑制异种移植物生长,在最高剂量(200毫克/千克)时表现大量的肿瘤收缩。Nutlin-3是p53途径在体内的选择性活化剂,并高度有效地抗SJSA-1骨肉瘤。有野生型p53和MDM2基因扩增的肿瘤对Nutlin-3α治疗应答最好。 [1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[3]
- 合并

Biacore研究:

竞争分析是在Biacore S51进行。甲系列S传感器芯片CM5衍生化用于固定一个PentaHis抗体来捕获His-标记的p53。捕获的水平是〜200响应单位(1单位响应对应于每毫米21 pg的蛋白质)。 MDM2蛋白的浓度被保持恒定在300 nM。将试验化合物溶解于10 mM DMSO中,并进一步稀释使每个MDM2测试样品中的浓度系列抑制剂。该试验是在25¡交流的电泳缓冲液(10 mM HEPES,0.15M的NaCl,2%DMSO)中运行。 MDM2-p53在抑制剂存在下的结合的计算方法是在没有抑制剂的结合的百分比,IC 50是使用微软EXCE计算。
细胞实验:[2]
- 合并
  • Cell lines: OSA, T778, RMS13, U2OS, SaOS-2
  • Concentrations: ~5 μM
  • Incubation Time: 120小时
  • Method: SRB
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: SJSA-1移植体
  • Dosages: 50, 100, 200 毫克/千克 每天两次
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (171.97 mM)
Ethanol 100 mg/mL (171.97 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+55% PEG 300+ddH2O
8mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 581.49
化学式

C30H30Cl2N4O4

CAS号 675576-98-4
储存条件 粉状
溶于溶剂
别名 (-)-Nutlin-3

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    What is the difference between S1061 (Nutlin-3) and S8059 (Nutlin-3a)?

  • 回答:

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

Mdm2 Signaling Pathway Map

相关Mdm2产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID