Alisertib (MLN8237)

For research use only.

Catalog No.S1133

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

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Selleck's Alisertib (MLN8237) has been cited by 203 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. 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 NYnsS|FxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\wNE42KM7:TR?= MUe3NkBp NXXheWlZTE2VTx?= Mn;4TWM2OD1yLkC0JO69VQ>? NF7XcJMzPjF|Nk[4OC=>
LS174T NHPLRoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;mS5F5OC53IN88US=> NXHhZVd4PzJiaB?= MnTiSG1UVw>? NULKcHVCUUN3ME2wMlA2KM7:TR?= NUC5S3hrOjZzM{[2PFQ>
T84 NVnDcIQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[wMlUh|ryP NH[1V2c4OiCq MV\EUXNQ NXG2NllTUUN3ME2wMlA6KM7:TR?= NIHzT3EzPjF|Nk[4OC=>
LS180 MnT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfqNE42KM7:TR?= MnfqO|IhcA>? MlK2SG1UVw>? MUHJR|UxRTFizszN NVXXNnk3OjZzM{[2PFQ>
SW948 NIjNc3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrNXI9tOC53IN88US=> NHzqRZo4OiCq M13xcmROW09? NX[yfXE5UUN3ME2xJO69VQ>? Ml\DNlYyOzZ4OES=
HCT15 NVLtOXhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\qVGwxNjVizszN MXe3NkBp MmjDSG1UVw>? MVvJR|UxRDBwNDFOwG0> M1jzSFI3OTN4Nki0
DLD-1 M1fhNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCwMlUh|ryP M1XOOlczKGh? NX\4PJVkTE2VTx?= MVfJR|UxRDBwODFOwG0> NXXYXYVlOjZzM{[2PFQ>
MIP-101 M1y0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\kdGVkOC53IN88US=> NWHwfFJDPzJiaB?= MnPGSG1UVw>? M3LoU2lEPTB;MTFOwG0> M1rvT|I3OTN4Nki0
SNU1544 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i1OlAvPSEQvF2= M1jJTVczKGh? NIrVRVBFVVOR MVnJR|UxRTFizszN NXXMSXU2OjZzM{[2PFQ>
OCI-Ly10 MX\DfZRwfG:6aXOgRZN{[Xl? NXX6[YJYPzJiaB?= MWPEUXNQ MWnJR|UxRTBwMEW4JO69VQ>? MYeyOVg4QDN|MR?=
SU-DHL2 M2rDN2N6fG:2b4jpZ{BCe3OjeR?= MnH3O|IhcA>? MmLQSG1UVw>? M3jQSGlEPTB;MD6wNUDPxE1? NVXFfFg{OjV6N{izN|E>
OCI-LY7 NHT4UGNEgXSxdH;4bYMhSXO|YYm= MkDQO|IhcA>? M4P6NGROW09? NI\sXHJKSzVyPUCuNFgyKM7:TR?= M2jCfFI2QDd6M{Ox
SU-DHL6 MmLMR5l1d3SxeHnjJGF{e2G7 NFXFUYM4OiCq MXPEUXNQ NHT4e|dKSzVyPUCuOFgzKM7:TR?= NG\sZpIzPTh5OEOzNS=>
Jeko-1 M3LtXGN6fG:2b4jpZ{BCe3OjeR?= M1T3SlczKGh? NFLtOlFFVVOR NGLoephKSzVyPUCuNFI6KM7:TR?= NGnk[ZAzPTh5OEOzNS=>
JVM-2 NH;6W4tEgXSxdH;4bYMhSXO|YYm= MUG3NkBp M1TUS2ROW09? MUnJR|UxRTBwMEGg{txO NXTTS4V2OjV6N{izN|E>
Rec-1 NUDEW2R3S3m2b4TvfIlkKEG|c3H5 MXq3NkBp NV\YXm9pTE2VTx?= M1jCcGlEPTB;MD6wPFch|ryP Ml\zNlU5Pzh|M{G=
