Alisertib (MLN8237)

Catalog No.S1133

Alisertib (MLN8237) Chemical Structure

Molecular Weight(MW): 518.92

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.

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Cited by 79 Publications

Purity & Quality Control

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. 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 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmwMlUh|ryP M4jPSVczKGh? Mn3QSG1UVw>? M1jz[mlEPTB;MD6wOEDPxE1? MlvCNlYyOzZ4OES=
LS174T MnHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2wMlUh|ryP M3XRN|czKGh? MljlSG1UVw>? NEjlcZlKSzVyPUCuNFUh|ryP M3fuOVI3OTN4Nki0
T84 MmfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlUh|ryP NGm0PZo4OiCq Mn61SG1UVw>? M37BUGlEPTB;MD6wPUDPxE1? NFr2fnozPjF|Nk[4OC=>
LS180 M4Xjc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:3XG4xNjVizszN NV:0bHVNPzJiaB?= MU\EUXNQ Mn:yTWM2OD1zIN88US=> M3LCdlI3OTN4Nki0
SW948 NVyxZ2NYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{e5NVAvPSEQvF2= MnXaO|IhcA>? M3frdWROW09? MXXJR|UxRTFizszN MYeyOlE{PjZ6NB?=
HCT15 NHLrTWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnqVIZFOC53IN88US=> MVW3NkBp NXq5e21RTE2VTx?= MnjxTWM2ODxyLkSg{txO NG[1cVAzPjF|Nk[4OC=>
DLD-1 NYTSd2ZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrkNE42KM7:TR?= MkTHO|IhcA>? MYPEUXNQ MlLaTWM2ODxyLkig{txO MYqyOlE{PjZ6NB?=
MIP-101 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjtNIQxNjVizszN M4PWWFczKGh? M2XGZWROW09? MULJR|UxRTFizszN MnLSNlYyOzZ4OES=
SNU1544 NF\OTnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2wMlUh|ryP NW\LSpA5PzJiaB?= NXPkWpl2TE2VTx?= MUPJR|UxRTFizszN MlezNlYyOzZ4OES=
OCI-Ly10 NVjOWHBvS3m2b4TvfIlkKEG|c3H5 Mk\tO|IhcA>? MXnEUXNQ MWjJR|UxRTBwMEW4JO69VQ>? NFHQe3MzPTh5OEOzNS=>
SU-DHL2 MnzCR5l1d3SxeHnjJGF{e2G7 NX;XfpB3PzJiaB?= M4qyNGROW09? MWTJR|UxRTBwMEGg{txO NWHNbpoyOjV6N{izN|E>
OCI-LY7 NYjUNZY5S3m2b4TvfIlkKEG|c3H5 NHW1XWI4OiCq M1ezNWROW09? NUPZfJpLUUN3ME2wMlA5OSEQvF2= NFXlTFAzPTh5OEOzNS=>
SU-DHL6 MXXDfZRwfG:6aXOgRZN{[Xl? MUS3NkBp MV7EUXNQ NXvuS4o4UUN3ME2wMlQ5OiEQvF2= MWOyOVg4QDN|MR?=
Jeko-1 M1zvdGN6fG:2b4jpZ{BCe3OjeR?= NGi5NY44OiCq NYHoNo9VTE2VTx?= NETOPHBKSzVyPUCuNFI6KM7:TR?= NHLKdZEzPTh5OEOzNS=>
JVM-2 MlLqR5l1d3SxeHnjJGF{e2G7 M{jVTFczKGh? NIf0T|NFVVOR MYHJR|UxRTBwMEGg{txO MXqyOVg4QDN|MR?=
Rec-1 MVnDfZRwfG:6aXOgRZN{[Xl? MmnWO|IhcA>? MXHEUXNQ NU[1em42UUN3ME2wMlA5PyEQvF2= NIn6[nozPTh5OEOzNS=>
Z-138 Mn7QR5l1d3SxeHnjJGF{e2G7 NH3pbJQ4OiCq NEPDN25FVVOR MVTJR|UxRTBwMEGzJO69VQ>? M4PPe|I2QDd6M{Ox
H9 M1TJeGN6fG:2b4jpZ{BCe3OjeR?= MYS3NkBp Mk\USG1UVw>? NVPNflBlUUN3ME2wMlYh|ryP NGfUT|gzPTh5OEOzNS=>
HH MoWwR5l1d3SxeHnjJGF{e2G7 MmW0O|IhcA>? NILTUYlFVVOR MkjqTWM2OD1yLkeg{txO NEXFO3MzPTh5OEOzNS=>
DND41 NEjUdoxEgXSxdH;4bYMhSXO|YYm= NIrUdJM4OiCq M4LVTWROW09? NVPmTlI4UUN3ME2wMlEh|ryP M1z0VFI2QDd6M{Ox
CCL119 NH;YbI1EgXSxdH;4bYMhSXO|YYm= NUDiRlJ4PzJiaB?= MVvEUXNQ NX3GbWRRUUN3ME2wMlA3OiEQvF2= MkjBNlU5Pzh|M{G=
J.Cam 1.6 NH:xN5dEgXSxdH;4bYMhSXO|YYm= Mm\QO|IhcA>? MmS2SG1UVw>? NWTnRolbUUN3ME2wMlExPSEQvF2= M{TZTFI2QDd6M{Ox
Sup-T1 M1HxWGN6fG:2b4jpZ{BCe3OjeR?= NHq2TVA4OiCq MU\EUXNQ MVjJR|UxRTJwMUSyJO69VQ>? NGjESZIzPTh5OEOzNS=>
Tib 152 MoPYR5l1d3SxeHnjJGF{e2G7 NHu1eo84OiCq M36yXmROW09? MoTFTWM2OD1yLkig{txO M4fFRlI2QDd6M{Ox
MCF7 NWmwUGZ4TnWwY4Tpc44hSXO|YYm= M1vFWlUh|ryP MnuxNlQhcA>? MXXEUXNQ MoTmTY5lfWOnczDHNk9OKGG{cnXzeC=> NGjDT40zPTh|NESwNS=>
MDA-MB-231 MV7GeY5kfGmxbjDBd5NigQ>? MW[1JO69VQ>? NW\FUplmOjRiaB?= NYL0OZM2TE2VTx?= NFKxRpNKdmS3Y3XzJGc{N01iYYLy[ZN1 Mo\LNlU5OzR2MEG=
MCF7 MonwSpVv[3Srb36gRZN{[Xl? MnPlOUDPxE1? NF\WZpEzPCCq M2\JcGROW09? MYjE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ Mn\tNlU5OzR2MEG=
MCF7 MmHESpVv[3Srb36gRZN{[Xl? Mnj1OUDPxE1? MV6yOEBp M2fPfmROW09? NGrlbZlF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? M4PTeVI2QDN2NECx
MCF7 MmOzSpVv[3Srb36gRZN{[Xl? MWe1JO69VQ>? MmnmNlQhcA>? NWTjZVdTTE2VTx?= NWTrTJlbTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> NF6yWXozPTh|NESwNS=>
MCF7 NV;5V3k2TnWwY4Tpc44hSXO|YYm= NHTG[Ic2KM7:TR?= MXmyOEBp MXXEUXNQ NUHRTYJjUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? MWGyOVg{PDRyMR?=
MCF7 NEfuPIRHfW6ldHnvckBCe3OjeR?= MlTQOUDPxE1? M3XVOVI1KGh? M1m3cWROW09? MYjJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEK3JGtqeDF? Mn2xNlU5OzR2MEG=
MDA-MB-231 NHW3XI1HfW6ldHnvckBCe3OjeR?= NHzrUFg2KM7:TR?= M2i0ZVI1KGh? MYHEUXNQ NGKxUZZF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy M{mye|I2QDN2NECx
MDA-MB-231 NXHiWYE{TnWwY4Tpc44hSXO|YYm= NYq4VoU2OSEQvF2= M33IelI1KGh? MkjUSG1UVw>? M1i2SGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz M1GyZlI2QDN2NECx
MDA-MB-231 NXLSRVBITnWwY4Tpc44hSXO|YYm= MWe1JO69VQ>? M2H6[VI1KGh? M2DnZmROW09? NYf6cHZ[TGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> M2O4UlI2QDN2NECx
MDA-MB-231 NGTFdXlHfW6ldHnvckBCe3OjeR?= M4\mfFUh|ryP NG\kR3kzPCCq NEm3PXdFVVOR NWW0XoZKUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? NVzDdJFbOjV6M{S0NFE>
MDA-MB-231 MnTGSpVv[3Srb36gRZN{[Xl? MlnQOUDPxE1? NXXqdno1OjRiaB?= MYrEUXNQ Ml;hTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz NGLWO5IzPTh|NESwNS=>
MDA-MB-231 NWjJNnpRTnWwY4Tpc44hSXO|YYm= M4ruO|Uh|ryP NF3uVZozPCCq MnLaSG1UVw>? MoTQTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIIC1Ny=> NYj0U4hzOjV6M{S0NFE>
MCF7 MnP4RZBweHSxc3nzJGF{e2G7 M1L2bFUh|ryP M1zBfFI1KGh? MmTOSG1UVw>? NUfNbpNJUW6mdXPld{BieG:ydH;0bYMh\GWjdHi= M1vJUFI2QDN2NECx
MDA-MB-231 NUi5PJB4SXCxcITvd4l{KEG|c3H5 MWK1JO69VQ>? M4DnZVI1KGh? MX\EUXNQ NXHkTIJwUW6mdXPld{BieG:ydH;0bYMh\GWjdHi= MUCyOVg{PDRyMR?=
MCF7 M2j3b2Z2dmO2aX;uJGF{e2G7 NGHPd5gyKM7:TR?= NYT0OpdUPzJiaB?= NGXDS2FFVVOR MoizTY5lfWOnczDheZRweGijZ3njJIRm[XSq M3XlNFI2QDN2NECx
MDA-MB-231 M1jST2Z2dmO2aX;uJGF{e2G7 NFfI[4wyKM7:TR?= NGDmZYg4OiCq MlzqSG1UVw>? NW\pSW9kUW6mdXPld{BifXSxcHjh[4lkKGSnYYTo M{nURlI2QDN2NECx
U-2 OS MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUi1NEDPxE1? MkjGNlQhcA>? NIr6TINFVVOR MX;JR|UxRTF4Lk[g{txO Ml\TNlU4QTJ6MUG=
MG-63 NVi5OIlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlS2OVAh|ryP M2rFeVI1KGh? MX\EUXNQ MYLJR|UxRTlwNTFOwG0> MnjvNlU4QTJ6MUG=
U-2 OS MXvBdI9xfG:|aYOgRZN{[Xl? MYW1JO69VQ>? NXnJW4JUOjRiaB?= MXTEUXNQ NEjwVGJKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp NGe2W2wzPTd7MkixNS=>
MG-63 MXnBdI9xfG:|aYOgRZN{[Xl? MVm1JO69VQ>? NFfsfVUzPCCq NWm2NHc2TE2VTx?= NWjKZXBwUW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>? MnTINlU4QTJ6MUG=
U-2 OS MVrGeY5kfGmxbjDBd5NigQ>? MnzaOUDPxE1? MWKyOEBp MX7EUXNQ M2nYRXBzd22xdHXzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? M4PoXVI2Pzl{OEGx
MG-63 M4PHR2Z2dmO2aX;uJGF{e2G7 Mke2OUDPxE1? NUH3PFlmOjRiaB?= NVW0e|ZDTE2VTx?= M3;pbnBzd22xdHXzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? MYOyOVc6OjhzMR?=
PANC-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX61NEDPxE1? M4jJb|I1KGh? MUHEUXNQ NHfMWXNKSzVyPUeuNUDPxE1? NULCfnYxOjV4M{KyNlU>
BxPC-3 NYjxRldVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnrVZBFPTBizszN NX;rfoJxOjRiaB?= M3zqcGROW09? MUnJR|UxRTZwODFOwG0> NIDtWpozPTZ|MkKyOS=>
PANC-1 MYDGeY5kfGmxbjDBd5NigQ>? NH;IV4w2KM7:TR?= MknBNlQhcA>? MYjEUXNQ MnjCTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDpckBIOi:PIIDoZZNm M1WxTlI2PjN{MkK1
BxPC-3 NUi5NWJRTnWwY4Tpc44hSXO|YYm= MkixOUDPxE1? M{DkT|I1KGh? MVLEUXNQ MYDJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> M3WxdlI2PjN{MkK1
PANC-1 NWjQTnl4TnWwY4Tpc44hSXO|YYm= NFrMPGY2KM7:TR?= M1T4flI1KGh? NUnaZoVqTE2VTx?= NV6zeXlQUW6mdXPld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? MmSxNlU3OzJ{MkW=
BxPC-3 M3fOPGZ2dmO2aX;uJGF{e2G7 NWPLOpVtPSEQvF2= MYCyOEBp M2G4SmROW09? NHHKZYxKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? NYH2[INHOjV4M{KyNlU>
SKOV3 M3\1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWxNFAh|ryP MUeyOEBp NUW4SXk5TE2VTx?= NH;iTXlKSzVyPUKwMlQ5KM7:TR?= MlfDNlU3OjR5NUC=
OVCAR4 NE\J[YtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX6xNFAh|ryP M2PJelI1KGh? MWrEUXNQ NYj5UG5MUUN3ME2yNk4yOyEQvF2= NVywVph6OjV4MkS3OVA>
SKOV3 NVHK[GhJTnWwY4Tpc44hSXO|YYm= M3\3UFUh|ryP MkXmO|IhcA>? M1TRfGROW09? NETYc49KdmS3Y3XzJGczN01iYYLy[ZN1 NYO0TmdCOjV4MkS3OVA>
OVCAR4 M1fYb2Z2dmO2aX;uJGF{e2G7 NYrBZlJQPSEQvF2= MoHtO|IhcA>? NVPJelZNTE2VTx?= M3T1bWlv\HWlZYOgS|IwVSCjcoLld5Q> M2\BN|I2PjJ2N{Ww
SKOV3 MUHBdI9xfG:|aYOgRZN{[Xl? NY\HTWhRPSEQvF2= NGDjfFkzPCCq M37sOmROW09? M3fQS2lv\HWlZYOgZZBweHSxc3nz NELTeoQzPTZ{NEe1NC=>
OVCAR4 NVjJeXZMSXCxcITvd4l{KEG|c3H5 M{XHWVUh|ryP NXrTe4k4OjRiaB?= NYqybFhiTE2VTx?= MX;JcoR2[2W|IHHwc5B1d3Orcx?= NVO2RmM6OjV4MkS3OVA>
AGS NUHFVFJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:5NlUh|ryP MXqyOEBp MkHJSG1UVw>? MYLJR|UxRTF7LkC5JO69VQ>? MX[yOVYxQTl{Mx?=
NCI-N78 M4nIOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKyOUDPxE1? M1zvNFI1KGh? M170XmROW09? NWTneHdJUUN3ME2yOk4{OyEQvF2= MmC1NlU3ODl7MkO=
AGS NXO5VYJxSXCxcITvd4l{KEG|c3H5 NHPLXYo2KM7:TR?= MYCyOEBp MXLEUXNQ NETzUXdKdmS3Y3XzJIFxd3C2b4Ppdy=> NV3NNHhbOjV4MEm5NlM>
NCI-N78 MULBdI9xfG:|aYOgRZN{[Xl? NYf0SmdNPSEQvF2= MlywNlQhcA>? M3LC[mROW09? M1S2emlv\HWlZYOgZZBweHSxc3nz M4fEeVI2PjB7OUKz
AGS NW\0W21TTnWwY4Tpc44hSXO|YYm= NWjDTmdkPSEQvF2= MojnNlQhcA>? NYHxVVF7TE2VTx?= MUjJcoR2[2W|IITo[UBifXSxcHjh[5k> NI\BW5UzPTZyOUmyNy=>
NCI-N78 M1\3OWZ2dmO2aX;uJGF{e2G7 NUnOUmxTPSEQvF2= Ml:4NlQhcA>? M{noR2ROW09? NWTibXhqUW6mdXPld{B1cGViYYX0c5Bp[We7 NFnvOJgzPTZyOUmyNy=>
HSC-3 MnTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXH0VJB{OSEQvF2= NWTjeWtKPDhiaB?= NILofmNKSzVyPUCuOVQh|ryP M4\rdlI2OzZ4MUSz
GB30 NULGZmh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUixJO69VQ>? MYi3JIQ> NVXudGpETE2VTx?= MWPJR|UxRTBwMEGxJO69VQ>? Mo\GNlUyODZ2Mki=
GB9 NWDYRYd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjrZYwyKM7:TR?= NFnWXHU4KGR? MUPEUXNQ M3iyVmlEPTB;MD6wNlQh|ryP MYSyOVExPjR{OB?=
GB169 NFf1S3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFj1blEyKM7:TR?= MkLHO{Bl MkDiSG1UVw>? M2HGfmlEPTB;MD6wN|Ih|ryP MWmyOVExPjR{OB?=
T24 M3z6bmZ2dmO2aX;uJGF{e2G7 MnLZNUDPxE1? Mli1OFghcA>? NHTSepVFVVOR MUDJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NH3keVczOzRyM{[zNy=>
RT4 MlXDSpVv[3Srb36gRZN{[Xl? NXvOVYlVOSEQvF2= NFrPV2M1QCCq NG\COWdFVVOR NHW0VI5KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M4\hVFI{PDB|NkOz
UM-UC-3 NVjFO4RWTnWwY4Tpc44hSXO|YYm= NH3rbZkyKM7:TR?= MYC0PEBp NWTzZnFlTE2VTx?= NHvKU2pKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MVuyN|QxOzZ|Mx?=
T24 NGDPcVZCeG:ydH;zbZMhSXO|YYm= NHS4RpM{NjF4IN88US=> Mn[3PVYhcA>? NVjRTZdOTE2VTx?= M1rOT2lEPTB;MD6wN|A3KM7:TR?= M1LaPVI{PDB|NkOz
RT4 NHTic21CeG:ydH;zbZMhSXO|YYm= NX\KXVc1Oy5zNjFOwG0> Mn7xPVYhcA>? NEHFN|RFVVOR M1i5NWlEPTB;MD6xNVk5KM7:TR?= MmP2NlM1ODN4M{O=
UM-UC-3 NFLWWWZCeG:ydH;zbZMhSXO|YYm= MUWzMlE3KM7:TR?= M{T6eFk3KGh? MoG2SG1UVw>? MlfOTWM2OD1yLkC0OFkh|ryP NYXqU5dJOjN2MEO2N|M>
OVCAR-5 NHH3PVBHfW6ldHnvckBCe3OjeR?= MmnuOVAhdk1? NVnSNoZPUW6qaXLpeJMh[2WubDDtbYdz[XSrb36= MUSyN|M{PDN{Nx?=
SKOV3ip2 NYTJUnR7TnWwY4Tpc44hSXO|YYm= NYSxU4VQPTBibl2= MVPJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NXX0ToZmOjN|M{SzNlc>
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RS4-11 NVjMfGRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LjelExKM7:TR?= NGWyR3c6PiCq M2noPWlEPTB;MD6wNVgh|ryP M2fie|IxOTB6M{O4
MOLT-4 MlfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELHd|MyOCEQvF2= MWe5OkBp NX3scHd[UUN3ME2wMlAzPiEQvF2= M1rGd|IxOTB6M{O4
CCRF-CEM MlnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXSxNEDPxE1? NHr5R286PiCq NH\4c45KSzVyPUCuNFk1KM7:TR?= MnPINlAyODh|M{i=
Kasumi-1 NUO3fI5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLMNlcyOCEQvF2= MVK5OkBp MnnRTWM2OD1yLkGwN{DPxE1? M4rKU|IxOTB6M{O4
Karpas-299 NUD5RVlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\ad4JoOTBizszN NGHQUng6PiCq NYT5em1lUUN3ME2wMlA{QCEQvF2= NEe4UmgzODFyOEOzPC=>
Ramos-RA1 MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7aWoRrOTBizszN M4nkeVk3KGh? NG[wSGVKSzVyPUCuNVI4KM7:TR?= NH:wZWEzODFyOEOzPC=>

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Severe combined immune-deficient (SCID) mice inoculated subcutaneously with MM1.S cells
  • Formulation: Formulated in 10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate
  • 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

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)

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*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 )

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* 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

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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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

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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)
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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.

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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.

Aurora Kinase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID