Welcome to SuperLan Chemical Co.,Ltd.
Home > Products > Cell Cycle > Aurora Kinase > MLN-8237

MLN-8237

(CAS No:1028486-01-2)
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. Phase 3.
CAS No:1028486-01-2
Molecular Weight(MW):518.92
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
Price and large packaging, please e-mail consultation:info@SuperLan-chem.com
QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 1028486-01-2
Molecular formula(MF) C27H20ClFN4O4
Molecular Weight(MW): 518.92
Alias 4-[[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid;MLN-8237;4-((9-chloro-7-(2-fluoro-6-Methoxyphenyl)-5H-benzo[c]pyriMido[4,5-e]azepin-2-yl)aMino)-2-Methoxybenzoic acid
Solubility
In vitro DMSO 27 mg/mL (52.03 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 15% Captisol 30 mg/mL
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. Phase 3.
Features First orally available inhibitor of Aurora A.
Targets
Aurora A [1]
(Cell-free assay)		 Aurora B [1]
(Cell-free assay)
1.2 nM 396.5 nM
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 dexamethasone, as well as additive effect with doxorubicin and bortezomib. [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 cisplatin (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]
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

... Click to View More Cell Line Experimental Data
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]
Copyright 2016 Shanghai Superlan Chemcial Technology Centre
Technical Support:chem960