Nutlin-3a
别名: (-)-Nutlin-3
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。
Nutlin-3a Chemical Structure
CAS: 675576-98-4
客户使用Selleck的Nutlin-3a发表文献87篇
产品质控
批次：
纯度：
99.79%
99.79
Nutlin-3a相关产品
| 相关靶点 | MDM2 MDMX p53-MDM2 interaction | 点击展开 |
|---|---|---|
| 相关产品 | Nutlin-3 RG-7112 Idasanutlin (RG7388) MI-773 (SAR405838) NSC 207895 NVP-CGM097 Siremadlin (HDM201) Nutlin-3b MX69 YH239-EE | 点击展开 |
| 相关化合物库 | 自噬化合物库 凋亡分子化合物库 铁死亡化合物库 细胞焦亡化合物库 线粒体靶向化合物库 | 点击展开 |
相关信号通路图
MDM2/MDMX抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MCF7 | Cell cycle assay | 4 uM | 14 days | Induction of cell cycle arrest in human MCF7 cells transfected with p53-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay | 16474381 |
| MCF7 | Cell cycle assay | 4 uM | 14 days | Induction of cell cycle arrest in human MCF7 cells transfected hnRNPK-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay | 16474381 |
| MCF7 | Antiproliferative assay | 4 uM | 14 days | Antiproliferative activity against human MCF7 cells at 4 uM after 14 days by coomassie staining | 16474381 |
| MCF7 | Antiproliferative assay | 4 uM | 14 days | Antiproliferative activity against human MCF7 cells assessed as appearance of flattened phenotype at 4 uM after 14 days by coomassie staining | 16474381 |
| MCF7 | Cell cycle assay | 4 uM | 14 days | Induction of cell cycle arrest in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay | 16474381 |
| SNJSA1 | Function assay | 1 to 10 uM | 6 hrs | Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of p21 protein at 1 to 10 uM after 6 hrs by Western blot analysis | 21314128 |
| SNJSA1 | Function assay | 1 to 10 uM | 6 hrs | Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of p53 protein at 1 to 10 uM after 6 hrs by Western blot analysis | 21314128 |
| SNJSA1 | Function assay | 1 to 10 uM | 6 hrs | Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of MDM2 protein at 1 to 10 uM after 6 hrs by Western blot analysis | 21314128 |
| HCT116 | Function assay | 50 uM | 24 hrs | Inhibition of p53-MDM2 (unknown origin) interaction expressed in p53-deficient human HCT116 cells at 50 uM after 24 hrs by BiFC-based FACS flow cytometric analysis | 24268795 |
| U2OS | Function assay | 2.5 uM | 12 hrs | Stabilization of p53 in human U2OS cells assessed as intracellular p53 level at 2.5 uM after 12 hrs by Western blotting | 26288684 |
| HCT116 | Function assay | 10 uM | 20 hrs | Inhibition of V1-p53/MDM2-V2 (unknown origin) interaction expressed in human HCT116 p53-/- cells at 10 uM after 20 hrs by biomolecular fluorescence complementation-based flow cytometric analysis | 28800455 |
| MCF7 | Function assay | 10 uM | 16 hrs | Inhibition of MDM2-p53 interaction in human MCF7 cells assessed as reversal of MDM2-dependent inhibition of p53-induced transcriptional activity at 10 uM after 16 hrs by dual-luciferase reporter gene assay | 23540934 |
| MCF7 | Apoptosis assay | 3 uM | 24 to 72 hrs | Induction of apoptosis in human MCF7 cells assessed as reduction in Bcl-xL expression level at 3 uM after 24 to 72 hrs by Western blotting analysis | 23802716 |
| MCF7 | Apoptosis assay | 3 uM | 24 to 72 hrs | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 3 uM after 24 to 72 hrs by annexin V-FITC/propidium iodide staining based FACS flow cytometry (Rvb = 4 %) | 23802716 |
| MCF7 | Apoptosis assay | 3 uM | 24 to 72 hrs | Induction of apoptosis in human MCF7 cells assessed as increase in p21 expression level at 3 uM after 24 to 72 hrs by Western blotting analysis | 23802716 |
| MCF7 | Apoptosis assay | 3 uM | 24 to 72 hrs | Induction of apoptosis in human MCF7 cells assessed as increase in Bcl-xS expression level at 3 uM after 24 to 72 hrs by Western blotting analysis | 23802716 |
| MCF7 | Apoptosis assay | 50 nM | 24 to 72 hrs | Induction of apoptosis in human MCF7 cells assessed as accumulation of caspase-3 cleavage product at 50 nM after 24 to 72 hrs by Western blotting analysis | 23802716 |
| MCF7 | Cell cycle assay | 3 uM | 24 to 72 hrs | Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 3 uM after 24 to 72 hrs by propidium iodide staining-based FACS analysis | 23802716 |
| SJSA1 | Function assay | 10 uM | Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as p53 activation at 10 uM by Western blot | 19928922 | |
| BJ | Function assay | 3 uM | Induction of p21CIP1 expression in irradiated human BJ cells at 3 uM by Western blot analysis | 16474381 | |
| BJ | Function assay | 3 uM | Induction of p21 expression in irradiated human BJ cells at 3 uM by Western blot analysis | 16474381 | |
| SJSA1 | Antiproliferative assay | 3 days | Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum, IC50 = 0.7 μM. | 22524527 | |
| HCT116 | Function assay | 24 hrs | Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs, IC50 = 1 μM. | 19856920 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay, IC50 = 1.3 μM. | 30221935 | |
| HCT116 | Function assay | 8 hrs | Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay, IC50 = 1.39 μM. | 19856920 | |
| HGF | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HGF cells after 24 hrs by MTT assay, IC50 = 1.4 μM. | 23802716 | |
| SJSA1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay, IC50 = 1.44 μM. | 30221935 | |
| SJSA1 | Cytotoxicity assay | 5 days | Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay, IC50 = 1.5 μM. | 24900694 | |
| RKO | Cytotoxicity assay | 5 days | Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay, IC50 = 1.5 μM. | 24900694 | |
| HCT116 | Cytotoxicity assay | 5 days | Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay, IC50 = 1.5 μM. | 24900694 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay, IC50 = 1.6 μM. | 24139845 | |
| SJSA1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay, IC50 = 1.9 μM. | 26985323 | |
| NGP | Cytotoxicity assay | 72 hrs | Cytotoxicity against human NGP cells after 72 hrs by sulforhodamine B assay, GI50 = 2.1 μM. | 21314128 | |
| LS | Cytotoxicity assay | 72 hrs | Cytotoxicity against human LS cells after 72 hrs by sulforhodamine B assay, GI50 = 2.3 μM. | 21314128 | |
| SJSA1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay, GI50 = 2.6 μM. | 21314128 | |
| MCF7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 2.9 μM. | 23802716 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay, IC50 = 4 μM. | 28987608 | |
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 4.62 μM. | 23601819 | |
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay, IC50 = 4.62 μM. | 23611770 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 5.01 μM. | 27101893 | |
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 5.1 μM. | 25479770 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 5.21 μM. | 27101893 | |
| UKF-NB-3 | Cytotoxicity assay | 96 hrs | Cytotoxicity against doxorubicin-resistant human UKF-NB-3 cells after 96 hrs by MTT assay, IC50 = 5.56 μM. | 20947617 | |
| SJSA1 | Function assay | 7 hrs | Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum, IC50 = 7.1 μM. | 22524527 | |
| HCT116 | Growth inhibition assay | 48 hrs | Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay, GI50 = 8 μM. | 29089230 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay, IC50 = 8.5 μM. | 30045621 | |
| HCT116 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis, GI50 = 9 μM. | 29691156 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay, IC50 = 9.07 μM. | 30045621 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay, IC50 = 9.58 μM. | 30045621 | |
| HepG2 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay, IC50 = 10.2 μM. | 23802716 | |
| NCI-H1299 | Antiproliferative assay | 72 hrs | Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay, IC50 = 10.4 μM. | 30221935 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 11.6 μM. | 25618595 | |
| Saos2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay, IC50 = 12.1 μM. | 22940704 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay, GI50 = 13 μM. | 21314128 | |
| U2OS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 14.31 μM. | 23046248 | |
| H1299 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay, IC50 = 14.7 μM. | 24139845 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 15 μM. | 22940704 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 15.12 μM. | 23046248 | |
| U937 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human U937 cells after 24 hrs by MTT assay, IC50 = 15.6 μM. | 23802716 | |
| Saos2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay, GI50 = 18 μM. | 21314128 | |
| U2OS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 19.6 μM. | 22940704 | |
| NCI-H1299 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay, IC50 = 19.76 μM. | 30045621 | |
| PC3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 20.04 μM. | 23601819 | |
| PC3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay, IC50 = 20.04 μM. | 23611770 | |
| NCI-H1299 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay, IC50 = 20.4 μM. | 22940704 | |
| NCI-H1299 | Antiproliferative assay | 72 hrs | Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay, IC50 = 20.48 μM. | 23046248 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 21.5 μM. | 27101893 | |
| SJSA1 | Cytotoxicity assay | 24 hrs | Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay, EC50 = 22.8 μM. | 29150077 | |
| C643 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human C643 cells after 24 hrs by MTT assay, IC50 = 23 μM. | 23802716 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 23.5 μM. | 25618595 | |
| U2OS | Antitumor assay | 72 hrs | Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay, IC50 = 24.61 μM. | 21996465 | |
| HCT116 | Growth inhibition assay | 48 hrs | Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay, GI50 = 27 μM. | 29089230 | |
| Calu | Cytotoxicity assay | 24 hrs | Cytotoxicity against human Calu cells after 24 hrs by MTT assay, IC50 = 27.2 μM. | 23802716 | |
| HCT116 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis, GI50 = 29 μM. | 29691156 | |
| MDA-MB-435S | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 29.6 μM. | 27101893 | |
| PC3 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human PC3 cells after 24 hrs by MTT assay, IC50 = 30.3 μM. | 23802716 | |
| Saos2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay, IC50 = 31.62 μM. | 23046248 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay, GI50 = 32.11 μM. | 24852275 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay, GI50 = 34 μM. | 21314128 | |
| HCT116 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay, GI50 = 39.65 μM. | 24268795 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50 = 47.59 μM. | 24852275 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay, IC50 = 47.8 μM. | 28987608 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, GI50 = 48.74 μM. | 24852275 | |
| MCF7 | Function assay | 18 hrs | Induction of p53 accumulation in human MCF7 cells after 18 hrs by Western blot analysis in presence of 2.5 mM caffeine | 16474381 | |
| MCF7 | Function assay | 24 hrs | Upregulation of p53 in human MCF7 cells after 24 hrs by Western blot analysis | 27010502 | |
| MCF7 | Function assay | 24 hrs | Upregulation of Mdm2 in human MCF7 cells after 24 hrs by Western blot analysis | 27010502 | |
| MCF7 | Function assay | 24 hrs | Increase in p53 expression in human MCF7 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy | 27010502 | |
| MCF7 | Function assay | 24 hrs | Upregulation of p21 in human MCF7 cells after 24 hrs by Western blot analysis | 27010502 | |
| IMR32 | Function assay | 24 hrs | Increase in p53 expression in human IMR32 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy | 27010502 | |
| 697 | Growth Inhibition Assay | IC50=5.4455 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=5.44244 μM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=4.91127 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=4.75072 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=4.62717 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=4.53019 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=4.50155 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=4.41411 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=4.33524 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=4.31768 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=4.27706 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=4.24392 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=4.07973 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=4.01959 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=3.85675 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=3.84333 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=3.80832 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=3.74297 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=3.65708 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=3.63552 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=3.62558 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=3.57986 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=3.53936 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=3.50848 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=3.44092 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=3.36322 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=3.30335 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=3.27843 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=3.26827 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=3.20966 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=3.17026 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=3.12694 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=3.12028 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=3.08496 μM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=3.05588 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=3.01623 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=2.97154 μM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=2.93882 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=2.9107 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=2.84439 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=2.82556 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=2.79502 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=2.72407 μM | SANGER | ||
| A172 | Growth Inhibition Assay | IC50=2.67588 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=2.65334 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=2.64577 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=2.64318 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=2.62471 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=2.61818 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=2.59324 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=2.57451 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=2.56576 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=2.56214 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=2.5411 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=2.50883 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=2.43155 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=2.42279 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=2.3501 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=2.32853 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=2.02246 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=1.81369 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=1.78604 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=1.60854 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=1.42072 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=1.26701 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=1.21572 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=1.04931 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=0.87096 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=0.6628 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=0.61237 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=5.57009 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=5.60029 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=5.73887 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=5.85667 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=6.01624 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=6.14828 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=6.22421 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=6.386 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=6.42428 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=6.55572 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=6.56183 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=6.58793 μM | SANGER | ||
| AM-38 | Growth Inhibition Assay | IC50=6.75639 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=6.76494 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=6.79026 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=6.87829 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=6.9323 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=7.24188 μM | SANGER | ||
| NCI-H1650 | Growth Inhibition Assay | IC50=7.39228 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=7.44879 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=7.48254 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=7.6297 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=7.87069 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=7.88694 μM | SANGER | ||
| RPMI-2650 | Growth Inhibition Assay | IC50=7.94414 μM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=8.21122 μM | SANGER | ||
| MKN45 | Growth Inhibition Assay | IC50=8.26602 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=8.52722 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=8.86695 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=9.10251 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=9.32811 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=9.55856 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=9.94476 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=10.3961 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=10.6508 μM | SANGER | ||
| NB12 | Growth Inhibition Assay | IC50=11.503 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=11.8695 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=11.9928 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=12.3086 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=12.4175 μM | SANGER | ||
| SHP-77 | Growth Inhibition Assay | IC50=12.5574 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=12.6573 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=12.8059 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=13.3973 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=13.4202 μM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=14.0347 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=14.1639 μM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=14.4953 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=14.6562 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=14.7111 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=15.0496 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=15.1466 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=15.3333 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=15.501 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=15.7205 μM | SANGER | ||
| NCI-H1666 | Growth Inhibition Assay | IC50=15.9399 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=15.9516 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=15.9989 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=16.0352 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=16.0384 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=16.5638 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=16.8909 μM | SANGER | ||
| SW900 | Growth Inhibition Assay | IC50=16.9132 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=17.5429 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=17.5841 μM | SANGER | ||
| UACC-62 | Growth Inhibition Assay | IC50=17.7637 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=19.8705 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=21.5649 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=21.5872 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=22.7379 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=23.3524 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=23.4946 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=23.714 μM | SANGER | ||
| HCC1954 | Growth Inhibition Assay | IC50=24.8844 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=26.4981 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=26.6488 μM | SANGER | ||
| NCI-H2052 | Growth Inhibition Assay | IC50=27.5684 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=29.4139 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=31.3008 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=32.4453 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=32.5046 μM | SANGER | ||
| SW1088 | Growth Inhibition Assay | IC50=32.9801 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=33.0797 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=33.1661 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=34.6073 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=34.6776 μM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=35.0007 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=35.6545 μM | SANGER | ||
| GAK | Growth Inhibition Assay | IC50=35.695 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=35.8818 μM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=36.1527 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=36.316 μM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=37.0691 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=37.7231 μM | SANGER | ||
| OVCAR-3 | Growth Inhibition Assay | IC50=39.3181 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=39.598 μM | SANGER | ||
| EFO-21 | Growth Inhibition Assay | IC50=40.5814 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=41.5084 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=43.8037 μM | SANGER | ||
| NCI-H2087 | Growth Inhibition Assay | IC50=45.0233 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=46.3137 μM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=46.7167 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=46.8857 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=48.0429 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=48.0558 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=49.4538 μM | SANGER | ||
| BL21 (DE3) | Function assay | Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay, Kd = 0.5 μM. | 18680271 | ||
| BL21 (DE3) | Function assay | Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay, Kd = 0.5 μM. | 18680271 | ||
| BL21 (DE3) | Function assay | Binding affinity to human recombinant Mdm2 F55W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration, Kd = 0.5 μM. | 18680271 | ||
| BL21 (DE3) | Function assay | Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration, Kd = 1 μM. | 18680271 | ||
| BL21 (DE3) | Function assay | Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration, Kd = 1 μM. | 18680271 | ||
| SJSA1 | Cytotoxicity assay | Cytotoxicity against human SJSA1 cells, IC50 = 1 μM. | 25396320 | ||
| RKO | Cytotoxicity assay | Cytotoxicity against human RKO cells, IC50 = 1 μM. | 25396320 | ||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells, IC50 = 1 μM. | 25396320 | ||
| SJSA1 | Growth inhibition assay | Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay, GI50 = 1.3 μM. | 21875801 | ||
| A2780 | Growth inhibition assay | Growth inhibition of human A2780 cells expressing MDM2 by SRB assay, GI50 = 1.6 μM. | 21875801 | ||
| SJSA1 | Antiproliferative assay | Antiproliferative activity against human SJSA1 cells, IC50 = 1.9 μM. | 24656661 | ||
| HCT116 | Growth inhibition assay | Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay, GI50 = 2.1 μM. | 21875801 | ||
| A2780/CP70 | Growth inhibition assay | Growth inhibition of human A2780/CP70 cells expressing isogenically paired p53 mutant by SRB assay, GI50 = 20.4 μM. | 21875801 | ||
| HCT116 | Growth inhibition assay | Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay, GI50 = 25.6 μM. | 21875801 | ||
| MCF7 | Function assay | Induction of p53 expression in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA by Western blot analysis | 16474381 | ||
| MCF7 | Function assay | Induction of p53 expression in human MCF7 cells by Western blot analysis | 16474381 | ||
| 点击查看更多细胞系数据 | |||||
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 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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] | |||
|---|---|---|---|---|
| 激酶实验 | 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 | 细胞系 | OSA, T778, RMS13, U2OS, SaOS-2 | ||
| 浓度 | ~5 μM | |||
| 孵育时间 | 120小时 | |||
| 方法 | SRB | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p53-Ser15 / p53-Ser37 / p53-Lys382 / MDM2 / CDC2 / PLK1 / HSC70 BMI-1 p53 / MDM2 / p21 / Bax / Bak / Noxa / cleaved caspase / pro-caspase |
|
23666059 | |
| Immunofluorescence | Ac-p300 P53 p-p21 / β-actin |
|
30240745 | |
| Growth inhibition assay | Cell viability |
|
26248031 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 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] | |
|---|---|---|
| 动物实验 | Animal Models | SJSA-1移植体 |
| Dosages | 50, 100, 200 毫克/千克 每天两次 | |
| Administration | 口服 | |
化学信息&溶解度
| 分子量 | 581.49 | 分子式 | C30H30Cl2N4O4 |
| CAS号 | 675576-98-4 | SDF | -- |
| 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 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (171.97 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
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）
mg/kg
g
μL
只
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
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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* 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.
Tags: buy Nutlin-3a | Nutlin-3a supplier | purchase Nutlin-3a | Nutlin-3a cost | Nutlin-3a manufacturer | order Nutlin-3a | Nutlin-3a distributor
