Alisertib (MLN8237)
中文名称：阿利色替
Alisertib (MLN8237)是一种选择性Aurora A抑制剂，无细胞试验中IC50为1.2 nM，作用于Aurora A比作用于Aurora B选择性强200倍以上。Alisertib 可诱导细胞周期阻滞、细胞凋亡与自噬。Phase 3。
Alisertib (MLN8237) Chemical Structure
CAS: 1028486-01-2
产品质控
批次：
纯度：
99.5%
99.5
常与Alisertib (MLN8237)一起在实验中被使用的化合物
Alisertib和Barasertib强烈抑制急性髓细胞性白血病细胞的生长和增殖。
Alisertib和Volasertib抑制AURKA和PLK1，并协同阻断弥漫性中线胶质瘤细胞的细胞周期进展。
Alisertib和Lenvatinib显着增强对裸鼠肿瘤生长的抑制并诱导细胞凋亡。
Alisertib和Irinotecan以及Temozolomide在MYCN非扩增肿瘤患者中显示出抗肿瘤活性。
DuBois SG, et al.Clin Cancer Res. 2018 Dec 15;24(24):6142-6149.
Alisertib和Paclitaxel在三阴性乳腺癌异种移植模型中具有相加和协同的抗肿瘤作用。
Alisertib (MLN8237)相关产品
相关信号通路图
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 |
|---|---|---|---|---|---|
| OE33 | Cytotoxic Assay | 0.5 μM | 24 h | Decreases cell survival | 22972611 |
| FLO-1 | Cytotoxic Assay | 0.5 μM | 24 h | Decreases cell survival | 22972611 |
| AGS | Cytotoxic Assay | 0.5 μM | 24 h | Decreases cell survival | 22972611 |
| TIB-48 | Cytotoxic Assay | 1 μM | 48 h | Induces apoptosis | 23153524 |
| CRL-2396 | Cytotoxic Assay | 1 μM | 48 h | Induces apoptosis | 23153524 |
| 2885 | Growth Inhibition Assay | 100 μM | 72 h | Attenuates cell growth | 23328114 |
| 2884 | Growth Inhibition Assay | 100 μM | 72 h | Attenuates cell growth | 23328114 |
| S462 | Growth Inhibition Assay | 100 μM | 72 h | Attenuates cell growth | 23328114 |
| UM-UC-3 | Apoptosis Assay | 3.16 μM | 96 h | IC50=0.0449 μM | 23403633 |
| RT4 | Apoptosis Assay | 3.16 μM | 96 h | IC50=0.1198 μM | 23403633 |
| T24 | Apoptosis Assay | 3.16 μM | 96 h | IC50=0.0306 μM | 23403633 |
| UM-UC-3 | Function Assay | 1 μM | 48 h | Induces cell cycle arrest | 23403633 |
| RT4 | Function Assay | 1 μM | 48 h | Induces cell cycle arrest | 23403633 |
| T24 | Function Assay | 1 μM | 48 h | Induces cell cycle arrest | 23403633 |
| GB169 | Growth Inhibition Assay | 1 μM | 7 d | IC50=0.032 μM | 25106428 |
| GB9 | Growth Inhibition Assay | 1 μM | 7 d | IC50=0.024 μM | 25106428 |
| GB30 | Growth Inhibition Assay | 1 μM | 7 d | IC50=0.011 μM | 25106428 |
| HSC-3 | Growth Inhibition Assay | 1 μM | 48 h | IC50=0.54 μM | 25366143 |
| NCI-N78 | Function Assay | 5 μM | 24 h | Induces the autophagy | 25609923 |
| AGS | Function Assay | 5 μM | 24 h | Induces the autophagy | 25609923 |
| NCI-N78 | Apoptosis Assay | 5 μM | 24 h | Induces apoptosis | 25609923 |
| AGS | Apoptosis Assay | 5 μM | 24 h | Induces apoptosis | 25609923 |
| NCI-N78 | Growth Inhibition Assay | 25 μM | 24 h | IC50=26.33 μM | 25609923 |
| AGS | Growth Inhibition Assay | 25 μM | 24 h | IC50=19.09 μM | 25609923 |
| OVCAR4 | Apoptosis Assay | 5 μM | 24 h | Induces apoptosis | 25624750 |
| SKOV3 | Apoptosis Assay | 5 μM | 24 h | Induces apoptosis | 25624750 |
| OVCAR4 | Function Assay | 5 μM | 72 h | Induces G2/M arrest | 25624750 |
| SKOV3 | Function Assay | 5 μM | 72 h | Induces G2/M arrest | 25624750 |
| OVCAR4 | Growth Inhibition Assay | 100 μM | 24 h | IC50=22.13 μM | 25624750 |
| SKOV3 | Growth Inhibition Assay | 100 μM | 24 h | IC50=20.48 μM | 25624750 |
| BxPC-3 | Function Assay | 5 μM | 24 h | Induces autophagic cell death | 25632225 |
| PANC-1 | Function Assay | 5 μM | 24 h | Induces autophagic cell death | 25632225 |
| BxPC-3 | Function Assay | 5 μM | 24 h | Induces cell cycle arrest in G2/M phase | 25632225 |
| PANC-1 | Function Assay | 5 μM | 24 h | Induces cell cycle arrest in G2/M phase | 25632225 |
| BxPC-3 | Growth Inhibition Assay | 50 μM | 24 h | IC50=6.8 μM | 25632225 |
| PANC-1 | Growth Inhibition Assay | 50 μM | 24 h | IC50=7.1 μM | 25632225 |
| MG-63 | Function Assay | 5 μM | 24 h | Promotes autophagic cell death | 25792811 |
| U-2 OS | Function Assay | 5 μM | 24 h | Promotes autophagic cell death | 25792811 |
| MG-63 | Apoptosis Assay | 5 μM | 24 h | Induces apoptotic cell death | 25792811 |
| U-2 OS | Apoptosis Assay | 5 μM | 24 h | Induces apoptotic cell death | 25792811 |
| MG-63 | Growth Inhibition Assay | 50 μM | 24 h | IC50=9.5 μM | 25792811 |
| U-2 OS | Growth Inhibition Assay | 50 μM | 24 h | IC50=16.6 μM | 25792811 |
| MDA-MB-231 | Function Assay | 1 μM | 72 h | Induces autophagic death | 25834401 |
| MCF7 | Function Assay | 1 μM | 72 h | Induces autophagic death | 25834401 |
| MDA-MB-231 | Apoptosis Assay | 5 μM | 24 h | Induces apoptotic death | 25834401 |
| MCF7 | Apoptosis Assay | 5 μM | 24 h | Induces apoptotic death | 25834401 |
| MDA-MB-231 | Function Assay | 5 μM | 24 h | Increases the expression level of p53 | 25834401 |
| MDA-MB-231 | Function Assay | 5 μM | 24 h | Increases the expression level of p27 Kip1 | 25834401 |
| MDA-MB-231 | Function Assay | 5 μM | 24 h | Increases the expression level of p21 Waf1/Cip1 | 25834401 |
| MDA-MB-231 | Function Assay | 5 μM | 24 h | Decreases the expression level of cyclin B1 | 25834401 |
| MDA-MB-231 | Function Assay | 1 μM | 24 h | Increases the expression level of CDK2 | 25834401 |
| MDA-MB-231 | Function Assay | 5 μM | 24 h | Decreases the expression level of CDK1/CDC2 | 25834401 |
| MCF7 | Function Assay | 5 μM | 24 h | Increases the expression level of p27 Kip1 | 25834401 |
| MCF7 | Function Assay | 5 μM | 24 h | Increases the expression level of p21 Waf1/Cip1 | 25834401 |
| MCF7 | Function Assay | 5 μM | 24 h | Decreases the expression level of cyclin B1 | 25834401 |
| MCF7 | Function Assay | 5 μM | 24 h | Decreases the expression level of CDK2 | 25834401 |
| MCF7 | Function Assay | 5 μM | 24 h | Decreases the expression level of CDK1/CDC2 | 25834401 |
| MDA-MB-231 | Function Assay | 5 μM | 24 h | Induces G3/M arrest | 25834401 |
| MCF7 | Function Assay | 5 μM | 24 h | Induces G2/M arrest | 25834401 |
| SNU1544 | Growth Inhibition Assay | 0.5 μM | 72 h | IC50=1 μM | 26136684 |
| MIP-101 | Growth Inhibition Assay | 0.5 μM | 72 h | IC50=1 μM | 26136684 |
| DLD-1 | Growth Inhibition Assay | 0.5 μM | 72 h | IC50<0.8 μM | 26136684 |
| HCT15 | Growth Inhibition Assay | 0.5 μM | 72 h | IC50<0.4 μM | 26136684 |
| SW948 | Growth Inhibition Assay | 0.5 μM | 72 h | IC50=1 μM | 26136684 |
| LS180 | Growth Inhibition Assay | 0.5 μM | 72 h | IC50=1 μM | 26136684 |
| T84 | Growth Inhibition Assay | 0.5 μM | 72 h | IC50=0.09 μM | 26136684 |
| LS174T | Growth Inhibition Assay | 0.5 μM | 72 h | IC50=0.05 μM | 26136684 |
| HCT116 | Growth Inhibition Assay | 0.5 μM | 72 h | IC50=0.04 μM | 26136684 |
| SKLMS | Cytotoxic Assay | 75 nM | 96 h | Induces apoptosis | 22821997 |
| Leio285 | Cytotoxic Assay | 75 nM | 96 h | Induces apoptosis | 22821997 |
| Mes-Sa | Cytotoxic Assay | 75 nM | 96 h | Induces apoptosis | 22821997 |
| DAOY | Cytotoxic Assay | 10 μM | 72 h | IC50=0.04 μM | 22669335 |
| IMR32 | Cytotoxic Assay | 10 μM | 72 h | IC50=0.03 μM | 22669335 |
| Molt-4 | Cytotoxic Assay | 10 μM | 72 h | IC50=0.02 μM | 22669335 |
| MOLM-13 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| HL-60 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| MV4-11 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| SKM-1 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| SH2 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| NOMO-1 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| OCL-AML2 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| PL-21 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| KG-1 | Growth Inhibition Assay | 3 μM | 72 h | Diminishes cell viability | 22488249 |
| A172 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.120 μM | 22274399 |
| U87 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.105 μM | 22274399 |
| U251 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.100 μM | 22274399 |
| T98 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.125 μM | 22274399 |
| LN18 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.210 μM | 22274399 |
| LN443 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.220 μM | 22274399 |
| HF66 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.225 μM | 22274399 |
| HF2303 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.060 μM | 22274399 |
| HF2359 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.060 μM | 22274399 |
| HF2414 | Cytotoxic Assay | 100 μM | 24 h | IC50=0.080 μM | 22274399 |
| A-673 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.032 μM | 21448591 |
| TC-32 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.039 μM | 21448591 |
| TC-71 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.102 μM | 21448591 |
| SK-N-MC | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.072 μM | 21448591 |
| CHLA-9 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.018 μM | 21448591 |
| CHLA-10 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.060 μM | 21448591 |
| CHLA-25 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.168 μM | 21448591 |
| CHLA-32 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.136 μM | 21448591 |
| CHLA-56 | Growth Inhibition Assay | 10 μM | 96 h | IC50=10 μM | 21448591 |
| CHLA-258 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.132 μM | 21448591 |
| COG-E-352 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.043 μM | 21448591 |
| CHLA-90 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.061 μM | 21448591 |
| CHLA-119 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.022 μM | 21448591 |
| CHLA-122 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.019 μM | 21448591 |
| CHLA-136 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.039 μM | 21448591 |
| CHLA-140 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.026 μM | 21448591 |
| LA-N-6 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.054 μM | 21448591 |
| NB-1643 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.037 μM | 21448591 |
| NB-EBc1 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.050 μM | 21448591 |
| SK-N-BE-1 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.028 μM | 21448591 |
| SK-N-BE-2 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.036 μM | 21448591 |
| SMS-KAN | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.034 μM | 21448591 |
| SMS-KANR | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.026 μM | 21448591 |
| SMS-KCN | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.019 μM | 21448591 |
| SMS-KCNR | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.010 μM | 21448591 |
| SMS-LHN | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.032 μM | 21448591 |
| SMS-MSN | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.022 μM | 21448591 |
| SMS-SAN | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.020 μM | 21448591 |
| Granta-4 | Cytotoxic Assay | 10 μM | 7 d | IC50=0.040 μM | 21291867 |
| DB | Cytotoxic Assay | 10 μM | 7 d | IC50=0.042 μM | 21291867 |
| RL | Cytotoxic Assay | 10 μM | 7 d | IC50=0.015 μM | 21291867 |
| K562 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.087 μM | 21091633 |
| LAMA-84 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.057 μM | 21091633 |
| MM15 | Growth Inhibition Assay | 4 μM | 72 h | IC50=0.13 μM | 20382844 |
| OPM1 | Growth Inhibition Assay | 4 μM | 72 h | IC50=0.03 μM | 20382844 |
| RPM1 | Growth Inhibition Assay | 4 μM | 72 h | IC50=10.32 μM | 20382844 |
| INA6 | Growth Inhibition Assay | 4 μM | 72 h | IC50=0.002 μM | 20382844 |
| OPM2 | Growth Inhibition Assay | 4 μM | 72 h | IC50=4.37 μM | 20382844 |
| MM1R | Growth Inhibition Assay | 4 μM | 72 h | IC50=1.68 μM | 20382844 |
| DOX40 | Growth Inhibition Assay | 4 μM | 72 h | IC50=5.48 μM | 20382844 |
| LR5 | Growth Inhibition Assay | 4 μM | 72 h | IC50=2.53 μM | 20382844 |
| U266 | Growth Inhibition Assay | 4 μM | 72 h | IC50=1.43 μM | 20382844 |
| RD | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.228 μM | 20108338 |
| Rh41 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.090 μM | 20108338 |
| Rh30 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.230 μM | 20108338 |
| BT-12 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.060 μM | 20108338 |
| CHLA-266 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.072 μM | 20108338 |
| TC-71 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.102 μM | 20108338 |
| SJ-GBM2 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.050 μM | 20108338 |
| NALM-6 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.062 μM | 20108338 |
| COG-LL-317 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.047 μM | 20108338 |
| RS4-11 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.018 μM | 20108338 |
| MOLT-4 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.026 μM | 20108338 |
| CCRF-CEM | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.094 μM | 20108338 |
| Kasumi-1 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.103 μM | 20108338 |
| Karpas-299 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.038 μM | 20108338 |
| Ramos-RA1 | Growth Inhibition Assay | 10 μM | 96 h | IC50=0.127 μM | 20108338 |
| Calu6 | Antitumor assay | 20 mg/kg | 21 days | Antitumor activity against human Calu6 cells xenografted in mouse assessed as tumor growth inhibition at 20 mg/kg, po bid administered for 21 days | 26101564 |
| HeLa Kyoto | Function assay | 0.25 uM | 20 hrs | Inhibition of Aurora A kinase localization at spindle microtubules in human HeLa Kyoto cells at 0.25 uM incubated for 20 hrs | 27391133 |
| MDA-MB-231 | Function assay | 1 uM | 48 hrs | Induction of chromosome alignment defects in human MDA-MB-231 cells at 1 uM after 48 hrs by DAPI staining based immunofluorescence assay | 29358147 |
| MDA-MB-231 | Function assay | 1 uM | 48 hrs | Induction of aberrant spindle formation with tripolar and tetrapolar occurrence in human MDA-MB-231 cells at 1 uM after 48 hrs by DAPI staining based immunofluorescence assay | 29358147 |
| MDA-MB-231 | Function assay | 0.5 uM | 48 hrs | Inhibition of alpha-tubulin in human MDA-MB-231 cells assessed as abolishment of regular location of protein at 0.5 uM after 48 hrs by DAPI staining based immunofluorescence assay | 29358147 |
| MDA-MB-231 | Function assay | 0.5 uM | 48 hrs | Inhibition of AURKA in human MDA-MB-231 cells assessed as abolishment of regular location of protein at 0.5 uM after 48 hrs by DAPI staining based immunofluorescence assay | 29358147 |
| TIB-48 | Growth Inhibition Assay | 100 μM | IC50=0.088 μM | 23153524 | |
| CRL-2396 | Growth Inhibition Assay | 100 μM | IC50=0.092 μM | 23153524 | |
| SKOV3ip2 | Function Assay | 50 nM | Inhibits cell migration | 23334327 | |
| OVCAR-5 | Function Assay | 50 nM | Inhibits cell migration | 23334327 | |
| Tib 152 | Cytotoxic Assay | 72 h | IC50=0.8 μM | 25878331 | |
| Sup-T1 | Cytotoxic Assay | 72 h | IC50=2.142 μM | 25878331 | |
| J.Cam 1.6 | Cytotoxic Assay | 72 h | IC50=0.105 μM | 25878331 | |
| CCL119 | Cytotoxic Assay | 72 h | IC50=0.062 μM | 25878331 | |
| DND41 | Cytotoxic Assay | 72 h | IC50=0.1 μM | 25878331 | |
| HH | Cytotoxic Assay | 72 h | IC50=0.7 μM | 25878331 | |
| H9 | Cytotoxic Assay | 72 h | IC50=0.6 μM | 25878331 | |
| Z-138 | Cytotoxic Assay | 72 h | IC50=0.013 μM | 25878331 | |
| Rec-1 | Cytotoxic Assay | 72 h | IC50=0.087 μM | 25878331 | |
| JVM-2 | Cytotoxic Assay | 72 h | IC50=0.01 μM | 25878331 | |
| Jeko-1 | Cytotoxic Assay | 72 h | IC50=0.029 μM | 25878331 | |
| SU-DHL6 | Cytotoxic Assay | 72 h | IC50=0.482 μM | 25878331 | |
| OCI-LY7 | Cytotoxic Assay | 72 h | IC50=0.081 μM | 25878331 | |
| SU-DHL2 | Cytotoxic Assay | 72 h | IC50=0.01 μM | 25878331 | |
| OCI-Ly10 | Cytotoxic Assay | 72 h | IC50=0.058 μM | 25878331 | |
| GSS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human GSS cells after 72 hrs by WST8 assay, IC50 = 0.039 μM. | 25625617 | |
| LU99A | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LU99A cells after 72 hrs by WST8 assay, IC50 = 0.062 μM. | 25625617 | |
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells after 72 hrs by WST8 assay, IC50 = 0.074 μM. | 25625617 | |
| LC2/ad | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LC2/ad cells after 72 hrs by WST8 assay, IC50 = 0.077 μM. | 25625617 | |
| MKN45 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MKN45 cells after 72 hrs by WST8 assay, IC50 = 0.093 μM. | 25625617 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay, IC50 = 0.095 μM. | 25625617 | |
| Lu116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Lu116 cells after 72 hrs by WST8 assay, IC50 = 0.097 μM. | 25625617 | |
| NCI-H358 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H358 cells after 72 hrs by WST8 assay, IC50 = 0.1 μM. | 25625617 | |
| MIAPaCa2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST8 assay, IC50 = 0.13 μM. | 25625617 | |
| PC14 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC14 cells after 72 hrs by WST8 assay, IC50 = 0.17 μM. | 25625617 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells after 72 hrs by WST8 assay, IC50 = 0.33 μM. | 25625617 | |
| HCT15 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT15 cells after 72 hrs by WST8 assay, IC50 = 0.74 μM. | 25625617 | |
| BL21 (DE3) Rosetta | Function assay | 30 mins | Inhibition of His-tagged human Aurora A kinase (122 to 40 residues) expressed in Escherichia coli BL21 (DE3) Rosetta cells using biotinylated STK2 substrate incubated for 30 mins by HTRF assay, IC50 = 0.00004 μM. | 27391133 | |
| HeLa Kyoto | Function assay | 20 hrs | Inhibition of Aurora B kinase in human HeLa Kyoto cells assessed as effect on distribution of phspho-histone H3 ser10 level incubated for 20 hrs, IC50 = 0.0015 μM. | 27391133 | |
| HeLa Kyoto | Function assay | 20 hrs | Inhibition of Aurora A kinase autophosphorylation at Thr288 in human HeLa Kyoto cells incubated for 20 hrs, IC50 = 0.0067 μM. | 27391133 | |
| Sf9 | Function assay | Competitive inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells in presence of ATP, Ki = 0.0003 μM. | 26101564 | ||
| Sf9 | Function assay | Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP, IC50 = 0.001 μM. | 26101564 | ||
| HCT116 | Function assay | Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis, IC50 = 0.007 μM. | 26101564 | ||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay, GI50 = 0.03 μM. | 26101564 | ||
| HCT116 | Function assay | Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis, IC50 = 1.5 μM. | 26101564 | ||
| multiple myeloma | Function assay | Suppression of cell mitosis in human multiple myeloma cells, IC50 = 0.003 μM. | 28918096 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Alisertib (MLN8237)是一种选择性Aurora A抑制剂，无细胞试验中IC50为1.2 nM，作用于Aurora A比作用于Aurora B选择性强200倍以上。Alisertib 可诱导细胞周期阻滞、细胞凋亡与自噬。Phase 3。 | ||
|---|---|---|---|
| 特性 | MLN8237 是第一个口服有效的小分子Aurora A激酶选择性抑制剂。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | MLN8237作用于Aurora A选择性比作用于结构相关的Aurora B 高200多倍，IC50为396.5 nM, 而对205种其他激酶则没有显著活性。[1] 0.5 μM MLN8237处理MM1.S和 OPM1 细胞，抑制 Aurora A磷酸化，而不影响 Aurora B调节的组蛋白H3磷酸化。MLN8237作用于多发性骨髓瘤(MM) 细胞系，显著抑制细胞增殖，IC50为0.003-1.71 μM。在BM 基质细胞，IL-6和 IGF-1 存在时，MLN8237作用于原代MM 细胞和MM细胞系，抗增殖活性比只有MLN8237单独作用时高很多。0.5 μM MLN8237 作用于原代MM细胞和细胞系，使G2/M 期细胞提高2到6倍，且显著诱导凋亡和衰老，涉及p53, p21 和p27的上调,及 PARP,caspase 3,和 caspase 9的裂解。此外, MLN8237和 Hexadecadrol联用具有协同作用，具有强抗MM 功效, 而和Doxorubicin 及LDP-341联用则具有另外的功能。[2] 0.5 μM MLN8237处理 FLO-1, OE19, 和OE33 食管腺癌细胞系，抑制集落形成，且显著提高多倍体细胞百分数,随后提高G1期细胞百分数,而与 NSC 119875(2.5 μM)联用则效果进一步提高，与单独用药相比，诱导产生更多, TAp73β, PUMA, NOXA, cleaved caspase-3, 和cleaved PARP。[3] |
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|---|---|---|---|---|
| 激酶实验 | Aurora A放射性闪光板酶实验 | |||
| 进行Aurora A放射性闪光板酶实验，测定体外MLN8237抑制程度。在Sf9细胞中表达重组Aurora A，然后使用GST亲和层析进行纯化。Aurora A 肽底物与生物素联合形成生物素-GLRRASLG。在50 mM Hepes (pH 7.5), 10 mM MgCl2, 5 mM DTT, 0.05% Tween-20, 2 μM 肽底物, 3.3 μCi/mL [γ-33 P]ATP 2 μM, 和浓度不断增高的MLN8237 的混合物中进行Aurora A激酶 (5 nM)实验。 | ||||
| 细胞实验 | 细胞系 | MM1.S, MM.1R, LR5, RPMI 8226, DOX40, OPM1, OPM2, INA6, 和U266 | ||
| 浓度 | 溶于DMSO,终浓度为~10 μM | |||
| 孵育时间 | 24, 48, 和72小时 | |||
| 方法 | 使用不同浓度MLN8237处理细胞24, 48,和72小时。通过MTT实验测定细胞活力，通过测定 3[3H]-胸甘渗透而测定细胞增殖。为了分析细胞周期，使用70%乙醇在-20oC下使细胞通透，然后与50 μg/mL PI 和20 单位/mL RNase-A温育。 通过流式细胞仪使用 BDFACS-Canto II和FlowJo软件分析DNA含量。 为了测定凋亡和衰老，使用异硫氰酸荧光素-annexin V和PI对细胞进行染色。通过流式细胞仪使用 BDFACS-Canto II和FlowJo软件测定凋亡细胞。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-AURKA(T288) / p-EIF4E(S209) / c-Myc phospho-Aurora A / Aurora B H3S10P / H3K27me2 / H3K27me3 / H3K9me2 / H3AcK / H4K16Ac |
|
28073841 | |
| Growth inhibition assay | Cell viability |
|
25632225 | |
| Immunofluorescence | acetylated α-tubulin / γ-tubulin E-cadherin / β-catenin / vimentin / p-SMAD5 Centrin-2 / tubulin phospho-Aurora A(T288) |
|
29401581 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | MLN8237口服处理，显著降低肿瘤负担，按15 mg/kg 和30 mg/kg剂量处理肿瘤生长抑制率(TGI) 分别为42%和80%,且与对照组相比，延迟小鼠寿命。[2] MLN8237 (30 mg/kg) 与NSC 119875(2 mg/kg) 联用作用于FLO-1移植瘤，与单独用药相比，抗癌活性增强，伴随着Ki-67表达受抑制，细胞核p73蛋白和cleaved caspase 3表达增强。[3] |
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|---|---|---|
| 动物实验 | Animal Models | 皮下接种 MM1.S 细胞的SCID鼠 |
| Dosages | ~30 mg/kg/day | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04479306 | Completed | Recurrent Lung Non-Small Cell Carcinoma|Stage IIIB Lung Cancer AJCC v8|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 |
M.D. Anderson Cancer Center |
June 18 2020 | Phase 1 |
| NCT02812056 | Withdrawn | Malignant Neoplasms of Digestive Organs|Malignant Neoplasms of Female Genital Organs|Malignant Neoplasms of Lip Oral Cavity and Pharynx|Malignant Neoplasms of Male Genital Organs |
M.D. Anderson Cancer Center|Millennium Pharmaceuticals Inc. |
September 2016 | Phase 1 |
| NCT02719691 | Completed | Metastatic Breast Cancer|Solid Tumors |
University of Colorado Denver |
May 13 2016 | Phase 1 |
| NCT02367352 | Terminated | Advanced Solid Tumors|Ovarian Cancer|Small Cell Lung Cancer |
Millennium Pharmaceuticals Inc.|Takeda |
March 19 2015 | Phase 1 |
化学信息&溶解度
| 分子量 | 518.92 | 分子式 | C27H20ClFN4O4 |
| CAS号 | 1028486-01-2 | SDF | Download Alisertib (MLN8237) SDF |
| Smiles | COC1=C(C(=CC=C1)F)C2=NCC3=CN=C(N=C3C4=C2C=C(C=C4)Cl)NC5=CC(=C(C=C5)C(=O)O)OC | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 25 mg/mL ( (48.17 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 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。
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常见问题及建议解决方法
问题 1:
What is the suggested formulation of this compound for mouse injection(i.p.)?
回答：
It can be dissolved in 6% DMSO/50% PEG 300/5% Tween 80/ddH2O at 10 mg/ml as a clear solution.
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