Alisertib (MLN8237)

For research use only.

Catalog No.S1133

224 publications

Alisertib (MLN8237) Chemical Structure

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. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.

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Selleck's Alisertib (MLN8237) has been cited by 224 publications

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Choose Selective Aurora Kinase Inhibitors

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

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 Mor0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjjZ3UxNjVizszN NWrtZ5ZrPzJiaB?= MUPEUXNQ M3rjTmlEPTB;MD6wOEDPxE1? M{nNflI3OTN4Nki0
LS174T MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[0NG8xNjVizszN NYHqdo1GPzJiaB?= MoTySG1UVw>? MUnJR|UxRTBwMEWg{txO M4e1blI3OTN4Nki0
T84 M3vUemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPZS2hGOC53IN88US=> NFT0N4E4OiCq MYLEUXNQ NXjhTnNyUUN3ME2wMlA6KM7:TR?= NW\rSFk2OjZzM{[2PFQ>
LS180 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\mXlAvPSEQvF2= MoHuO|IhcA>? NWfnV4hQTE2VTx?= M1juRWlEPTB;MTFOwG0> M2nLSFI3OTN4Nki0
SW948 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTZNE42KM7:TR?= MnX6O|IhcA>? NH\2e4ZFVVOR NXG5RnU3UUN3ME2xJO69VQ>? MnS4NlYyOzZ4OES=
HCT15 M{PEbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn0NYlrOC53IN88US=> NWO4NWREPzJiaB?= MV7EUXNQ M4\ZemlEPTB:MD60JO69VQ>? NEXMWWYzPjF|Nk[4OC=>
DLD-1 NVLSNoFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCwMlUh|ryP MVe3NkBp NXn1[GJYTE2VTx?= NGnPeJFKSzVyPECuPEDPxE1? Mk\INlYyOzZ4OES=
MIP-101 Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zTR|AvPSEQvF2= Mm[5O|IhcA>? NHrxNGhFVVOR NEDDTGRKSzVyPUGg{txO NEWxZmMzPjF|Nk[4OC=>
SNU1544 NILVXJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\KNE42KM7:TR?= MXi3NkBp NHe3R4JFVVOR M12xRWlEPTB;MTFOwG0> MVmyOlE{PjZ6NB?=
OCI-Ly10 NYW2V4J{S3m2b4TvfIlkKEG|c3H5 NHnVTGs4OiCq MVzEUXNQ NWDSZXFLUUN3ME2wMlA2QCEQvF2= M4LwRlI2QDd6M{Ox
SU-DHL2 NHTCOHZEgXSxdH;4bYMhSXO|YYm= NVTGOHJ2PzJiaB?= NIDZe3ZFVVOR M133VGlEPTB;MD6wNUDPxE1? NYWwSI5QOjV6N{izN|E>
OCI-LY7 NY\ZNWxUS3m2b4TvfIlkKEG|c3H5 NF3VSII4OiCq NU\OcGdQTE2VTx?= NHzoc2JKSzVyPUCuNFgyKM7:TR?= NFnFc5kzPTh5OEOzNS=>
SU-DHL6 MnvjR5l1d3SxeHnjJGF{e2G7 NGfKZ3I4OiCq MXfEUXNQ Ml;zTWM2OD1yLkS4NkDPxE1? MlTuNlU5Pzh|M{G=
Jeko-1 Mo\4R5l1d3SxeHnjJGF{e2G7 NGnzUpE4OiCq NYLQ[2xnTE2VTx?= NFrrdYlKSzVyPUCuNFI6KM7:TR?= MkK2NlU5Pzh|M{G=
JVM-2 M3XydmN6fG:2b4jpZ{BCe3OjeR?= M1\Ic|czKGh? M2fDRWROW09? MnjyTWM2OD1yLkCxJO69VQ>? NIr4XYszPTh5OEOzNS=>
Rec-1 MYHDfZRwfG:6aXOgRZN{[Xl? NX3WdoE4PzJiaB?= MmSySG1UVw>? Ml;ITWM2OD1yLkC4O{DPxE1? M{\xPVI2QDd6M{Ox
Z-138 MWfDfZRwfG:6aXOgRZN{[Xl? MlLVO|IhcA>? NEO2RmRFVVOR MXLJR|UxRTBwMEGzJO69VQ>? NVrwT2Z7OjV6N{izN|E>
H9 NVPLephoS3m2b4TvfIlkKEG|c3H5 NULzV2R1PzJiaB?= NH3kTWpFVVOR MmPrTWM2OD1yLk[g{txO NVnqdlZqOjV6N{izN|E>
HH NVztWnRYS3m2b4TvfIlkKEG|c3H5 NXTYUGVsPzJiaB?= M3iw[mROW09? MV3JR|UxRTBwNzFOwG0> NV:2OGhDOjV6N{izN|E>
DND41 M4Oxd2N6fG:2b4jpZ{BCe3OjeR?= MVS3NkBp Mn7GSG1UVw>? MXnJR|UxRTBwMTFOwG0> MVWyOVg4QDN|MR?=
CCL119 MlSxR5l1d3SxeHnjJGF{e2G7 NUnsdJRXPzJiaB?= MV\EUXNQ M4[zVmlEPTB;MD6wOlIh|ryP MkDSNlU5Pzh|M{G=
J.Cam 1.6 NUj4[YlrS3m2b4TvfIlkKEG|c3H5 MXe3NkBp MX;EUXNQ NF3xfGVKSzVyPUCuNVA2KM7:TR?= Mm[3NlU5Pzh|M{G=
Sup-T1 Mle4R5l1d3SxeHnjJGF{e2G7 NVzi[3N6PzJiaB?= MXvEUXNQ Mn\VTWM2OD1{LkG0NkDPxE1? MU[yOVg4QDN|MR?=
Tib 152 NFPPfmJEgXSxdH;4bYMhSXO|YYm= NX;JNZVTPzJiaB?= MoTNSG1UVw>? NHG4eYtKSzVyPUCuPEDPxE1? M{\ZdVI2QDd6M{Ox
MCF7 NVrncGNnTnWwY4Tpc44hSXO|YYm= MYO1JO69VQ>? NVu5TFdxOjRiaB?= M1rqRmROW09? MYHJcoR2[2W|IFeyM20h[XK{ZYP0 MnLNNlU5OzR2MEG=
MDA-MB-231 MYfGeY5kfGmxbjDBd5NigQ>? M4LIUlUh|ryP NHKwO4ozPCCq NFzwb3VFVVOR NYDTTXJtUW6mdXPld{BIOy:PIHHydoV{fA>? NYXDXJV6OjV6M{S0NFE>
MCF7 NVrRempCTnWwY4Tpc44hSXO|YYm= NGq5Smk2KM7:TR?= NXS3OGo{OjRiaB?= NGLSfotFVVOR NEHB[XFF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy MUeyOVg{PDRyMR?=
MCF7 MkniSpVv[3Srb36gRZN{[Xl? NVjLUHFZPSEQvF2= MX2yOEBp Ml;XSG1UVw>? MV;E[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=> NHnWRWEzPTh|NESwNS=>
MCF7 MXXGeY5kfGmxbjDBd5NigQ>? Mn\JOUDPxE1? MUKyOEBp M{SzN2ROW09? NX;2cYhDTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> NVztRZRlOjV6M{S0NFE>
MCF7 NY\xWFBXTnWwY4Tpc44hSXO|YYm= MX21JO69VQ>? NGjX[VMzPCCq M1H4[GROW09? MlTXTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> M{D2VlI2QDN2NECx
MCF7 Mmr3SpVv[3Srb36gRZN{[Xl? Mk\jOUDPxE1? NEC4SIczPCCq MkG3SG1UVw>? M3THdGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= MYWyOVg{PDRyMR?=
MDA-MB-231 NGizUm5HfW6ldHnvckBCe3OjeR?= MoXvOUDPxE1? NXTsXJNMOjRiaB?= M4jsV2ROW09? NX7mfWRFTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzFxQ1TDNi=> MYqyOVg{PDRyMR?=
MDA-MB-231 MWPGeY5kfGmxbjDBd5NigQ>? NILYOIEyKM7:TR?= NUHjWHhIOjRiaB?= NGPMNoVFVVOR NHPC[5ZKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NIrjU5MzPTh|NESwNS=>
MDA-MB-231 NF:2fXhHfW6ldHnvckBCe3OjeR?= MYe1JO69VQ>? NIPYVYYzPCCq M3qxdWROW09? M2fRfmRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= M3LEW|I2QDN2NECx
MDA-MB-231 NW\ib|dXTnWwY4Tpc44hSXO|YYm= NUTkXlhNPSEQvF2= Mn7TNlQhcA>? NELQSFRFVVOR MoXqTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> NE\l[W0zPTh|NESwNS=>
MDA-MB-231 MV7GeY5kfGmxbjDBd5NigQ>? M3XkSFUh|ryP MUOyOEBp MoDuSG1UVw>? MkW2TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz M{jZdFI2QDN2NECx
MDA-MB-231 NELl[npHfW6ldHnvckBCe3OjeR?= NInPT3I2KM7:TR?= MWOyOEBp MWLEUXNQ NFvy[YpKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFU{ NFvYTW0zPTh|NESwNS=>
MCF7 NFvhTY9CeG:ydH;zbZMhSXO|YYm= M{fFPFUh|ryP NVfqUFU6OjRiaB?= NYDRTllETE2VTx?= NYTuUlJyUW6mdXPld{BieG:ydH;0bYMh\GWjdHi= MlHvNlU5OzR2MEG=
MDA-MB-231 M4[0eGFxd3C2b4Ppd{BCe3OjeR?= MmDHOUDPxE1? MWOyOEBp NXjzVlc5TE2VTx?= NEPHWYRKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= NFPD[IgzPTh|NESwNS=>
MCF7 MlnRSpVv[3Srb36gRZN{[Xl? M1vkb|Eh|ryP MVi3NkBp Moj6SG1UVw>? MlXHTY5lfWOnczDheZRweGijZ3njJIRm[XSq MkjINlU5OzR2MEG=
MDA-MB-231 MVrGeY5kfGmxbjDBd5NigQ>? MVixJO69VQ>? MkT1O|IhcA>? NXXWelAyTE2VTx?= NV\1PGExUW6mdXPld{BifXSxcHjh[4lkKGSnYYTo MlTsNlU5OzR2MEG=
U-2 OS M2qyUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PqN|UxKM7:TR?= MXeyOEBp NFHub21FVVOR MmixTWM2OD1zNj62JO69VQ>? MmHyNlU4QTJ6MUG=
MG-63 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUS1NEDPxE1? M3nIVlI1KGh? NXrkW5hRTE2VTx?= MYnJR|UxRTlwNTFOwG0> Mlj1NlU4QTJ6MUG=
U-2 OS MVfBdI9xfG:|aYOgRZN{[Xl? Mm\XOUDPxE1? NHHSOW8zPCCq NEHwTWxFVVOR NFHKZZFKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp MVyyOVc6OjhzMR?=
MG-63 M4flfmFxd3C2b4Ppd{BCe3OjeR?= Mn23OUDPxE1? MoPYNlQhcA>? NHTqeGhFVVOR NXTaXFhJUW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>? MXGyOVc6OjhzMR?=
U-2 OS MWDGeY5kfGmxbjDBd5NigQ>? M3vwSFUh|ryP NVXZfVl1OjRiaB?= M{DLUWROW09? MUfQdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> MXmyOVc6OjhzMR?=
MG-63 NGjiZYJHfW6ldHnvckBCe3OjeR?= MlnnOUDPxE1? MVWyOEBp NF3HT2VFVVOR MV\Qdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> MmfjNlU4QTJ6MUG=
PANC-1 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYK1NEDPxE1? M4fyOlI1KGh? NFHVPXJFVVOR M3yyRmlEPTB;Nz6xJO69VQ>? M3nEOVI2PjN{MkK1
BxPC-3 MoPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfufGk2OCEQvF2= MYeyOEBp M{LnPWROW09? MXrJR|UxRTZwODFOwG0> MnvlNlU3OzJ{MkW=
PANC-1 M1TkVGZ2dmO2aX;uJGF{e2G7 Mme4OUDPxE1? M3vsc|I1KGh? MWTEUXNQ NWPMV4Z{UW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBqdiCJMj;NJJBp[XOn MVOyOVY{OjJ{NR?=
BxPC-3 Mnr5SpVv[3Srb36gRZN{[Xl? MmfhOUDPxE1? NYDSZXpLOjRiaB?= MVrEUXNQ MWnJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> M17wb|I2PjN{MkK1
PANC-1 NYLzWZVOTnWwY4Tpc44hSXO|YYm= MmDjOUDPxE1? NVz5bm4yOjRiaB?= MY\EUXNQ NFjyWpJKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? NXiycFFxOjV4M{KyNlU>
BxPC-3 NWfrcZBkTnWwY4Tpc44hSXO|YYm= NXPnWJVOPSEQvF2= M3HDb|I1KGh? MnTVSG1UVw>? NUnPTXhiUW6mdXPld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? NX3hN5BSOjV4M{KyNlU>
SKOV3 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPtVJdVOTByIN88US=> M1XNUlI1KGh? NWLUW4ZLTE2VTx?= NETEZ|JKSzVyPUKwMlQ5KM7:TR?= NH\JepkzPTZ{NEe1NC=>
OVCAR4 MofiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXCVW0yODBizszN MY[yOEBp M3\ZOmROW09? NIXTWWFKSzVyPUKyMlE{KM7:TR?= Moi4NlU3OjR5NUC=
SKOV3 NEG2R2hHfW6ldHnvckBCe3OjeR?= NY\3[25uPSEQvF2= M4XZWVczKGh? NYPBUXZzTE2VTx?= M4\Jb2lv\HWlZYOgS|IwVSCjcoLld5Q> NU\nc|QyOjV4MkS3OVA>
OVCAR4 MWHGeY5kfGmxbjDBd5NigQ>? M4LTRVUh|ryP MYe3NkBp NWTYfnF{TE2VTx?= NHHL[JNKdmS3Y3XzJGczN01iYYLy[ZN1 NX7hT4k4OjV4MkS3OVA>
SKOV3 MknhRZBweHSxc3nzJGF{e2G7 NGXOW5o2KM7:TR?= M3;2TlI1KGh? NV;jbYs1TE2VTx?= MVTJcoR2[2W|IHHwc5B1d3Orcx?= MXmyOVYzPDd3MB?=
OVCAR4 NYT2T4t4SXCxcITvd4l{KEG|c3H5 MWq1JO69VQ>? MmnQNlQhcA>? NGLtdplFVVOR NV\GfYFTUW6mdXPld{BieG:ydH;zbZM> NGn2U28zPTZ{NEe1NC=>
AGS NUm3XFY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjQWYwzPSEQvF2= NWPWNYRqOjRiaB?= NH7zTnJFVVOR NWC3Z|RYUUN3ME2xPU4xQSEQvF2= M3zkZVI2PjB7OUKz
NCI-N78 NWracldLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr0NlUh|ryP NYfMeIp5OjRiaB?= NFH5OHlFVVOR MUXJR|UxRTJ4LkOzJO69VQ>? M1;SeFI2PjB7OUKz
AGS Mnz2RZBweHSxc3nzJGF{e2G7 M1rmO|Uh|ryP MWWyOEBp M4\ObmROW09? NU\v[VZZUW6mdXPld{BieG:ydH;zbZM> MU[yOVYxQTl{Mx?=
NCI-N78 M1[yWWFxd3C2b4Ppd{BCe3OjeR?= NVXRd3poPSEQvF2= NGDnS5MzPCCq NYLUcnhZTE2VTx?= MV\JcoR2[2W|IHHwc5B1d3Orcx?= NIWwdFUzPTZyOUmyNy=>
AGS NGO4UmZHfW6ldHnvckBCe3OjeR?= MYq1JO69VQ>? Mk[4NlQhcA>? NFP1WZlFVVOR NEDZUZdKdmS3Y3XzJJRp\SCjdYTvdIhi\3l? M4LpSlI2PjB7OUKz
NCI-N78 M{\XV2Z2dmO2aX;uJGF{e2G7 M4eycVUh|ryP NU\JPIZUOjRiaB?= NEe3XWpFVVOR NE\VXlFKdmS3Y3XzJJRp\SCjdYTvdIhi\3l? M3Txc|I2PjB7OUKz
HSC-3 NFG3cmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTyWIlEOSEQvF2= NEG3[5Y1QCCq MVXJR|UxRTBwNUSg{txO NIe2boEzPTN4NkG0Ny=>
GB30 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWxJO69VQ>? NXfldJlRPyCm MVXEUXNQ Mmi2TWM2OD1yLkCxNUDPxE1? MlXtNlUyODZ2Mki=
GB9 NFruc2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTuXZY2OSEQvF2= NIHZPIg4KGR? Ml;PSG1UVw>? M2G2d2lEPTB;MD6wNlQh|ryP MVuyOVExPjR{OB?=
GB169 MoTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;ZZpJYOSEQvF2= M2fDWVch\A>? NX;uRpBrTE2VTx?= NV\lVlI2UUN3ME2wMlA{OiEQvF2= M{L3fVI2OTB4NEK4
T24 NE\t[plHfW6ldHnvckBCe3OjeR?= NXi4U5JROSEQvF2= NHHxfWk1QCCq NIDpR|dFVVOR MkPLTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MneyNlM1ODN4M{O=
RT4 MWDGeY5kfGmxbjDBd5NigQ>? MUmxJO69VQ>? NYXUcFAxPDhiaB?= Mk\5SG1UVw>? MoK2TY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MYmyN|QxOzZ|Mx?=
UM-UC-3 M1fkbmZ2dmO2aX;uJGF{e2G7 NFjVdHgyKM7:TR?= M2fh[|Q5KGh? MkDUSG1UVw>? MYjJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NV7pXpVSOjN2MEO2N|M>
T24 MkD3RZBweHSxc3nzJGF{e2G7 M{LMNFMvOTZizszN M3Xm[Vk3KGh? M2DvZmROW09? M3rvO2lEPTB;MD6wN|A3KM7:TR?= MWOyN|QxOzZ|Mx?=
RT4 NGWxN49CeG:ydH;zbZMhSXO|YYm= NHLtVIg{NjF4IN88US=> NWW5W2ZUQTZiaB?= NYXSbllvTE2VTx?= NUfKTmV2UUN3ME2wMlEyQThizszN NVPDT4RtOjN2MEO2N|M>
UM-UC-3 M3ruT2Fxd3C2b4Ppd{BCe3OjeR?= NWW1RXBwOy5zNjFOwG0> M{DLPFk3KGh? MYXEUXNQ MYjJR|UxRTBwMES0PUDPxE1? NFraSogzOzRyM{[zNy=>
OVCAR-5 MWnGeY5kfGmxbjDBd5NigQ>? NVja[25QPTBibl2= MYDJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NX;PbmJCOjN|M{SzNlc>
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RS4-11 Ml7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjiUHIyOCEQvF2= MX25OkBp NIHxOlBKSzVyPUCuNFE5KM7:TR?= NVnOW|liOjBzMEizN|g>
MOLT-4 MlL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\3NVAh|ryP NHf0N2Y6PiCq NWq1blFxUUN3ME2wMlAzPiEQvF2= M3HFZ|IxOTB6M{O4
CCRF-CEM MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTr[nQyOCEQvF2= M4r2clk3KGh? NHHTe5dKSzVyPUCuNFk1KM7:TR?= NF[zSHczODFyOEOzPC=>
Kasumi-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fDbFExKM7:TR?= NV30bXl{QTZiaB?= NF;6[GdKSzVyPUCuNVA{KM7:TR?= MmnxNlAyODh|M{i=
Karpas-299 NUm4OIJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPtNVAh|ryP MXq5OkBp NXHrTJZiUUN3ME2wMlA{QCEQvF2= MUGyNFExQDN|OB?=
Ramos-RA1 MnHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f5fVExKM7:TR?= NHHSRoI6PiCq M13vdmlEPTB;MD6xNlch|ryP MYCyNFExQDN|OB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AURKA(T288) / p-EIF4E(S209) / c-Myc; 

PubMed: 28073841     


Inhibition of AURKA with alisertib downregulated p-EIF4E (S209) and c-MYC protein levels as assayed by Western blotting.

phospho-Aurora A / Aurora B; 

PubMed: 22863010     


MLN8237differentially inhibited phosphorylation of Aurora kinases. CMK cells were incubated with 0.1 µM paclitaxel for 18 hr, then DMSO or MLN8237 was added and incubated for 2 hr. The degree of phosphorylation of the Aurora kinases in each sample was determined by Western blot.

H3S10P / H3K27me2 / H3K27me3 / H3K9me2 / H3AcK / H4K16Ac; 

PubMed: 29477140     


THP-1 cells were treated with alisertib or DMSO for 48 h. The levels of histone modifications were detected by western blot analysis with the indicated antibodies. H3 was used as a loading control.

28073841 22863010 29477140
Growth inhibition assay
Cell viability; 

PubMed: 25632225     


PANC-1 and BxPC-3 cells were treated with ALS at concentrations ranging from 0.1 μM to 50 μM for 24 hours. The viability of PANC-1 and BxPC-3 cells determined by MTT assay. ALS, alisertib.

25632225
Immunofluorescence
acetylated α-tubulin / γ-tubulin; 

PubMed: 29401581     


Representative immunofluorescence (IF) image and graph in human PKD1-mutant WT9-7, WT9-12 cells or hTERT-RPE1 (RPE1) cells after 2 hours treatment with vehicle, ganetespib , or alisertib to inhibit AURKA, or combination of alisertib and ganetespib. acetylated α-tubulin (red); γ-tubulin (green); DAPI (blue). Scale bars, 5 μm.

E-cadherin / β-catenin / vimentin / p-SMAD5; 

PubMed: 23334326     


Immunofluorescence analysis of CD24 (-/low) cells treated with1 μM MLN8237 for 48 and 72 h showing reversion of EMT. E-cadherin and p-SMAD5 were labeled in red, β-catenin and vimentin were labeled in green, and DNA was labeled in blue with Hoechst dye.

Centrin-2 / tubulin; 

PubMed: 30899434     


Following inhibition of Aurora A kinase activity with 100 nM alisertib, cells with two or excess centrosomes similarly exhibit disorganized mitotic spindles. Cells with extra centrosomes are efficiently clustered into bipolar spindles prior to anaphase onset while those with supernumerary centrosomes undergo multipolar mitoses. Centrin-2, a marker of centrioles is shown in green, tubulin in red, and chromatin in blue. AurA inhibitor: alisertib.

phospho-Aurora A(T288); 

PubMed: 20382844     


MM1.S cells were treated with DMSO or MLN8237 (0.5μM) for 24 hours and then stained with anti-phospho (Thr288)-Aurora-A kinase antibody (red), αtubulin (green), and DNA (blue). Overlapping localization is shown in the merged images. Arrow indicates Aurora-A autophosphorylation on Thr288 in the centrosome (original magnification ×40). Magnified single mitotic cell image is shown in the right panel. 

29401581 23334326 30899434 20382844
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]

Protocol

Kinase Assay:[1]
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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:[2]
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  • 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 fluorescein isothiocyanate-annexin V and PI. Apoptotic cells are determined by flow cytometric analysis using BDFACS-Canto II and FlowJo software.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Severe combined immune-deficient (SCID) mice inoculated subcutaneously with MM1.S cells
  • Dosages: ~30 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 27 mg/mL (52.03 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+30% PEG300+5%Tween-80+ddH2O
For best results, use promptly after mixing.
8mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 518.92
Formula

C27H20ClFN4O4

CAS No. 1028486-01-2
Storage powder
in solvent
Synonyms N/A
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04479306 Recruiting Drug: Alisertib|Drug: Osimertinib|Drug: Sapanisertib EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma|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|National Cancer Institute (NCI) June 18 2020 Phase 1
NCT02812056 Withdrawn Drug: Alisertib|Drug: TAK-228 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 Recruiting Drug: Alisertib|Drug: MLN0128 Metastatic Breast Cancer|Solid Tumors University of Colorado Denver May 13 2016 Phase 1
NCT02367352 Terminated Drug: Alisertib|Drug: Paclitaxel Advanced Solid Tumors|Ovarian Cancer|Small Cell Lung Cancer Millennium Pharmaceuticals Inc.|Takeda March 19 2015 Phase 1

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

Aurora Kinase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID