Home Cell Cycle Aurora Kinase inhibitor - Autophagy activator - Apoptosis related activator Alisertib (MLN8237) For research use only.

Alisertib (MLN8237)

Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.

Alisertib (MLN8237) Chemical Structure

Alisertib (MLN8237) Chemical Structure

CAS No. 1028486-01-2

Purity & Quality Control

Products often used together with Alisertib (MLN8237)

Barasertib (AZD1152-HQPA)

Alisertib and Barasertib strongly inhibit the growth and proliferation of AML cells.

Qi J, et al. Biomed Pharmacother. 2019 Sep;117:109113.

Volasertib

Alisertib and Volasertib inhibit AURKA and PLK1 and synergistically block cell cycle progression in diffuse midline glioma cells.

Metselaar DS, et al. iScience. 2022 May 13;25(6):104398.

Alisertib (MLN8237) Related Products

Signaling Pathway

Aurora Kinase Signaling Pathways

Aurora Kinase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 Growth Inhibition Assay 0.5 μM 72 h DMSO IC50=0.04 μM 26136684
LS174T Growth Inhibition Assay 0.5 μM 72 h DMSO IC50=0.05 μM 26136684
T84 Growth Inhibition Assay 0.5 μM 72 h DMSO IC50=0.09 μM 26136684
LS180 Growth Inhibition Assay 0.5 μM 72 h DMSO IC50=1 μM 26136684
SW948 Growth Inhibition Assay 0.5 μM 72 h DMSO IC50=1 μM 26136684
HCT15 Growth Inhibition Assay 0.5 μM 72 h DMSO IC50<0.4 μM 26136684
DLD-1 Growth Inhibition Assay 0.5 μM 72 h DMSO IC50<0.8 μM 26136684
MIP-101 Growth Inhibition Assay 0.5 μM 72 h DMSO IC50=1 μM 26136684
SNU1544 Growth Inhibition Assay 0.5 μM 72 h DMSO IC50=1 μM 26136684
OCI-Ly10 Cytotoxic Assay 72 h DMSO IC50=0.058 μM 25878331
SU-DHL2 Cytotoxic Assay 72 h DMSO IC50=0.01 μM 25878331
OCI-LY7 Cytotoxic Assay 72 h DMSO IC50=0.081 μM 25878331
SU-DHL6 Cytotoxic Assay 72 h DMSO IC50=0.482 μM 25878331
Jeko-1 Cytotoxic Assay 72 h DMSO IC50=0.029 μM 25878331
JVM-2 Cytotoxic Assay 72 h DMSO IC50=0.01 μM 25878331
Rec-1 Cytotoxic Assay 72 h DMSO IC50=0.087 μM 25878331
Z-138 Cytotoxic Assay 72 h DMSO IC50=0.013 μM 25878331
H9 Cytotoxic Assay 72 h DMSO IC50=0.6 μM 25878331
HH Cytotoxic Assay 72 h DMSO IC50=0.7 μM 25878331
DND41 Cytotoxic Assay 72 h DMSO IC50=0.1 μM 25878331
CCL119 Cytotoxic Assay 72 h DMSO IC50=0.062 μM 25878331
J.Cam 1.6 Cytotoxic Assay 72 h DMSO IC50=0.105 μM 25878331
Sup-T1 Cytotoxic Assay 72 h DMSO IC50=2.142 μM 25878331
Tib 152 Cytotoxic Assay 72 h DMSO IC50=0.8 μM 25878331
MCF7 Function Assay 5 μM 24 h DMSO Induces G2/M arrest 25834401
MDA-MB-231 Function Assay 5 μM 24 h DMSO Induces G3/M arrest 25834401
MCF7 Function Assay 5 μM 24 h DMSO Decreases the expression level of CDK1/CDC2 25834401
MCF7 Function Assay 5 μM 24 h DMSO Decreases the expression level of CDK2 25834401
MCF7 Function Assay 5 μM 24 h DMSO Decreases the expression level of cyclin B1 25834401
MCF7 Function Assay 5 μM 24 h DMSO Increases the expression level of p21 Waf1/Cip1 25834401
MCF7 Function Assay 5 μM 24 h DMSO Increases the expression level of p27 Kip1 25834401
MDA-MB-231 Function Assay 5 μM 24 h DMSO Decreases the expression level of CDK1/CDC2 25834401
MDA-MB-231 Function Assay 1 μM 24 h DMSO Increases the expression level of CDK2 25834401
MDA-MB-231 Function Assay 5 μM 24 h DMSO Decreases the expression level of cyclin B1 25834401
MDA-MB-231 Function Assay 5 μM 24 h DMSO Increases the expression level of p21 Waf1/Cip1 25834401
MDA-MB-231 Function Assay 5 μM 24 h DMSO Increases the expression level of p27 Kip1 25834401
MDA-MB-231 Function Assay 5 μM 24 h DMSO Increases the expression level of p53 25834401
MCF7 Apoptosis Assay 5 μM 24 h DMSO Induces apoptotic death 25834401
MDA-MB-231 Apoptosis Assay 5 μM 24 h DMSO Induces apoptotic death 25834401
MCF7 Function Assay 1 μM 72 h DMSO Induces autophagic death 25834401
MDA-MB-231 Function Assay 1 μM 72 h DMSO Induces autophagic death 25834401
U-2 OS Growth Inhibition Assay 50 μM 24 h DMSO IC50=16.6 μM 25792811
MG-63 Growth Inhibition Assay 50 μM 24 h DMSO IC50=9.5 μM 25792811
U-2 OS Apoptosis Assay 5 μM 24 h DMSO Induces apoptotic cell death 25792811
MG-63 Apoptosis Assay 5 μM 24 h DMSO Induces apoptotic cell death 25792811
U-2 OS Function Assay 5 μM 24 h DMSO Promotes autophagic cell death 25792811
MG-63 Function Assay 5 μM 24 h DMSO Promotes autophagic cell death 25792811
PANC-1 Growth Inhibition Assay 50 μM 24 h DMSO IC50=7.1 μM 25632225
BxPC-3 Growth Inhibition Assay 50 μM 24 h DMSO IC50=6.8 μM 25632225
PANC-1 Function Assay 5 μM 24 h DMSO Induces cell cycle arrest in G2/M phase 25632225
BxPC-3 Function Assay 5 μM 24 h DMSO Induces cell cycle arrest in G2/M phase 25632225
PANC-1 Function Assay 5 μM 24 h DMSO Induces autophagic cell death 25632225
BxPC-3 Function Assay 5 μM 24 h DMSO Induces autophagic cell death 25632225
SKOV3 Growth Inhibition Assay 100 μM 24 h DMSO IC50=20.48 μM 25624750
OVCAR4 Growth Inhibition Assay 100 μM 24 h DMSO IC50=22.13 μM 25624750
SKOV3 Function Assay 5 μM 72 h DMSO Induces G2/M arrest 25624750
OVCAR4 Function Assay 5 μM 72 h DMSO Induces G2/M arrest 25624750
SKOV3 Apoptosis Assay 5 μM 24 h DMSO Induces apoptosis 25624750
OVCAR4 Apoptosis Assay 5 μM 24 h DMSO Induces apoptosis 25624750
AGS Growth Inhibition Assay 25 μM 24 h DMSO IC50=19.09 μM 25609923
NCI-N78 Growth Inhibition Assay 25 μM 24 h DMSO IC50=26.33 μM 25609923
AGS Apoptosis Assay 5 μM 24 h DMSO Induces apoptosis 25609923
NCI-N78 Apoptosis Assay 5 μM 24 h DMSO Induces apoptosis 25609923
AGS Function Assay 5 μM 24 h DMSO Induces the autophagy 25609923
NCI-N78 Function Assay 5 μM 24 h DMSO Induces the autophagy 25609923
HSC-3 Growth Inhibition Assay 1 μM 48 h IC50=0.54 μM 25366143
GB30 Growth Inhibition Assay 1 μM 7 d DMSO IC50=0.011 μM 25106428
GB9 Growth Inhibition Assay 1 μM 7 d DMSO IC50=0.024 μM 25106428
GB169 Growth Inhibition Assay 1 μM 7 d DMSO IC50=0.032 μM 25106428
T24 Function Assay 1 μM 48 h DMSO Induces cell cycle arrest 23403633
RT4 Function Assay 1 μM 48 h DMSO Induces cell cycle arrest 23403633
UM-UC-3 Function Assay 1 μM 48 h DMSO Induces cell cycle arrest 23403633
T24 Apoptosis Assay 3.16 μM 96 h DMSO IC50=0.0306 μM 23403633
RT4 Apoptosis Assay 3.16 μM 96 h DMSO IC50=0.1198 μM 23403633
UM-UC-3 Apoptosis Assay 3.16 μM 96 h DMSO IC50=0.0449 μM 23403633
OVCAR-5 Function Assay 50 nM Inhibits cell migration 23334327
SKOV3ip2 Function Assay 50 nM Inhibits cell migration 23334327
S462 Growth Inhibition Assay 100 μM 72 h DMSO Attenuates cell growth 23328114
2884 Growth Inhibition Assay 100 μM 72 h DMSO Attenuates cell growth 23328114
2885 Growth Inhibition Assay 100 μM 72 h DMSO Attenuates cell growth 23328114
CRL-2396 Growth Inhibition Assay 100 μM water IC50=0.092 μM 23153524
TIB-48 Growth Inhibition Assay 100 μM water IC50=0.088 μM 23153524
CRL-2396 Cytotoxic Assay 1 μM 48 h water Induces apoptosis 23153524
TIB-48 Cytotoxic Assay 1 μM 48 h water Induces apoptosis 23153524
AGS Cytotoxic Assay 0.5 μM 24 h DMSO Decreases cell survival 22972611
FLO-1 Cytotoxic Assay 0.5 μM 24 h DMSO Decreases cell survival 22972611
OE33 Cytotoxic Assay 0.5 μM 24 h DMSO Decreases cell survival 22972611
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 DMSO IC50=0.04 μM 22669335
IMR32 Cytotoxic Assay 10 μM 72 h DMSO IC50=0.03 μM 22669335
Molt-4 Cytotoxic Assay 10 μM 72 h DMSO 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 DMSO IC50=0.120 μM 22274399
U87 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.105 μM 22274399
U251 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.100 μM 22274399
T98 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.125 μM 22274399
LN18 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.210 μM 22274399
LN443 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.220 μM 22274399
HF66 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.225 μM 22274399
HF2303 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.060 μM 22274399
HF2359 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.060 μM 22274399
HF2414 Cytotoxic Assay 100 μM 24 h DMSO IC50=0.080 μM 22274399
A-673 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.032 μM 21448591
TC-32 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.039 μM 21448591
TC-71 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.102 μM 21448591
SK-N-MC Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.072 μM 21448591
CHLA-9 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.018 μM 21448591
CHLA-10 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.060 μM 21448591
CHLA-25 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.168 μM 21448591
CHLA-32 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.136 μM 21448591
CHLA-56 Growth Inhibition Assay 10 μM 96 h DMSO IC50=10 μM 21448591
CHLA-258 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.132 μM 21448591
COG-E-352 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.043 μM 21448591
CHLA-90 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.061 μM 21448591
CHLA-119 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.022 μM 21448591
CHLA-122 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.019 μM 21448591
CHLA-136 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.039 μM 21448591
CHLA-140 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.026 μM 21448591
LA-N-6 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.054 μM 21448591
NB-1643 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.037 μM 21448591
NB-EBc1 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.050 μM 21448591
SK-N-BE-1 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.028 μM 21448591
SK-N-BE-2 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.036 μM 21448591
SMS-KAN Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.034 μM 21448591
SMS-KANR Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.026 μM 21448591
SMS-KCN Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.019 μM 21448591
SMS-KCNR Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.010 μM 21448591
SMS-LHN Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.032 μM 21448591
SMS-MSN Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.022 μM 21448591
SMS-SAN Growth Inhibition Assay 10 μM 96 h DMSO 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 DMSO IC50=0.13 μM 20382844
OPM1 Growth Inhibition Assay 4 μM 72 h DMSO IC50=0.03 μM 20382844
RPM1 Growth Inhibition Assay 4 μM 72 h DMSO IC50=10.32 μM 20382844
INA6 Growth Inhibition Assay 4 μM 72 h DMSO IC50=0.002 μM 20382844
OPM2 Growth Inhibition Assay 4 μM 72 h DMSO IC50=4.37 μM 20382844
MM1R Growth Inhibition Assay 4 μM 72 h DMSO IC50=1.68 μM 20382844
DOX40 Growth Inhibition Assay 4 μM 72 h DMSO IC50=5.48 μM 20382844
LR5 Growth Inhibition Assay 4 μM 72 h DMSO IC50=2.53 μM 20382844
U266 Growth Inhibition Assay 4 μM 72 h DMSO 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
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
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
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
multiple myeloma Function assay Suppression of cell mitosis in human multiple myeloma cells, IC50 = 0.003 μM. 28918096
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
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
Click to View More Cell Line Experimental Data

Biological Activity

Description Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Features First orally available inhibitor of Aurora A.
Targets
Aurora A [1]
(Cell-free assay)
1.2 nM
In vitro
In vitro

MLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases. [1] MLN8237 (0.5 μM) treatment inhibits the phosphorylation of Aurora A in MM1.S and OPM1 cells, without affecting the Aurora B mediated histone H3 phosphorylation. MLN8237 significantly inhibits cell proliferation in multiple myeloma (MM) cell lines with IC50 values of 0.003-1.71 μM. MLN8237 displays more potent anti-proliferation activity against primary MM cells and MM cell lines in the presence of BM stroma cells, as well as IL-6 and IGF-1 than against MM cells alone. MLN8237 (0.5 μM) induces 2- to 6-fold increase in G2/M phase in primary MM cells and cell lines, as well as significant apoptosis and senescence, involving the up-regulation of p53, p21 and p27, as well as PARP, caspase 3, and caspase 9 cleavage. In addition, MLN8237 shows strong synergistic anti-MM effect with Hexadecadrol, as well as additive effect with doxorubicin and LDP-341. [2] MLN8237 (0.5 μM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage of polyploid cells, and subsequently an increase in the percentage of cells in the sub-G1 phase, which can be further enhanced in combination with NSC 119875(2.5 μM), involving the higher induction of TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP as compared with a single-agent treatment. [3]
Kinase Assay Aurora A radioactive Flashplate enzyme assay
Aurora A radioactive Flashplate enzyme assay is conducted to determine the nature and degree of MLN8237-mediated inhibition in vitro. Recombinant Aurora A is expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A is conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) is assayed in 50 mM Hepes (pH 7.5), 10 mM MgCl2, 5 mM DTT, 0.05% Tween 20, 2 μM peptide substrate, 3.3 μCi/mL [γ-33P]ATP at 2 μM, and increasing concentrations of MLN8237 by using Image FlashPlates.
Cell Research Cell lines MM1.S, MM.1R, LR5, RPMI 8226, DOX40, OPM1, OPM2, INA6, and U266
Concentrations Dissolved in DMSO, final concentrations ~10 μM
Incubation Time 24, 48, and 72 hours
Method

Cells are exposed to various concentrations of MLN8237 for 24, 48, and 72 hours. Cells viability is measured using MTT assay, and cell proliferation is measured using 3[H]-thymidine incorporation. For cell cycle analysis, cells are permeabilized by 70% ethanol at -20 °C, and incubated with 50 μg/mL PI and 20 units/mL RNase-A. DNA content is analyzed by flow cytometry using BDFACS-Canto II and FlowJo software. For the detection of apoptosis and senescence, cells are stained with Resorcinolphthalein isothiocyanate-annexin V and PI. Apoptotic cells are determined by flow cytometric analysis using BDFACS-Canto II and FlowJo software.
Experimental Result Images Methods Biomarkers Images 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
In Vivo
In vivo

MLN8237 significantly reduces the tumor burden with tumor growth inhibition (TGI) of 42% and 80% at 15 mg/kg and 30 mg/kg, respectively, and prolongs the survival of mice compared with the control. [2]
Animal Research Animal Models Severe combined immune-deficient (SCID) mice inoculated subcutaneously with MM1.S cells
Dosages ~30 mg/kg/day
Administration Orally
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

Chemical Information & Solubility

Molecular Weight 518.92 Formula

C27H20ClFN4O4
CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (96.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
What is the suggested formulation of this compound for mouse injection(i.p.)?

Answer:
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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