Z-138 NWfJWYRmS3m2b4TvfIlkKEG|c3H5 NGHI[lg4OiCq MWfEUXNQ MYrJR|UxRTBwMEGzJO69VQ>? M{XSV|I2QDd6M{Ox
H9 Mn3RR5l1d3SxeHnjJGF{e2G7 NXrre3JxPzJiaB?= NVHPWXoyTE2VTx?= NWDtZZROUUN3ME2wMlYh|ryP NYjp[HIxOjV6N{izN|E>
HH M3HKSGN6fG:2b4jpZ{BCe3OjeR?= NFrxcXo4OiCq MXPEUXNQ NHjTeWVKSzVyPUCuO{DPxE1? MVyyOVg4QDN|MR?=
DND41 MXrDfZRwfG:6aXOgRZN{[Xl? NVnFS29JPzJiaB?= MUDEUXNQ M3TiNGlEPTB;MD6xJO69VQ>? NUfZXXluOjV6N{izN|E>
CCL119 Ml21R5l1d3SxeHnjJGF{e2G7 MnKxO|IhcA>? NH3hSZhFVVOR MnzxTWM2OD1yLkC2NkDPxE1? MUSyOVg4QDN|MR?=
J.Cam 1.6 NV\ZdFdOS3m2b4TvfIlkKEG|c3H5 NVzsR3Y5PzJiaB?= NV\2R4xpTE2VTx?= NYWwS5hEUUN3ME2wMlExPSEQvF2= M2PoWFI2QDd6M{Ox
Sup-T1 MWDDfZRwfG:6aXOgRZN{[Xl? NYrlZodSPzJiaB?= MoDlSG1UVw>? NVTUOI1qUUN3ME2yMlE1OiEQvF2= MlrCNlU5Pzh|M{G=
Tib 152 NEHMNXREgXSxdH;4bYMhSXO|YYm= M4DoRlczKGh? MV3EUXNQ NVTucYNXUUN3ME2wMlgh|ryP M1rwOVI2QDd6M{Ox
MCF7 MnHBSpVv[3Srb36gRZN{[Xl? MWS1JO69VQ>? MnfJNlQhcA>? NEPweVNFVVOR MVLJcoR2[2W|IFeyM20h[XK{ZYP0 MmXjNlU5OzR2MEG=
MDA-MB-231 MmHhSpVv[3Srb36gRZN{[Xl? M2C5cFUh|ryP MViyOEBp M{\4fGROW09? M37I[Wlv\HWlZYOgS|MwVSCjcoLld5Q> M2f0UlI2QDN2NECx
MCF7 NWj0R5c2TnWwY4Tpc44hSXO|YYm= M1XqZ|Uh|ryP NFXXUHkzPCCq M2rTe2ROW09? NVW3e2RZTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzFxQ1TDNi=> NUD3SY9mOjV6M{S0NFE>
MCF7 Ml2xSpVv[3Srb36gRZN{[Xl? MWK1JO69VQ>? MWOyOEBp MV3EUXNQ M37ESGRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz NV;UTFIzOjV6M{S0NFE>
MCF7 MVTGeY5kfGmxbjDBd5NigQ>? M1PLXVUh|ryP MlPFNlQhcA>? M2rKRWROW09? NVfoeGxtTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> MWqyOVg{PDRyMR?=
MCF7 M4jaS2Z2dmO2aX;uJGF{e2G7 MoGzOUDPxE1? M1PxWFI1KGh? NVnae2JyTE2VTx?= MVnJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> MYSyOVg{PDRyMR?=
MCF7 MmfNSpVv[3Srb36gRZN{[Xl? NEHjcJg2KM7:TR?= MViyOEBp M3G5fGROW09? MkjmTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz MmDDNlU5OzR2MEG=
MDA-MB-231 M1PKbmZ2dmO2aX;uJGF{e2G7 M365PVUh|ryP MkixNlQhcA>? NVL4fYVKTE2VTx?= MWTE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ NYnwRY1qOjV6M{S0NFE>
MDA-MB-231 MlnKSpVv[3Srb36gRZN{[Xl? NVK2[oY1OSEQvF2= MnnsNlQhcA>? NYjGOpFSTE2VTx?= M3PyWWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz MmmyNlU5OzR2MEG=
MDA-MB-231 M3rYV2Z2dmO2aX;uJGF{e2G7 MX[1JO69VQ>? NEe0[lMzPCCq MXfEUXNQ NU\COo1YTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> M{j6e|I2QDN2NECx
MDA-MB-231 M3vUbmZ2dmO2aX;uJGF{e2G7 NILZXms2KM7:TR?= M3nkb|I1KGh? NXrLNWc2TE2VTx?= MmfjTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> MVyyOVg{PDRyMR?=
MDA-MB-231 MmS1SpVv[3Srb36gRZN{[Xl? MYK1JO69VQ>? M2fuVVI1KGh? MmHFSG1UVw>? NF\zOo5KdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= MXmyOVg{PDRyMR?=
MDA-MB-231 NHTJRXRHfW6ldHnvckBCe3OjeR?= MXO1JO69VQ>? MWqyOEBp NFvaXHFFVVOR NHv0SXVKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFU{ M2e4elI2QDN2NECx
MCF7 NGnCb4ZCeG:ydH;zbZMhSXO|YYm= MVO1JO69VQ>? NXj3dYJuOjRiaB?= M1raUGROW09? M4XrU2lv\HWlZYOgZZBweHSxdHnjJIRm[XSq NVL1fYdnOjV6M{S0NFE>
MDA-MB-231 MnrjRZBweHSxc3nzJGF{e2G7 NH6wOGE2KM7:TR?= NYDodlBJOjRiaB?= NWDUNXQyTE2VTx?= MlPBTY5lfWOnczDhdI9xfG:2aXOg[IVifGh? MmTQNlU5OzR2MEG=
MCF7 NVHR[m9qTnWwY4Tpc44hSXO|YYm= MV6xJO69VQ>? NGjpeXk4OiCq NWO4RWlTTE2VTx?= MmK3TY5lfWOnczDheZRweGijZ3njJIRm[XSq M2THUVI2QDN2NECx
MDA-MB-231 NVrZcJpHTnWwY4Tpc44hSXO|YYm= NWX4cVlVOSEQvF2= MnjhO|IhcA>? NYThVXU1TE2VTx?= NX;Fc2pmUW6mdXPld{BifXSxcHjh[4lkKGSnYYTo M1nQVlI2QDN2NECx
U-2 OS MormS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfnOVAh|ryP MnvJNlQhcA>? NFPFSYtFVVOR MmK0TWM2OD1zNj62JO69VQ>? M2\EbFI2Pzl{OEGx
MG-63 NIX5SZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnNOVAh|ryP Mmr1NlQhcA>? MWjEUXNQ MXTJR|UxRTlwNTFOwG0> M2n0TlI2Pzl{OEGx
U-2 OS NIP4SpVCeG:ydH;zbZMhSXO|YYm= NXzocG13PSEQvF2= NETuRlgzPCCq NXTUVZJKTE2VTx?= M2GxUWlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> MV:yOVc6OjhzMR?=
MG-63 M3O0NmFxd3C2b4Ppd{BCe3OjeR?= MYG1JO69VQ>? MoHBNlQhcA>? Ml\NSG1UVw>? NV;HRmZ2UW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>? NELvfI4zPTd7MkixNS=>
U-2 OS NFfLUVlHfW6ldHnvckBCe3OjeR?= NEXxeFc2KM7:TR?= MmrINlQhcA>? MWjEUXNQ NXPjN|d6WHKxbX;0[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq M3noOVI2Pzl{OEGx
MG-63 Mn7WSpVv[3Srb36gRZN{[Xl? M{fBTVUh|ryP NXXjTpNsOjRiaB?= M16wVGROW09? MU\Qdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> NInWVIQzPTd7MkixNS=>
PANC-1 NGTObVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHwdYEzPTBizszN MVKyOEBp MkjBSG1UVw>? MV7JR|UxRTdwMTFOwG0> MkHwNlU3OzJ{MkW=
BxPC-3 MkGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonzOVAh|ryP NF2yXmwzPCCq NITKPZhFVVOR M{fxc2lEPTB;Nj64JO69VQ>? MmGwNlU3OzJ{MkW=
PANC-1 MoHjSpVv[3Srb36gRZN{[Xl? MmPxOUDPxE1? MVOyOEBp NHqw[nNFVVOR NFXFNlVKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NVXQdW9qOjV4M{KyNlU>
BxPC-3 M2jKOWZ2dmO2aX;uJGF{e2G7 M4i5PVUh|ryP MmH1NlQhcA>? NWrKVJNwTE2VTx?= NEHofGtKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NVe5cVRFOjV4M{KyNlU>
PANC-1 M1\IOGZ2dmO2aX;uJGF{e2G7 MV21JO69VQ>? NH62eoIzPCCq NV3lSY9LTE2VTx?= NFnKZm9KdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? MWmyOVY{OjJ{NR?=
BxPC-3 MVLGeY5kfGmxbjDBd5NigQ>? MWK1JO69VQ>? NV;MUnI6OjRiaB?= M{nt[mROW09? M3v3O2lv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MlTmNlU3OzJ{MkW=
SKOV3 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M12z[FExOCEQvF2= NX\GfIluOjRiaB?= MYLEUXNQ M3LEZmlEPTB;MkCuOFgh|ryP NWexNIo3OjV4MkS3OVA>
OVCAR4 NECwb3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDUZ4wyODBizszN NHPjSpkzPCCq Mmi5SG1UVw>? Ml[3TWM2OD1{Mj6xN{DPxE1? MnrxNlU3OjR5NUC=
SKOV3 MXfGeY5kfGmxbjDBd5NigQ>? NGTaPVM2KM7:TR?= NFruem04OiCq M3;ONWROW09? NXvuU4VFUW6mdXPld{BIOi:PIHHydoV{fA>? NIWybYkzPTZ{NEe1NC=>
OVCAR4 MYDGeY5kfGmxbjDBd5NigQ>? NITYTFQ2KM7:TR?= NYnQ[o5CPzJiaB?= Mlu3SG1UVw>? NV71UJBOUW6mdXPld{BIOi:PIHHydoV{fA>? M2D0b|I2PjJ2N{Ww
SKOV3 M3uzVmFxd3C2b4Ppd{BCe3OjeR?= MYG1JO69VQ>? M2LqeFI1KGh? NIfnRlhFVVOR M17pT2lv\HWlZYOgZZBweHSxc3nz MXKyOVYzPDd3MB?=
OVCAR4 M2Dyd2Fxd3C2b4Ppd{BCe3OjeR?= NGG1So82KM7:TR?= MXuyOEBp NYTlWGpmTE2VTx?= M2TVPGlv\HWlZYOgZZBweHSxc3nz M2TGXFI2PjJ2N{Ww
AGS NY\BTppKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1exdFI2KM7:TR?= MkXzNlQhcA>? MnK1SG1UVw>? MlPGTWM2OD1zOT6wPUDPxE1? NWj5O2czOjV4MEm5NlM>
NCI-N78 M{DkU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKyOUDPxE1? NGi1TZMzPCCq MV;EUXNQ M1XubWlEPTB;Mk[uN|Mh|ryP NXHCeJU{OjV4MEm5NlM>
AGS MonaRZBweHSxc3nzJGF{e2G7 NHjPbYk2KM7:TR?= MUSyOEBp NH36cmpFVVOR NX\pNmhuUW6mdXPld{BieG:ydH;zbZM> NXnw[VNsOjV4MEm5NlM>
NCI-N78 NWjqSYo2SXCxcITvd4l{KEG|c3H5 NITu[FI2KM7:TR?= M1LUO|I1KGh? MkDRSG1UVw>? NYfwfZVxUW6mdXPld{BieG:ydH;zbZM> NH\aUXczPTZyOUmyNy=>
AGS MljzSpVv[3Srb36gRZN{[Xl? MkLnOUDPxE1? MWiyOEBp NGjSSYdFVVOR NYD2VI4zUW6mdXPld{B1cGViYYX0c5Bp[We7 MlnGNlU3ODl7MkO=
NCI-N78 NWi3c204TnWwY4Tpc44hSXO|YYm= M{SzVlUh|ryP NFLlT3EzPCCq MojrSG1UVw>? NIjYSVJKdmS3Y3XzJJRp\SCjdYTvdIhi\3l? NHeyNHczPTZyOUmyNy=>
HSC-3 NFS2V5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUKxJO69VQ>? MmLYOFghcA>? NEjPPFBKSzVyPUCuOVQh|ryP NXrUVmtyOjV|Nk[xOFM>
GB30 M37tTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzNNUDPxE1? M1zrcFch\A>? NH;FTJVFVVOR MYjJR|UxRTBwMEGxJO69VQ>? MVKyOVExPjR{OB?=
GB9 NHSzOGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3vOZcyKM7:TR?= NV63T4h2PyCm NXjRWmJETE2VTx?= M3zuPWlEPTB;MD6wNlQh|ryP MnrPNlUyODZ2Mki=
GB169 NU\2dmo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLoNUDPxE1? NHu3Z|M4KGR? M2DtWGROW09? NFLodYtKSzVyPUCuNFMzKM7:TR?= MVWyOVExPjR{OB?=
T24 MYLGeY5kfGmxbjDBd5NigQ>? NVG1VJJoOSEQvF2= NEK5W3c1QCCq M2PQOmROW09? MUjJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MXuyN|QxOzZ|Mx?=
RT4 MoLvSpVv[3Srb36gRZN{[Xl? MmGxNUDPxE1? NVG0RY5mPDhiaB?= NF7xRZRFVVOR MmT0TY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= Mn\SNlM1ODN4M{O=
UM-UC-3 MYLGeY5kfGmxbjDBd5NigQ>? NV;4WYY3OSEQvF2= MYm0PEBp MYTEUXNQ NWr0ZlVMUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MVuyN|QxOzZ|Mx?=
T24 NX;uZ2pJSXCxcITvd4l{KEG|c3H5 MmPqN{4yPiEQvF2= NIDicVI6PiCq MkPkSG1UVw>? MnTDTWM2OD1yLkCzNFYh|ryP MYWyN|QxOzZ|Mx?=
RT4 MnvKRZBweHSxc3nzJGF{e2G7 NYD0SZVlOy5zNjFOwG0> M1zxTVk3KGh? NYS4TIFUTE2VTx?= M2PxRmlEPTB;MD6xNVk5KM7:TR?= MoTlNlM1ODN4M{O=
UM-UC-3 M13VfGFxd3C2b4Ppd{BCe3OjeR?= MYSzMlE3KM7:TR?= M1H2OVk3KGh? NV:1UI4yTE2VTx?= NV\pNlR{UUN3ME2wMlA1PDlizszN NHnNcWMzOzRyM{[zNy=>
OVCAR-5 NYrob5kzTnWwY4Tpc44hSXO|YYm= NVHwXJVPPTBibl2= M4\ocGlvcGmkaYTzJINmdGxibXnndoF1cW:w NUjWcm01OjN|M{SzNlc>
SKOV3ip2 MmLUSpVv[3Srb36gRZN{[Xl? MoTJOVAhdk1? MXLJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? MWWyN|M{PDN{Nx?=
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RS4-11 NE\PdI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HadFExKM7:TR?= M17Ke|k3KGh? Ml31TWM2OD1yLkCxPEDPxE1? M{fUeFIxOTB6M{O4
MOLT-4 M4Psfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF6yN2syOCEQvF2= MkXtPVYhcA>? MVLJR|UxRTBwMEK2JO69VQ>? MYWyNFExQDN|OB?=
CCRF-CEM NYnRS3pzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;ONVAh|ryP NHTyTIE6PiCq NIfJeY5KSzVyPUCuNFk1KM7:TR?= NEHyTJIzODFyOEOzPC=>
Kasumi-1 M4TXdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:yc5BPOTBizszN MYO5OkBp MV7JR|UxRTBwMUCzJO69VQ>? MUiyNFExQDN|OB?=
Karpas-299 NXTYcHhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33zZlExKM7:TR?= MXK5OkBp NH\SS|FKSzVyPUCuNFM5KM7:TR?= NFX3ZZAzODFyOEOzPC=>
Ramos-RA1 NETrSIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjQXlAyOCEQvF2= Mk\tPVYhcA>? MXrJR|UxRTBwMUK3JO69VQ>? NWiwXlBjOjBzMEizN|g>

... 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=C(N=C(NC4=CC(=C(C=C4)C(O)=O)OC)N=C3)C5=C2C=C(Cl)C=C5

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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
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

Aurora Kinase Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID