Home Cell Cycle Aurora Kinase inhibitor - Autophagy activator - Apoptosis related activator Alisertib (MLN8237) 仅限科研使用

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

Alisertib (MLN8237) Chemical Structure

CAS: 1028486-01-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1375.12 现货
5mg 983.87 现货
50mg 5505.84 现货
200mg 14496.3 现货
1g 40868.1 现货
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常与Alisertib (MLN8237)一起在实验中被使用的化合物

Barasertib (AZD1152-HQPA)

Alisertib和Barasertib强烈抑制急性髓细胞性白血病细胞的生长和增殖。

Volasertib

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。

Lenvatinib

Alisertib和Lenvatinib显着增强对裸鼠肿瘤生长的抑制并诱导细胞凋亡。

Irinotecan

Alisertib和Irinotecan以及Temozolomide在MYCN非扩增肿瘤患者中显示出抗肿瘤活性。

Paclitaxel

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

Aurora Kinase Signaling Pathways

Aurora Kinase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(PMID)
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
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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
Aurora A [1]
(Cell-free assay)
1.2 nM
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]
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。
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]
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
  • https://pubmed.ncbi.nlm.nih.gov/22016509/
  • https://pubmed.ncbi.nlm.nih.gov/20382844/
  • https://pubmed.ncbi.nlm.nih.gov/22302096/

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)

体外溶解度
批次：

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
批次：

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

摩尔浓度计算器

质量 浓度 体积 分子量

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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操作手册

如果有其他问题，请给我们留言。

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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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