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Alisertib (MLN8237)

中文名稱：阿利色替

Alisertib (MLN8237)是一種選擇性Aurora A抑制劑，無細胞試驗中IC50為1.2 nM，作用于Aurora A比作用于Aurora B選擇性強200倍以上。Alisertib 可誘導細胞周期阻滯、細胞凋亡與自噬。Phase 3。

Alisertib (MLN8237) Chemical Structure

Alisertib (MLN8237) Chemical Structure

CAS: 1028486-01-2

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1375.12 現(xiàn)貨
5mg 983.87 現(xiàn)貨
50mg 5505.84 現(xiàn)貨
200mg 14496.3 現(xiàn)貨
1g 40868.1 現(xiàn)貨
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常與Alisertib (MLN8237)一起在實驗中被使用的化合物

Barasertib (AZD1152-HQPA)

Alisertib和Barasertib強烈抑制急性髓細胞性白血病細胞的生長和增殖。

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

Volasertib

Alisertib和Volasertib抑制AURKA和PLK1，并協(xié)同阻斷彌漫性中線膠質(zhì)瘤細胞的細胞周期進展。

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

Lenvatinib

Alisertib和Lenvatinib顯著增強對裸鼠腫瘤生長的抑制并誘導細胞凋亡。

Hao J, et al. Biomed Res Int. 2021; 2021: 6613439.

Irinotecan

Alisertib和Irinotecan以及Temozolomide在MYCN非擴增腫瘤患者中顯示出抗腫瘤活性。

DuBois SG, et al.Clin Cancer Res. 2018 Dec 15;24(24):6142-6149.

Paclitaxel

Alisertib和Paclitaxel在三陰性乳腺癌異種移植模型中具有相加和協(xié)同的抗腫瘤作用。

Falchook G, et al. JAMA Oncol. 2019 Jan; 5(1): e183773.

Alisertib (MLN8237)相關(guān)產(chǎn)品

相關(guān)信號通路圖

Aurora Kinase Signaling Pathways

Aurora Kinase信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Alisertib (MLN8237)是一種選擇性Aurora A抑制劑，無細胞試驗中IC50為1.2 nM，作用于Aurora A比作用于Aurora B選擇性強200倍以上。Alisertib 可誘導細胞周期阻滯、細胞凋亡與自噬。Phase 3。
特性 MLN8237 是第一個口服有效的小分子Aurora A激酶選擇性抑制劑。
靶點
Aurora A [1]
(Cell-free assay)
1.2 nM
體外研究(In Vitro)
體外研究活性

MLN8237作用于Aurora A選擇性比作用于結(jié)構(gòu)相關(guān)的Aurora B 高200多倍，IC50為396.5 nM, 而對205種其他激酶則沒有顯著活性。[1] 0.5 μM MLN8237處理MM1.S和 OPM1 細胞，抑制 Aurora A磷酸化，而不影響 Aurora B調(diào)節(jié)的組蛋白H3磷酸化。MLN8237作用于多發(fā)性骨髓瘤(MM) 細胞系，顯著抑制細胞增殖，IC50為0.003-1.71 μM。在BM 基質(zhì)細胞，IL-6和 IGF-1 存在時，MLN8237作用于原代MM 細胞和MM細胞系，抗增殖活性比只有MLN8237單獨作用時高很多。0.5 μM MLN8237 作用于原代MM細胞和細胞系，使G2/M 期細胞提高2到6倍，且顯著誘導凋亡和衰老，涉及p53, p21 和p27的上調(diào),及 PARP,caspase 3,和 caspase 9的裂解。此外, MLN8237和 Hexadecadrol聯(lián)用具有協(xié)同作用，具有強抗MM 功效, 而和Doxorubicin 及LDP-341聯(lián)用則具有另外的功能。[2] 0.5 μM MLN8237處理 FLO-1, OE19, 和OE33 食管腺癌細胞系，抑制集落形成，且顯著提高多倍體細胞百分數(shù),隨后提高G1期細胞百分數(shù),而與 NSC 119875(2.5 μM)聯(lián)用則效果進一步提高，與單獨用藥相比，誘導產(chǎn)生更多, TAp73β, PUMA, NOXA, cleaved caspase-3, 和cleaved PARP。[3]
激酶實驗 Aurora A放射性閃光板酶實驗
進行Aurora A放射性閃光板酶實驗，測定體外MLN8237抑制程度。在Sf9細胞中表達重組Aurora A，然后使用GST親和層析進行純化。Aurora A 肽底物與生物素聯(lián)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, 和濃度不斷增高的MLN8237 的混合物中進行Aurora A激酶 (5 nM)實驗。
細胞實驗 細胞系 MM1.S, MM.1R, LR5, RPMI 8226, DOX40, OPM1, OPM2, INA6, 和U266
濃度 溶于DMSO,終濃度為~10 μM
孵育時間 24, 48, 和72小時
方法

使用不同濃度MLN8237處理細胞24, 48,和72小時。通過MTT實驗測定細胞活力，通過測定 3[3H]-胸甘滲透而測定細胞增殖。為了分析細胞周期，使用70%乙醇在-20oC下使細胞通透，然后與50 μg/mL PI 和20 單位/mL RNase-A溫育。 通過流式細胞儀使用 BDFACS-Canto II和FlowJo軟件分析DNA含量。 為了測定凋亡和衰老，使用異硫氰酸熒光素-annexin V和PI對細胞進行染色。通過流式細胞儀使用 BDFACS-Canto II和FlowJo軟件測定凋亡細胞。
實驗圖片 檢測方法 檢測指標 實驗圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

MLN8237口服處理，顯著降低腫瘤負擔，按15 mg/kg 和30 mg/kg劑量處理腫瘤生長抑制率(TGI) 分別為42%和80%,且與對照組相比，延遲小鼠壽命。[2] MLN8237 (30 mg/kg) 與NSC 119875(2 mg/kg) 聯(lián)用作用于FLO-1移植瘤，與單獨用藥相比，抗癌活性增強，伴隨著Ki-67表達受抑制，細胞核p73蛋白和cleaved caspase 3表達增強。[3]
動物實驗 Animal Models 皮下接種 MM1.S 細胞的SCID鼠
Dosages ~30 mg/kg/day
Administration 口服處理
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

化學信息&溶解度

分子量 518.92 分子式

C27H20ClFN4O4
CAS號 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
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 25 mg/mL ( (48.17 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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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