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 68 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 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITNUmoxNjVizszN NVmxS3hVPzJiaB?= MonuSG1UVw>? MnH0TWM2OD1yLkC0JO69VQ>? M13HW|I3OTN4Nki0
LS174T NIX1TIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWwMlUh|ryP NEHxTZM4OiCq M1Xqd2ROW09? NEe5NlBKSzVyPUCuNFUh|ryP NFKxdIQzPjF|Nk[4OC=>
T84 MonOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PlOVAvPSEQvF2= NUHwVVF7PzJiaB?= NIXRXJpFVVOR NYLTfFExUUN3ME2wMlA6KM7:TR?= NYD6Z5ZNOjZzM{[2PFQ>
LS180 NI\ETplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljHNE42KM7:TR?= MoTIO|IhcA>? MV;EUXNQ NIm2b49KSzVyPUGg{txO NXXaRo42OjZzM{[2PFQ>
SW948 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\uNE42KM7:TR?= MlH5O|IhcA>? NVnQR|ljTE2VTx?= M2fQRmlEPTB;MTFOwG0> NY\FZWhVOjZzM{[2PFQ>
HCT15 M{fZZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHWyUGMxNjVizszN MVG3NkBp M{XmfmROW09? NV\oTlVGUUN3MEywMlQh|ryP MXqyOlE{PjZ6NB?=
DLD-1 MnfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDiPGYxNjVizszN MYC3NkBp M3fl[WROW09? MoO5TWM2ODxyLkig{txO MknYNlYyOzZ4OES=
MIP-101 MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTnNE42KM7:TR?= NIK3RpA4OiCq MV3EUXNQ MVLJR|UxRTFizszN M2fCVlI3OTN4Nki0
SNU1544 M2nUNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\iclM3OC53IN88US=> NGC3fow4OiCq MXHEUXNQ Mo\nTWM2OD1zIN88US=> MoPrNlYyOzZ4OES=
OCI-Ly10 NWHpb4V7S3m2b4TvfIlkKEG|c3H5 M1ntc|czKGh? MVPEUXNQ MlvyTWM2OD1yLkC1PEDPxE1? M1PXblI2QDd6M{Ox
SU-DHL2 M{fnR2N6fG:2b4jpZ{BCe3OjeR?= NFfIdXo4OiCq MofXSG1UVw>? MX\JR|UxRTBwMEGg{txO M2L6UFI2QDd6M{Ox
OCI-LY7 NUTsNFhmS3m2b4TvfIlkKEG|c3H5 NFi5[4Y4OiCq M3y1XmROW09? NIT2c|ZKSzVyPUCuNFgyKM7:TR?= NFTp[IIzPTh5OEOzNS=>
SU-DHL6 NUTicXp5S3m2b4TvfIlkKEG|c3H5 MVi3NkBp NF21WplFVVOR NX2zW3k4UUN3ME2wMlQ5OiEQvF2= MoPkNlU5Pzh|M{G=
Jeko-1 NWHzNIF4S3m2b4TvfIlkKEG|c3H5 NX;obWp6PzJiaB?= M2TE[GROW09? MWjJR|UxRTBwMEK5JO69VQ>? NXLtNFJYOjV6N{izN|E>
JVM-2 MlPSR5l1d3SxeHnjJGF{e2G7 NX7jOoNYPzJiaB?= MkLGSG1UVw>? NEHiWVZKSzVyPUCuNFEh|ryP NX3PNYhROjV6N{izN|E>
Rec-1 M{fIVmN6fG:2b4jpZ{BCe3OjeR?= MYO3NkBp NWDaVlJmTE2VTx?= MXfJR|UxRTBwMEi3JO69VQ>? NVHh[ms3OjV6N{izN|E>
Z-138 NFzPdoZEgXSxdH;4bYMhSXO|YYm= MkjIO|IhcA>? M1eyV2ROW09? NFHJe4pKSzVyPUCuNFE{KM7:TR?= M2rrXlI2QDd6M{Ox
H9 NX[yR5lPS3m2b4TvfIlkKEG|c3H5 Mof4O|IhcA>? MnjqSG1UVw>? NYTsVGpJUUN3ME2wMlYh|ryP MnjaNlU5Pzh|M{G=
HH NY\ndllMS3m2b4TvfIlkKEG|c3H5 NUPxUnRlPzJiaB?= MXvEUXNQ NV3MdVJoUUN3ME2wMlch|ryP Ml7INlU5Pzh|M{G=
DND41 M1PTOmN6fG:2b4jpZ{BCe3OjeR?= Mn7oO|IhcA>? NInBcWJFVVOR M1zKZWlEPTB;MD6xJO69VQ>? M17weVI2QDd6M{Ox
CCL119 MXXDfZRwfG:6aXOgRZN{[Xl? MV63NkBp NYrsVoFRTE2VTx?= NGXVcppKSzVyPUCuNFYzKM7:TR?= MmTKNlU5Pzh|M{G=
J.Cam 1.6 NXjTOW83S3m2b4TvfIlkKEG|c3H5 NYDjfWtyPzJiaB?= MUDEUXNQ NFPYW45KSzVyPUCuNVA2KM7:TR?= NIPrRnEzPTh5OEOzNS=>
Sup-T1 M3uzTGN6fG:2b4jpZ{BCe3OjeR?= NWjhOlhvPzJiaB?= Ml7vSG1UVw>? MmXTTWM2OD1{LkG0NkDPxE1? NIfON4gzPTh5OEOzNS=>
Tib 152 NYL0VZVuS3m2b4TvfIlkKEG|c3H5 NIG3cnM4OiCq NUHaVox3TE2VTx?= MXfJR|UxRTBwODFOwG0> MWiyOVg4QDN|MR?=
MCF7 Mor0SpVv[3Srb36gRZN{[Xl? NUHOfnUyPSEQvF2= NH\Rb4ozPCCq MXzEUXNQ MXPJcoR2[2W|IFeyM20h[XK{ZYP0 MXGyOVg{PDRyMR?=
MDA-MB-231 M{HRRWZ2dmO2aX;uJGF{e2G7 NYfQS|J3PSEQvF2= M1XqbFI1KGh? M3jGPGROW09? M{nmOmlv\HWlZYOgS|MwVSCjcoLld5Q> MkDTNlU5OzR2MEG=
MCF7 NXvscYFTTnWwY4Tpc44hSXO|YYm= NWfaPYxYPSEQvF2= M{jiR|I1KGh? NVnwWnFPTE2VTx?= NHXSSpFF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy MVyyOVg{PDRyMR?=
MCF7 NFPGTYJHfW6ldHnvckBCe3OjeR?= NV7NR3ZjPSEQvF2= NHfUWJgzPCCq NIHs[5RFVVOR NF;NfpBF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NEfyWJYzPTh|NESwNS=>
MCF7 M1;TVGZ2dmO2aX;uJGF{e2G7 NGPyUYQ2KM7:TR?= NXjWZVVFOjRiaB?= NFfnOGxFVVOR M3fJcmRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= Mof3NlU5OzR2MEG=
MCF7 MWTGeY5kfGmxbjDBd5NigQ>? NWP4TZZsPSEQvF2= NYSxZnNLOjRiaB?= NEf3N3pFVVOR NIe4PJVKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFIyKFejZkGvR4lxOQ>? NHTkUWQzPTh|NESwNS=>
MCF7 MXvGeY5kfGmxbjDBd5NigQ>? NVjoXHZKPSEQvF2= NFTUSIMzPCCq MWrEUXNQ MULJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEK3JGtqeDF? Mo\ZNlU5OzR2MEG=
MDA-MB-231 NI\yZ|BHfW6ldHnvckBCe3OjeR?= MYe1JO69VQ>? MXOyOEBp MWjEUXNQ MmfNSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|EwS0SFMh?= NIX6fFEzPTh|NESwNS=>
MDA-MB-231 NFL6SZhHfW6ldHnvckBCe3OjeR?= MoLxNUDPxE1? MUGyOEBp NU\mfJQ4TE2VTx?= MWXJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=> MmnRNlU5OzR2MEG=
MDA-MB-231 MoexSpVv[3Srb36gRZN{[Xl? MojUOUDPxE1? NWTEWW9GOjRiaB?= MlnySG1UVw>? MXPE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz MmLhNlU5OzR2MEG=
MDA-MB-231 M{jkTGZ2dmO2aX;uJGF{e2G7 MnrWOUDPxE1? NXfqNpNjOjRiaB?= NU\VVVhWTE2VTx?= MX7JcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> M3W3Z|I2QDN2NECx
MDA-MB-231 NFW3fpNHfW6ldHnvckBCe3OjeR?= MXe1JO69VQ>? MlL2NlQhcA>? MYHEUXNQ M4jKO2lv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= M330dVI2QDN2NECx
MDA-MB-231 NYnKVZdGTnWwY4Tpc44hSXO|YYm= NFn3Nlc2KM7:TR?= MUeyOEBp MmHKSG1UVw>? NGr5TWhKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFU{ NYnXOVVKOjV6M{S0NFE>
MCF7 Mn:1RZBweHSxc3nzJGF{e2G7 NHf0eoU2KM7:TR?= M3zJXlI1KGh? MYnEUXNQ M{LtXmlv\HWlZYOgZZBweHSxdHnjJIRm[XSq M3TSV|I2QDN2NECx
MDA-MB-231 M{iwNmFxd3C2b4Ppd{BCe3OjeR?= NH;MUHo2KM7:TR?= NYj4XI9lOjRiaB?= Mn3uSG1UVw>? NF2zWHhKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= MmHoNlU5OzR2MEG=
MCF7 NGjt[lJHfW6ldHnvckBCe3OjeR?= MnXVNUDPxE1? M33lU|czKGh? NF3zTFBFVVOR MVfJcoR2[2W|IHH1eI9xcGGpaXOg[IVifGh? M3jwb|I2QDN2NECx
MDA-MB-231 NGnWZZhHfW6ldHnvckBCe3OjeR?= M{\sUlEh|ryP MYi3NkBp MVrEUXNQ NUDkc3pvUW6mdXPld{BifXSxcHjh[4lkKGSnYYTo Ml:yNlU5OzR2MEG=
U-2 OS NUG0bpI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfiT2dLPTBizszN NYrEepl2OjRiaB?= MYDEUXNQ M1\SPGlEPTB;MU[uOkDPxE1? MlTYNlU4QTJ6MUG=
MG-63 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4r2elUxKM7:TR?= MUGyOEBp M4\EdGROW09? M1m2NGlEPTB;OT61JO69VQ>? M{f2NlI2Pzl{OEGx
U-2 OS NYHrOmQ4SXCxcITvd4l{KEG|c3H5 NGDyXnQ2KM7:TR?= NHvDTYEzPCCq NXPDR4NpTE2VTx?= NFP0fIFKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp NEDmR5MzPTd7MkixNS=>
MG-63 MXvBdI9xfG:|aYOgRZN{[Xl? MWm1JO69VQ>? M3\oWVI1KGh? MV;EUXNQ MUPJcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo MVOyOVc6OjhzMR?=
U-2 OS M4rzNmZ2dmO2aX;uJGF{e2G7 NFiyPGc2KM7:TR?= NEew[4czPCCq MXHEUXNQ MnXGVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MmTsNlU4QTJ6MUG=
MG-63 MXTGeY5kfGmxbjDBd5NigQ>? MXu1JO69VQ>? MYOyOEBp NYjTbnZITE2VTx?= NFHsbpJRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? NIe4XoEzPTd7MkixNS=>
PANC-1 MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjxRm82OCEQvF2= MYCyOEBp MVjEUXNQ M2jMNGlEPTB;Nz6xJO69VQ>? M1SwVFI2PjN{MkK1
BxPC-3 NWrYU3lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xmb|UxKM7:TR?= MXmyOEBp MWTEUXNQ MULJR|UxRTZwODFOwG0> MViyOVY{OjJ{NR?=
PANC-1 MW\GeY5kfGmxbjDBd5NigQ>? NXXvRWlSPSEQvF2= NH\FWXQzPCCq NWmz[5JKTE2VTx?= NG\ITWZKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NUHWSVROOjV4M{KyNlU>
BxPC-3 M4L0fWZ2dmO2aX;uJGF{e2G7 MkDZOUDPxE1? NV\pTlg1OjRiaB?= NFu3PHNFVVOR M1KzeGlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hTzJxTTDwbIF{\Q>? MYKyOVY{OjJ{NR?=
PANC-1 M2izbGZ2dmO2aX;uJGF{e2G7 MYW1JO69VQ>? NWL2c5BwOjRiaB?= M4\ZZWROW09? NEfYUlVKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? M1PGVVI2PjN{MkK1
BxPC-3 NEPSZ5lHfW6ldHnvckBCe3OjeR?= Mn30OUDPxE1? NHvJeVgzPCCq MYLEUXNQ M{Tpcmlv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp M4XYc|I2PjN{MkK1
SKOV3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnJNVAxKM7:TR?= Ml;ONlQhcA>? Mn3zSG1UVw>? Mnr0TWM2OD1{MD60PEDPxE1? M17lUlI2PjJ2N{Ww
OVCAR4 NELSXGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\0XJo6OTByIN88US=> MXKyOEBp MlzDSG1UVw>? NF;oNm5KSzVyPUKyMlE{KM7:TR?= MW[yOVYzPDd3MB?=
SKOV3 MkXjSpVv[3Srb36gRZN{[Xl? MUi1JO69VQ>? M2HYVlczKGh? NWHOSYFITE2VTx?= MWnJcoR2[2W|IFeyM20h[XK{ZYP0 M{\DRlI2PjJ2N{Ww
OVCAR4 MnO4SpVv[3Srb36gRZN{[Xl? NFq3Um02KM7:TR?= M4\iWFczKGh? MX\EUXNQ M4DLbmlv\HWlZYOgS|IwVSCjcoLld5Q> M{DCPFI2PjJ2N{Ww
SKOV3 Ml7KRZBweHSxc3nzJGF{e2G7 NUfFNpA1PSEQvF2= MlHZNlQhcA>? MX;EUXNQ M3HrRmlv\HWlZYOgZZBweHSxc3nz NIf2Um8zPTZ{NEe1NC=>
OVCAR4 NFW3N25CeG:ydH;zbZMhSXO|YYm= M{\GclUh|ryP NFS3c2wzPCCq M{DKZ2ROW09? MmLoTY5lfWOnczDhdI9xfG:|aYO= MXWyOVYzPDd3MB?=
AGS NXr0fGh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\6O3FVOjVizszN Mn21NlQhcA>? NVLPV4ZFTE2VTx?= NUHNVnByUUN3ME2xPU4xQSEQvF2= MX6yOVYxQTl{Mx?=
NCI-N78 Mnm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfSNlUh|ryP NGfrcnUzPCCq MVXEUXNQ NYDnUpN[UUN3ME2yOk4{OyEQvF2= MXuyOVYxQTl{Mx?=
AGS MmC2RZBweHSxc3nzJGF{e2G7 MkPsOUDPxE1? NH3tZZQzPCCq MWjEUXNQ M4\tcWlv\HWlZYOgZZBweHSxc3nz MV6yOVYxQTl{Mx?=
NCI-N78 NIDZSnVCeG:ydH;zbZMhSXO|YYm= MYG1JO69VQ>? NH7BV5MzPCCq NGLDPJpFVVOR M1rW[2lv\HWlZYOgZZBweHSxc3nz NWewT2t{OjV4MEm5NlM>
AGS Mnz6SpVv[3Srb36gRZN{[Xl? M{jmdFUh|ryP NVLJUpB2OjRiaB?= M3KzR2ROW09? MlTPTY5lfWOnczD0bIUh[XW2b4DoZYd6 M1mwN|I2PjB7OUKz
NCI-N78 MlrWSpVv[3Srb36gRZN{[Xl? MkL0OUDPxE1? MXmyOEBp M3HFTWROW09? NUXnfW9pUW6mdXPld{B1cGViYYX0c5Bp[We7 NEjZRoszPTZyOUmyNy=>
HSC-3 NUDQT2pjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTmR3kyKM7:TR?= MUG0PEBp M1XmeGlEPTB;MD61OEDPxE1? NYf2elVIOjV|Nk[xOFM>
GB30 NX\Sb4dVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPob2IyKM7:TR?= NUXUeFhjPyCm NYCzfnE{TE2VTx?= NE\YPZhKSzVyPUCuNFEyKM7:TR?= NWX0bpJCOjVzME[0Nlg>
GB9 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;JRXcyKM7:TR?= NEnuVGk4KGR? Mnq3SG1UVw>? NVrjN|djUUN3ME2wMlAzPCEQvF2= MWeyOVExPjR{OB?=
GB169 NV31enNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfQUYUyKM7:TR?= NXflTVQzPyCm MYLEUXNQ MWfJR|UxRTBwMEOyJO69VQ>? MljJNlUyODZ2Mki=
T24 NUnjWlU6TnWwY4Tpc44hSXO|YYm= NX7CeWNsOSEQvF2= NXn3[45IPDhiaB?= M{D1fmROW09? MYfJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MkSyNlM1ODN4M{O=
RT4 M1TvSmZ2dmO2aX;uJGF{e2G7 MmGyNUDPxE1? MmXjOFghcA>? NUKxXXNCTE2VTx?= NHrnUWNKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NF6xd5MzOzRyM{[zNy=>
UM-UC-3 NILL[HZHfW6ldHnvckBCe3OjeR?= NHXVfZQyKM7:TR?= MVy0PEBp NEPW[W1FVVOR NX7rXHR6UW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M{\VSFI{PDB|NkOz
T24 MV;BdI9xfG:|aYOgRZN{[Xl? MlvFN{4yPiEQvF2= MlSyPVYhcA>? M1n3fWROW09? M2TMSGlEPTB;MD6wN|A3KM7:TR?= MoHQNlM1ODN4M{O=
RT4 NEfKe2VCeG:ydH;zbZMhSXO|YYm= M4LXbFMvOTZizszN M4rNPFk3KGh? NYL0OpU1TE2VTx?= NFX0XJlKSzVyPUCuNVE6QCEQvF2= MmmzNlM1ODN4M{O=
UM-UC-3 MUXBdI9xfG:|aYOgRZN{[Xl? NIizRpM{NjF4IN88US=> MX25OkBp MUTEUXNQ NFLYfoJKSzVyPUCuNFQ1QSEQvF2= MVuyN|QxOzZ|Mx?=
OVCAR-5 MoK1SpVv[3Srb36gRZN{[Xl? MkKxOVAhdk1? NYXtd29oUW6qaXLpeJMh[2WubDDtbYdz[XSrb36= MXSyN|M{PDN{Nx?=
SKOV3ip2 MUPGeY5kfGmxbjDBd5NigQ>? MX[1NEBvVQ>? M4fxOmlvcGmkaYTzJINmdGxibXnndoF1cW:w M4\2ZlI{OzN2M{K3
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CCRF-CEM MnKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWexNEDPxE1? MWe5OkBp M2m1SWlEPTB;MD6wPVQh|ryP NEXqSYkzODFyOEOzPC=>
Kasumi-1 NIq3U2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYCxNEDPxE1? Mo\CPVYhcA>? M1LIWWlEPTB;MD6xNFMh|ryP M{LFXFIxOTB6M{O4
Karpas-299 MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFuwWYkyOCEQvF2= NUPjWFlVQTZiaB?= MVjJR|UxRTBwMEO4JO69VQ>? MnnJNlAyODh|M{i=
Ramos-RA1 NEHPNnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXGxNEDPxE1? NX\GN4F5QTZiaB?= NELLRVBKSzVyPUCuNVI4KM7:TR?= Ml\rNlAyODh|M{i=

... 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 (g) = Concentration (mol/L) × Volume (L) × 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02860000 Recruiting Estrogen Receptor Status|HER2/Neu Negative|Invasive Breast Carcinoma|Postmenopausal|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Mayo Clinic|National Cancer Institute (NCI) July 6 2017 Phase 2
NCT02860000 Recruiting Estrogen Receptor Status|HER2/Neu Negative|Invasive Breast Carcinoma|Postmenopausal|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Mayo Clinic|National Cancer Institute (NCI) July 6 2017 Phase 2
NCT02700022 Terminated Diffuse Large B-cell Lymphoma|Follicular Lymphoma|Burkitt Lymphoma UNC Lineberger Comprehensive Cancer Center|Millennium Pharmaceuticals Inc. October 2016 Phase 1
NCT02700022 Terminated Diffuse Large B-cell Lymphoma|Follicular Lymphoma|Burkitt Lymphoma UNC Lineberger Comprehensive Cancer Center|Millennium Pharmaceuticals Inc. October 2016 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
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

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