Alisertib (MLN8237)

For research use only. Not for use in humans.

Catalog No.S1133

199 publications

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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Selleck's Alisertib (MLN8237) has been cited by 199 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 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4X0e|AvPSEQvF2= NVruW5NnPzJiaB?= MXfEUXNQ NW\PbZZLUUN3ME2wMlA1KM7:TR?= MkiyNlYyOzZ4OES=
LS174T NXfWVoYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV74d455OC53IN88US=> NXvuOoRMPzJiaB?= NGL2UFFFVVOR NXPjUXFvUUN3ME2wMlA2KM7:TR?= M{PrWVI3OTN4Nki0
T84 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXyNE42KM7:TR?= M4m4S|czKGh? MnLwSG1UVw>? NVrxSlA{UUN3ME2wMlA6KM7:TR?= M{m5UVI3OTN4Nki0
LS180 NV7qOHl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nMeFAvPSEQvF2= NH:1c5M4OiCq MXHEUXNQ NYXDb2s3UUN3ME2xJO69VQ>? NGn4eogzPjF|Nk[4OC=>
SW948 NUm2dZc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{W5NlAvPSEQvF2= M{nINlczKGh? NYDvbJhxTE2VTx?= MkW1TWM2OD1zIN88US=> Mo\BNlYyOzZ4OES=
HCT15 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[1NE42KM7:TR?= NIHWS5g4OiCq NWWxVG5yTE2VTx?= MlzkTWM2ODxyLkSg{txO M4HNSFI3OTN4Nki0
DLD-1 MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;qbFAvPSEQvF2= NWXFXZB2PzJiaB?= M1rQO2ROW09? M1XUb2lEPTB:MD64JO69VQ>? NFThW4szPjF|Nk[4OC=>
MIP-101 Mn\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PH[lAvPSEQvF2= NWqzXFRkPzJiaB?= NUH1NZd2TE2VTx?= MofxTWM2OD1zIN88US=> NGLwbIEzPjF|Nk[4OC=>
SNU1544 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofVNE42KM7:TR?= MmG4O|IhcA>? M4XNeGROW09? MkW4TWM2OD1zIN88US=> M4j0PVI3OTN4Nki0
OCI-Ly10 NFHsWmVEgXSxdH;4bYMhSXO|YYm= NITVZo84OiCq MWXEUXNQ MXHJR|UxRTBwMEW4JO69VQ>? NXrBe212OjV6N{izN|E>
SU-DHL2 NFLJN4REgXSxdH;4bYMhSXO|YYm= MmHVO|IhcA>? M{HIbGROW09? NY\FbZBrUUN3ME2wMlAyKM7:TR?= NYfIT5VXOjV6N{izN|E>
OCI-LY7 MVTDfZRwfG:6aXOgRZN{[Xl? MWq3NkBp NVnvTo9sTE2VTx?= NVLGWHF3UUN3ME2wMlA5OSEQvF2= MlWwNlU5Pzh|M{G=
SU-DHL6 NX\LOGNES3m2b4TvfIlkKEG|c3H5 Ml7jO|IhcA>? MW\EUXNQ MVXJR|UxRTBwNEiyJO69VQ>? MW[yOVg4QDN|MR?=
Jeko-1 NUXuVXFiS3m2b4TvfIlkKEG|c3H5 NXHxO2lqPzJiaB?= Mn3NSG1UVw>? MmXYTWM2OD1yLkCyPUDPxE1? NEfRb3AzPTh5OEOzNS=>
JVM-2 M1TINmN6fG:2b4jpZ{BCe3OjeR?= MnK0O|IhcA>? M{HIPGROW09? NInQTVNKSzVyPUCuNFEh|ryP NInhcXAzPTh5OEOzNS=>
Rec-1 NHzGd|lEgXSxdH;4bYMhSXO|YYm= MU[3NkBp M3rUV2ROW09? NH;YWXZKSzVyPUCuNFg4KM7:TR?= M362T|I2QDd6M{Ox
Z-138 MlSxR5l1d3SxeHnjJGF{e2G7 NVHLeZc2PzJiaB?= MknySG1UVw>? NWHRT257UUN3ME2wMlAyOyEQvF2= M1e4dFI2QDd6M{Ox
H9 MonSR5l1d3SxeHnjJGF{e2G7 NGr5Ro04OiCq M17JcmROW09? MUDJR|UxRTBwNjFOwG0> MYmyOVg4QDN|MR?=
HH MYPDfZRwfG:6aXOgRZN{[Xl? NVLjW3VDPzJiaB?= NYHnOYhFTE2VTx?= MXTJR|UxRTBwNzFOwG0> Ml;aNlU5Pzh|M{G=
DND41 NE\NXopEgXSxdH;4bYMhSXO|YYm= NFG4b2I4OiCq NG\EPFNFVVOR M4HueWlEPTB;MD6xJO69VQ>? NEXtVpozPTh5OEOzNS=>
CCL119 M{f6R2N6fG:2b4jpZ{BCe3OjeR?= M1jERlczKGh? MUnEUXNQ NY\zV|Z5UUN3ME2wMlA3OiEQvF2= NVXNcVJ7OjV6N{izN|E>
J.Cam 1.6 NF\qSVNEgXSxdH;4bYMhSXO|YYm= NVn1VIlUPzJiaB?= M{D5NmROW09? MmDhTWM2OD1yLkGwOUDPxE1? Mn;1NlU5Pzh|M{G=
Sup-T1 MlTiR5l1d3SxeHnjJGF{e2G7 MYi3NkBp NYHH[2FzTE2VTx?= M3jsS2lEPTB;Mj6xOFIh|ryP M4XDdFI2QDd6M{Ox
Tib 152 NWG0S45LS3m2b4TvfIlkKEG|c3H5 NHHpdlg4OiCq NILVdJVFVVOR MWLJR|UxRTBwODFOwG0> NHHjOpMzPTh5OEOzNS=>
MCF7 M{LSbGZ2dmO2aX;uJGF{e2G7 NFPFXHk2KM7:TR?= MoTGNlQhcA>? MYjEUXNQ M1TTO2lv\HWlZYOgS|IwVSCjcoLld5Q> NEXCWVEzPTh|NESwNS=>
MDA-MB-231 NHvPS3FHfW6ldHnvckBCe3OjeR?= MXq1JO69VQ>? Moe1NlQhcA>? MVrEUXNQ M3Pt[2lv\HWlZYOgS|MwVSCjcoLld5Q> Mm\oNlU5OzR2MEG=
MCF7 MlO2SpVv[3Srb36gRZN{[Xl? NUnwWYUxPSEQvF2= MnPQNlQhcA>? MUHEUXNQ MXLE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ Mlz0NlU5OzR2MEG=
MCF7 NV30fmJuTnWwY4Tpc44hSXO|YYm= MYS1JO69VQ>? M12yelI1KGh? NXr2b5JsTE2VTx?= NIHvSotF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NHO4TG4zPTh|NESwNS=>
MCF7 NV;HTYNzTnWwY4Tpc44hSXO|YYm= M4rIOlUh|ryP M37GW|I1KGh? MYXEUXNQ NHLlc4hF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx M1:5OlI2QDN2NECx
MCF7 M4mydmZ2dmO2aX;uJGF{e2G7 MoXXOUDPxE1? NXi3TIh3OjRiaB?= Mm\QSG1UVw>? MkO2TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> NFfsU4EzPTh|NESwNS=>
MCF7 M{m0b2Z2dmO2aX;uJGF{e2G7 NGj3R5k2KM7:TR?= M3K5TVI1KGh? MljBSG1UVw>? M4LGWGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= MXGyOVg{PDRyMR?=
MDA-MB-231 MkO4SpVv[3Srb36gRZN{[Xl? M1rWRVUh|ryP M2TDfFI1KGh? Mny3SG1UVw>? NIjWb5ZF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy MoDTNlU5OzR2MEG=
MDA-MB-231 NEfPfVJHfW6ldHnvckBCe3OjeR?= NWjGemp2OSEQvF2= NVLlOFFOOjRiaB?= MYPEUXNQ MXPJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=> MkfpNlU5OzR2MEG=
MDA-MB-231 NYTwSmNvTnWwY4Tpc44hSXO|YYm= NGjXRZo2KM7:TR?= NInQW5czPCCq NEjpXZpFVVOR NI\uTopF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx NWrsU4tYOjV6M{S0NFE>
MDA-MB-231 NUfQV2M4TnWwY4Tpc44hSXO|YYm= NVS5foNvPSEQvF2= NXnlcHpuOjRiaB?= M2riW2ROW09? NXzDdpJZUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? MlmwNlU5OzR2MEG=
MDA-MB-231 MXPGeY5kfGmxbjDBd5NigQ>? NH\HR282KM7:TR?= M2\pelI1KGh? NY\DPJlKTE2VTx?= NV7BV2UxUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzPyCNaYCx MXeyOVg{PDRyMR?=
MDA-MB-231 MoPZSpVv[3Srb36gRZN{[Xl? NHPQWFc2KM7:TR?= MonhNlQhcA>? MVLEUXNQ NXG0VXM2UW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJA2Ow>? NF\5dlQzPTh|NESwNS=>
MCF7 NYjUZ2RVSXCxcITvd4l{KEG|c3H5 NES3NHg2KM7:TR?= M1X2[FI1KGh? MYrEUXNQ NHqxWnhKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= M1jtS|I2QDN2NECx
MDA-MB-231 NX3ub|ZESXCxcITvd4l{KEG|c3H5 NFr5eWI2KM7:TR?= MXiyOEBp MkTYSG1UVw>? M1j0cmlv\HWlZYOgZZBweHSxdHnjJIRm[XSq MmPvNlU5OzR2MEG=
MCF7 M1jRXmZ2dmO2aX;uJGF{e2G7 M2jUSFEh|ryP MUK3NkBp MYXEUXNQ MUTJcoR2[2W|IHH1eI9xcGGpaXOg[IVifGh? NELUbpUzPTh|NESwNS=>
MDA-MB-231 NYTL[W9ITnWwY4Tpc44hSXO|YYm= MYSxJO69VQ>? NUP4flRiPzJiaB?= M2\Re2ROW09? NELmPGRKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= MXGyOVg{PDRyMR?=
U-2 OS M3:1fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWO1NEDPxE1? M{XlelI1KGh? MXjEUXNQ NX\IWXdKUUN3ME2xOk43KM7:TR?= NYLXOYF1OjV5OUK4NVE>
MG-63 NVrkWlhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;SOVAh|ryP M4KzTFI1KGh? NGHpUFZFVVOR MnjETWM2OD17LkWg{txO Mn;xNlU4QTJ6MUG=
U-2 OS MnTHRZBweHSxc3nzJGF{e2G7 NYKyXW4{PSEQvF2= MmjVNlQhcA>? NVnkfWpjTE2VTx?= MkC0TY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> NWX1eIVHOjV5OUK4NVE>
MG-63 NGfkOHhCeG:ydH;zbZMhSXO|YYm= MkPMOUDPxE1? NVnTWIVGOjRiaB?= NH;PWHJFVVOR MoroTY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> MkS0NlU4QTJ6MUG=
U-2 OS MYnGeY5kfGmxbjDBd5NigQ>? M{nXcVUh|ryP M2XINVI1KGh? M2\TOGROW09? NWj3O5YyWHKxbX;0[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq MljsNlU4QTJ6MUG=
MG-63 NGnWUVRHfW6ldHnvckBCe3OjeR?= NGrNU4Q2KM7:TR?= MWqyOEBp NEW0enJFVVOR M3XPWHBzd22xdHXzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? NGm0SIUzPTd7MkixNS=>
PANC-1 M3ricmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoiwOVAh|ryP MlrwNlQhcA>? NGHqSGNFVVOR NITHS2dKSzVyPUeuNUDPxE1? MUeyOVY{OjJ{NR?=
BxPC-3 MmjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XzcVUxKM7:TR?= Ml\xNlQhcA>? MoXDSG1UVw>? M2X1dWlEPTB;Nj64JO69VQ>? M376[lI2PjN{MkK1
PANC-1 MmCzSpVv[3Srb36gRZN{[Xl? MV21JO69VQ>? M1W2elI1KGh? NFjadJRFVVOR M3fZVGlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hTzJxTTDwbIF{\Q>? MWqyOVY{OjJ{NR?=
BxPC-3 MU\GeY5kfGmxbjDBd5NigQ>? MnPhOUDPxE1? MV:yOEBp NHyxNnhFVVOR MV;JcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> NUnhV2pnOjV4M{KyNlU>
PANC-1 NF;UdVlHfW6ldHnvckBCe3OjeR?= NFraRpg2KM7:TR?= NGHWbZYzPCCq MV\EUXNQ MVXJcoR2[2W|IHH1eI9xcGGpaXOgZ4VtdCCmZXH0bC=> NFnCN44zPTZ|MkKyOS=>
BxPC-3 NUHEe3RiTnWwY4Tpc44hSXO|YYm= MV21JO69VQ>? M{G3OlI1KGh? NFntdHhFVVOR M1[wPWlv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp M2rOZlI2PjN{MkK1
SKOV3 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOxNFAh|ryP M{HVbFI1KGh? Mn\mSG1UVw>? NXvNVmU5UUN3ME2yNE41QCEQvF2= Ml21NlU3OjR5NUC=
OVCAR4 M4qwb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHqeIdjOTByIN88US=> M4W3elI1KGh? NEXaRZpFVVOR MYLJR|UxRTJ{LkGzJO69VQ>? NILSZokzPTZ{NEe1NC=>
SKOV3 M3vhXGZ2dmO2aX;uJGF{e2G7 MVW1JO69VQ>? NELWXII4OiCq M2rKRmROW09? MkPaTY5lfWOnczDHNk9OKGG{cnXzeC=> Ml7SNlU3OjR5NUC=
OVCAR4 NH7aW|FHfW6ldHnvckBCe3OjeR?= NIrFbI02KM7:TR?= NG\5NIk4OiCq NFq3RVlFVVOR MnWyTY5lfWOnczDHNk9OKGG{cnXzeC=> MVeyOVYzPDd3MB?=
SKOV3 MXvBdI9xfG:|aYOgRZN{[Xl? NHTZVGc2KM7:TR?= NFjrfYgzPCCq MoC0SG1UVw>? NUHUVVZsUW6mdXPld{BieG:ydH;zbZM> M4DlXVI2PjJ2N{Ww
OVCAR4 NWexfpg2SXCxcITvd4l{KEG|c3H5 MlzXOUDPxE1? NW\nW5J4OjRiaB?= M1P5XmROW09? MVXJcoR2[2W|IHHwc5B1d3Orcx?= NF\CRlkzPTZ{NEe1NC=>
AGS NInvOIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\HOW12OjVizszN NXHCclVCOjRiaB?= NEPme2VFVVOR MmXkTWM2OD1zOT6wPUDPxE1? NHu4fVAzPTZyOUmyNy=>
NCI-N78 NVHSdGpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXkWWMzPSEQvF2= M3rxV|I1KGh? MWDEUXNQ NH\oZ|VKSzVyPUK2MlM{KM7:TR?= NE\6W48zPTZyOUmyNy=>
AGS NULt[|d7SXCxcITvd4l{KEG|c3H5 MlHPOUDPxE1? MnL2NlQhcA>? MmjLSG1UVw>? NFjy[2FKdmS3Y3XzJIFxd3C2b4Ppdy=> NHznWIwzPTZyOUmyNy=>
NCI-N78 MYXBdI9xfG:|aYOgRZN{[Xl? M{nPSFUh|ryP NWLlfHp2OjRiaB?= MnvhSG1UVw>? NVSzVYx3UW6mdXPld{BieG:ydH;zbZM> NHm2c3YzPTZyOUmyNy=>
AGS M{THVWZ2dmO2aX;uJGF{e2G7 NHe4SVg2KM7:TR?= MYSyOEBp MU\EUXNQ NHLXZpZKdmS3Y3XzJJRp\SCjdYTvdIhi\3l? NYHPTpFLOjV4MEm5NlM>
NCI-N78 NHP2elJHfW6ldHnvckBCe3OjeR?= MmS0OUDPxE1? NGe1O4UzPCCq MX3EUXNQ MonyTY5lfWOnczD0bIUh[XW2b4DoZYd6 NXLLR2JPOjV4MEm5NlM>
HSC-3 MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fheVEh|ryP M3XSfFQ5KGh? Mo\FTWM2OD1yLkW0JO69VQ>? NELMSWMzPTN4NkG0Ny=>
GB30 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvlSYQyKM7:TR?= NXLme5VUPyCm M2PTeGROW09? NWPxVZhVUUN3ME2wMlAyOSEQvF2= NWXLTIlzOjVzME[0Nlg>
GB9 NEH5N2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3sT|YyKM7:TR?= MUW3JIQ> Mk\FSG1UVw>? MkLnTWM2OD1yLkCyOEDPxE1? MXKyOVExPjR{OB?=
GB169 M3XO[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfRXW9iOSEQvF2= NWDZUoVPPyCm NWHzZo1CTE2VTx?= MUPJR|UxRTBwMEOyJO69VQ>? NHGzWnAzPTFyNkSyPC=>
T24 NIDBXGJHfW6ldHnvckBCe3OjeR?= MnfONUDPxE1? NITvbZA1QCCq NGHmfGRFVVOR M4nBOmlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NV2weFc1OjN2MEO2N|M>
RT4 M2rP[WZ2dmO2aX;uJGF{e2G7 MnrPNUDPxE1? MWq0PEBp MkTFSG1UVw>? MYTJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 M2PQNFI{PDB|NkOz
UM-UC-3 MVzGeY5kfGmxbjDBd5NigQ>? MlmwNUDPxE1? MnrLOFghcA>? MUTEUXNQ NVLLbVFWUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NH;sZmgzOzRyM{[zNy=>
T24 NX7JW4J6SXCxcITvd4l{KEG|c3H5 MmrzN{4yPiEQvF2= NFf3O5c6PiCq MX3EUXNQ NXXuVWpGUUN3ME2wMlA{ODZizszN M{jEUlI{PDB|NkOz
RT4 MVrBdI9xfG:|aYOgRZN{[Xl? Mni1N{4yPiEQvF2= M{jsTlk3KGh? Mn:0SG1UVw>? NHK4cotKSzVyPUCuNVE6QCEQvF2= NFjRTnQzOzRyM{[zNy=>
UM-UC-3 Ml\qRZBweHSxc3nzJGF{e2G7 NEjHSGM{NjF4IN88US=> NVHJPYxDQTZiaB?= NWPIb2FDTE2VTx?= NIPoeZBKSzVyPUCuNFQ1QSEQvF2= NVjLVWt4OjN2MEO2N|M>
OVCAR-5 Mmi4SpVv[3Srb36gRZN{[Xl? M2PtTlUxKG6P M1;ifWlvcGmkaYTzJINmdGxibXnndoF1cW:w NID0VHQzOzN|NEOyOy=>
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RS4-11 Mnu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{S4fFExKM7:TR?= M1nEfFk3KGh? MVjJR|UxRTBwMEG4JO69VQ>? NWT0NlFxOjBzMEizN|g>
MOLT-4 NWjIPGlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqxNEDPxE1? MWq5OkBp NYTRSm9FUUN3ME2wMlAzPiEQvF2= MWiyNFExQDN|OB?=
CCRF-CEM M4TmdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLkVJI{OTBizszN MUO5OkBp NEPlSVhKSzVyPUCuNFk1KM7:TR?= MUWyNFExQDN|OB?=
Kasumi-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXixNEDPxE1? MYe5OkBp MWjJR|UxRTBwMUCzJO69VQ>? NVX0NWQxOjBzMEizN|g>
Karpas-299 NWHiXGlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLuOINEOTBizszN M4HvXlk3KGh? NEX3dnBKSzVyPUCuNFM5KM7:TR?= NEL1So4zODFyOEOzPC=>
Ramos-RA1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexNEDPxE1? NFO5bpc6PiCq M3uzZmlEPTB;MD6xNlch|ryP MUmyNFExQDN|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
  • 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
Smiles COC1=C(C(=CC=C1)F)C2=NCC3=C(N=C(NC4=CC(=C(C=C4)C(O)=O)OC)N=C3)C5=C2C=C(Cl)C=C5

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
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

Aurora Kinase Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID