Alisertib (MLN8237)

For research use only.

Catalog No.S1133

210 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 210 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 M4nJSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTtOmF{OC53IN88US=> NXrQRVdqPzJiaB?= MWLEUXNQ NFvBboxKSzVyPUCuNFQh|ryP NF3CSW4zPjF|Nk[4OC=>
LS174T Mo\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfJXHdvOC53IN88US=> NVLNc4ZlPzJiaB?= M4XsfWROW09? MWLJR|UxRTBwMEWg{txO NIfJ[GQzPjF|Nk[4OC=>
T84 MlPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInQeFYxNjVizszN MXG3NkBp M4THV2ROW09? NILrNpVKSzVyPUCuNFkh|ryP NV7me4dWOjZzM{[2PFQ>
LS180 NGTv[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvVZ|IxNjVizszN NGL1SIQ4OiCq M1XwPGROW09? NUS0doZ4UUN3ME2xJO69VQ>? NWnyd2xxOjZzM{[2PFQ>
SW948 NGTacXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;1d|AvPSEQvF2= MkjoO|IhcA>? MWXEUXNQ MkS2TWM2OD1zIN88US=> MWWyOlE{PjZ6NB?=
HCT15 NXnQXI5QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\hdIUxNjVizszN MX23NkBp NEG5dpNFVVOR MnjITWM2ODxyLkSg{txO MornNlYyOzZ4OES=
DLD-1 M1L1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTPNE42KM7:TR?= M2HkclczKGh? NVHPTYhvTE2VTx?= NFThcIRKSzVyPECuPEDPxE1? NGS3S2IzPjF|Nk[4OC=>
MIP-101 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLqbZgxNjVizszN MlPmO|IhcA>? NUfWVJRNTE2VTx?= M2\Q[WlEPTB;MTFOwG0> NFflNIgzPjF|Nk[4OC=>
SNU1544 M3yzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHrXo97OC53IN88US=> NHnPV3E4OiCq Mn3SSG1UVw>? MWDJR|UxRTFizszN NX7IXGZFOjZzM{[2PFQ>
OCI-Ly10 MXHDfZRwfG:6aXOgRZN{[Xl? M1;tO|czKGh? NGHlN2FFVVOR NGH6T5ZKSzVyPUCuNFU5KM7:TR?= MonvNlU5Pzh|M{G=
SU-DHL2 MWfDfZRwfG:6aXOgRZN{[Xl? M{nnTFczKGh? MnvkSG1UVw>? MUDJR|UxRTBwMEGg{txO NXXUcmdJOjV6N{izN|E>
OCI-LY7 Ml\4R5l1d3SxeHnjJGF{e2G7 NFHuc|E4OiCq MnLpSG1UVw>? M37H[2lEPTB;MD6wPFEh|ryP MlLsNlU5Pzh|M{G=
SU-DHL6 MoDlR5l1d3SxeHnjJGF{e2G7 NGPHbGo4OiCq Mli5SG1UVw>? NYj0T3YyUUN3ME2wMlQ5OiEQvF2= MX:yOVg4QDN|MR?=
Jeko-1 NWXaVnRqS3m2b4TvfIlkKEG|c3H5 NHzHWmU4OiCq NHLRcHVFVVOR MX\JR|UxRTBwMEK5JO69VQ>? M3:w[|I2QDd6M{Ox
JVM-2 Mn3zR5l1d3SxeHnjJGF{e2G7 M371eVczKGh? NGnKdHdFVVOR MVrJR|UxRTBwMEGg{txO NX3K[nZIOjV6N{izN|E>
Rec-1 NXH3dZZ2S3m2b4TvfIlkKEG|c3H5 NHPaNlk4OiCq MYjEUXNQ NUjVWWtEUUN3ME2wMlA5PyEQvF2= M3;ieVI2QDd6M{Ox
Z-138 M3PKXmN6fG:2b4jpZ{BCe3OjeR?= M1;6W|czKGh? NGDvcpRFVVOR M3:zbmlEPTB;MD6wNVMh|ryP M1PPSVI2QDd6M{Ox
H9 MmTwR5l1d3SxeHnjJGF{e2G7 MUW3NkBp NIHPNYRFVVOR MYfJR|UxRTBwNjFOwG0> MUSyOVg4QDN|MR?=
HH MVPDfZRwfG:6aXOgRZN{[Xl? MVG3NkBp M4DjRWROW09? NWXBenVWUUN3ME2wMlch|ryP NYXMdXA2OjV6N{izN|E>
DND41 NXH2SXFVS3m2b4TvfIlkKEG|c3H5 NXj1[Jl2PzJiaB?= NVLNOIZETE2VTx?= M2Hx[2lEPTB;MD6xJO69VQ>? MXSyOVg4QDN|MR?=
CCL119 MUHDfZRwfG:6aXOgRZN{[Xl? MlvnO|IhcA>? MmDLSG1UVw>? NUXZfm1RUUN3ME2wMlA3OiEQvF2= M2ezflI2QDd6M{Ox
J.Cam 1.6 NH7KOpREgXSxdH;4bYMhSXO|YYm= M1;EVFczKGh? M{W4WmROW09? MUjJR|UxRTBwMUC1JO69VQ>? NVTZV3QzOjV6N{izN|E>
Sup-T1 NYTpTZJsS3m2b4TvfIlkKEG|c3H5 MofXO|IhcA>? NYLqZoF5TE2VTx?= MmDxTWM2OD1{LkG0NkDPxE1? MXKyOVg4QDN|MR?=
Tib 152 NELueW5EgXSxdH;4bYMhSXO|YYm= NHGwTWY4OiCq Moe5SG1UVw>? NFfQTYtKSzVyPUCuPEDPxE1? Mne3NlU5Pzh|M{G=
MCF7 NXrwb2ZMTnWwY4Tpc44hSXO|YYm= MkDpOUDPxE1? M3Ht[VI1KGh? M4LyN2ROW09? NXXGcVJlUW6mdXPld{BIOi:PIHHydoV{fA>? MXyyOVg{PDRyMR?=
MDA-MB-231 MUHGeY5kfGmxbjDBd5NigQ>? MofIOUDPxE1? NInRcoEzPCCq MXnEUXNQ NYmzZ3pRUW6mdXPld{BIOy:PIHHydoV{fA>? M4nTflI2QDN2NECx
MCF7 NE\JRlVHfW6ldHnvckBCe3OjeR?= NV;EenF6PSEQvF2= NEnONmczPCCq MlnMSG1UVw>? M1z1bWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsyN0OGQ{K= NVL5VppvOjV6M{S0NFE>
MCF7 NGToS4xHfW6ldHnvckBCe3OjeR?= NYXhPWJ4PSEQvF2= M3X3NFI1KGh? NInO[3hFVVOR MoHmSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|I> NY\wd|ZIOjV6M{S0NFE>
MCF7 NXv1emh3TnWwY4Tpc44hSXO|YYm= NH3XV|I2KM7:TR?= NWnaOYttOjRiaB?= Mn[1SG1UVw>? M1vNPGRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= MlrPNlU5OzR2MEG=
MCF7 M2XacWZ2dmO2aX;uJGF{e2G7 NFzDdng2KM7:TR?= Mlq2NlQhcA>? MX3EUXNQ MlrLTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> NEHZR3EzPTh|NESwNS=>
MCF7 M3uybWZ2dmO2aX;uJGF{e2G7 MojUOUDPxE1? M2jueVI1KGh? MXvEUXNQ NULyRWZuUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzPyCNaYCx M4DPVFI2QDN2NECx
MDA-MB-231 M3qxN2Z2dmO2aX;uJGF{e2G7 MUi1JO69VQ>? NV3RSHBsOjRiaB?= Mo[wSG1UVw>? NGjPNIdF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy NHXUZpEzPTh|NESwNS=>
MDA-MB-231 MnjtSpVv[3Srb36gRZN{[Xl? NFryfZIyKM7:TR?= MXmyOEBp M2jKXmROW09? MV\JcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=> Mm[wNlU5OzR2MEG=
MDA-MB-231 M3e5OWZ2dmO2aX;uJGF{e2G7 NHzleXA2KM7:TR?= MmjPNlQhcA>? MkTwSG1UVw>? M{jnZWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= MoS4NlU5OzR2MEG=
MDA-MB-231 Mnz2SpVv[3Srb36gRZN{[Xl? NE\kT5Q2KM7:TR?= MXKyOEBp M4XvZmROW09? MXjJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> NX7ONlRuOjV6M{S0NFE>
MDA-MB-231 MlnsSpVv[3Srb36gRZN{[Xl? MkPjOUDPxE1? MmXMNlQhcA>? MnnUSG1UVw>? NHzjWo5KdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= NEDS[5EzPTh|NESwNS=>
MDA-MB-231 NIf3bYZHfW6ldHnvckBCe3OjeR?= MXq1JO69VQ>? MmX4NlQhcA>? Mo\ISG1UVw>? MmSxTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIIC1Ny=> NWjENnBpOjV6M{S0NFE>
MCF7 NUTselFLSXCxcITvd4l{KEG|c3H5 MVK1JO69VQ>? NH22[W8zPCCq M3LpcGROW09? NHf4PGVKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= MYCyOVg{PDRyMR?=
MDA-MB-231 NIW4e2tCeG:ydH;zbZMhSXO|YYm= MlHPOUDPxE1? NHvNTI0zPCCq MVfEUXNQ NUDHWIR7UW6mdXPld{BieG:ydH;0bYMh\GWjdHi= NX3XUVVDOjV6M{S0NFE>
MCF7 NWLlV4V1TnWwY4Tpc44hSXO|YYm= M{jHUlEh|ryP NYewWmg2PzJiaB?= MXrEUXNQ NHS4WYdKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= MnHuNlU5OzR2MEG=
MDA-MB-231 NWThRmY6TnWwY4Tpc44hSXO|YYm= NUn2WJJqOSEQvF2= M3faNVczKGh? M{jmcmROW09? M4nTdmlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= MWCyOVg{PDRyMR?=
U-2 OS NWW1[plLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P2d|UxKM7:TR?= MnnFNlQhcA>? NFTaW|VFVVOR MVvJR|UxRTF4Lk[g{txO NIPVUWIzPTd7MkixNS=>
MG-63 NVLjeGhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHDU|g2OCEQvF2= NVSyU2l{OjRiaB?= NInz[5hFVVOR NV;sbnJuUUN3ME25MlUh|ryP M4XUNVI2Pzl{OEGx
U-2 OS M4n5PWFxd3C2b4Ppd{BCe3OjeR?= NULIeWJ1PSEQvF2= M1voT|I1KGh? NIjQV5hFVVOR NEnJWmlKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp M2K0WVI2Pzl{OEGx
MG-63 NF\oPYpCeG:ydH;zbZMhSXO|YYm= MVO1JO69VQ>? MkPYNlQhcA>? M3HQNmROW09? M1vvemlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> M3zjbFI2Pzl{OEGx
U-2 OS MlH0SpVv[3Srb36gRZN{[Xl? M1fqdVUh|ryP NVTiOmZjOjRiaB?= M3LLTWROW09? MVzQdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> NGTDRnAzPTd7MkixNS=>
MG-63 NVPoVoM5TnWwY4Tpc44hSXO|YYm= MnzpOUDPxE1? NGTkPHczPCCq MnfpSG1UVw>? NVewbpZoWHKxbX;0[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq M1S2SlI2Pzl{OEGx
PANC-1 MmjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfLOYdNPTBizszN NGTmdZQzPCCq M{LydmROW09? NV;JZldjUUN3ME23MlEh|ryP NX3EWnE6OjV4M{KyNlU>
BxPC-3 NH72TI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zy[lUxKM7:TR?= M{\zNlI1KGh? M{nHe2ROW09? MWfJR|UxRTZwODFOwG0> NEW2b4gzPTZ|MkKyOS=>
PANC-1 NFHVfYRHfW6ldHnvckBCe3OjeR?= MlnpOUDPxE1? NXLKe45UOjRiaB?= MVjEUXNQ NITtO21KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? M4WxRVI2PjN{MkK1
BxPC-3 MX\GeY5kfGmxbjDBd5NigQ>? NXH5elRVPSEQvF2= NUjPNphPOjRiaB?= MYDEUXNQ MnTvTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDpckBIOi:PIIDoZZNm NEHvZmgzPTZ|MkKyOS=>
PANC-1 NVXub2xETnWwY4Tpc44hSXO|YYm= MYq1JO69VQ>? NI\NbWQzPCCq NEfOPWRFVVOR MknETY5lfWOnczDheZRweGijZ3njJINmdGxiZHXheIg> NVjCZWN3OjV4M{KyNlU>
BxPC-3 Mof1SpVv[3Srb36gRZN{[Xl? NGrnNVI2KM7:TR?= MYOyOEBp NGCzTIdFVVOR NInGTZVKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? NVf6dZRsOjV4M{KyNlU>
SKOV3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlftNVAxKM7:TR?= MWOyOEBp NV\FTolLTE2VTx?= MlX5TWM2OD1{MD60PEDPxE1? MXSyOVYzPDd3MB?=
OVCAR4 NIPJZXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPXeGxOOTByIN88US=> MoDnNlQhcA>? NYW3d2tYTE2VTx?= NF75WY5KSzVyPUKyMlE{KM7:TR?= M{\PTlI2PjJ2N{Ww
SKOV3 Mof0SpVv[3Srb36gRZN{[Xl? MljjOUDPxE1? NIL5bZA4OiCq M2XkemROW09? MYrJcoR2[2W|IFeyM20h[XK{ZYP0 M{nCe|I2PjJ2N{Ww
OVCAR4 M3TtcWZ2dmO2aX;uJGF{e2G7 NGT4OFI2KM7:TR?= MUO3NkBp NELTUoNFVVOR M1rCeWlv\HWlZYOgS|IwVSCjcoLld5Q> NFLCcVkzPTZ{NEe1NC=>
SKOV3 MV7BdI9xfG:|aYOgRZN{[Xl? M1nZb|Uh|ryP NEXBW4QzPCCq M4nuU2ROW09? MnLYTY5lfWOnczDhdI9xfG:|aYO= NHPiO28zPTZ{NEe1NC=>
OVCAR4 M4TyV2Fxd3C2b4Ppd{BCe3OjeR?= MUK1JO69VQ>? NUjwblB6OjRiaB?= NIPXZWFFVVOR NWDqSGZQUW6mdXPld{BieG:ydH;zbZM> NET1ZWUzPTZ{NEe1NC=>
AGS M2rNVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLwNlUh|ryP NYr5UXgyOjRiaB?= NYqxWFBzTE2VTx?= NWTtRnJwUUN3ME2xPU4xQSEQvF2= NVriVWJxOjV4MEm5NlM>
NCI-N78 NXHCbGVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHjfZczOjVizszN NWD2U|FvOjRiaB?= NVnVPYJkTE2VTx?= M1XlXWlEPTB;Mk[uN|Mh|ryP MoqxNlU3ODl7MkO=
AGS M3nFNmFxd3C2b4Ppd{BCe3OjeR?= NEO5RY02KM7:TR?= NGixVogzPCCq MlPvSG1UVw>? NHmwTXRKdmS3Y3XzJIFxd3C2b4Ppdy=> NUHCfHJyOjV4MEm5NlM>
NCI-N78 MXrBdI9xfG:|aYOgRZN{[Xl? Mki1OUDPxE1? MoP4NlQhcA>? MVLEUXNQ MoXZTY5lfWOnczDhdI9xfG:|aYO= MUWyOVYxQTl{Mx?=
AGS MlzISpVv[3Srb36gRZN{[Xl? NFn1Z2U2KM7:TR?= NUP5dY8{OjRiaB?= NFLrNpZFVVOR MmP3TY5lfWOnczD0bIUh[XW2b4DoZYd6 MVuyOVYxQTl{Mx?=
NCI-N78 M{myfmZ2dmO2aX;uJGF{e2G7 NF\MWHg2KM7:TR?= NUO0bIVqOjRiaB?= M4XDVmROW09? NXj0XpZRUW6mdXPld{B1cGViYYX0c5Bp[We7 MkL6NlU3ODl7MkO=
HSC-3 Mmj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33zWFEh|ryP MXe0PEBp M3i4NmlEPTB;MD61OEDPxE1? MUWyOVM3PjF2Mx?=
GB30 MkDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWxJO69VQ>? MoH2O{Bl NH\mSYZFVVOR MVTJR|UxRTBwMEGxJO69VQ>? MYeyOVExPjR{OB?=
GB9 Mn24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSxJO69VQ>? MofTO{Bl MYfEUXNQ NGSyTmxKSzVyPUCuNFI1KM7:TR?= NEn6OFkzPTFyNkSyPC=>
GB169 NInteHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ThclEh|ryP NWSxN4J7PyCm M4GzfGROW09? MWHJR|UxRTBwMEOyJO69VQ>? MknoNlUyODZ2Mki=
T24 Ml23SpVv[3Srb36gRZN{[Xl? NE\SWIQyKM7:TR?= Mk\MOFghcA>? M13ZSGROW09? NIPFTHhKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MViyN|QxOzZ|Mx?=
RT4 NXnZSGhtTnWwY4Tpc44hSXO|YYm= MnzFNUDPxE1? Mm\1OFghcA>? MkG4SG1UVw>? MVrJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NIrycVIzOzRyM{[zNy=>
UM-UC-3 M3;BVmZ2dmO2aX;uJGF{e2G7 NGDkbY4yKM7:TR?= NFvDV|M1QCCq MnTvSG1UVw>? MXPJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NIntenUzOzRyM{[zNy=>
T24 NV2yU5l5SXCxcITvd4l{KEG|c3H5 NG\Qd2g{NjF4IN88US=> NFnJepE6PiCq NVHrZoNXTE2VTx?= NFzFTmtKSzVyPUCuNFMxPiEQvF2= NFH3eXYzOzRyM{[zNy=>
RT4 MX\BdI9xfG:|aYOgRZN{[Xl? MoHwN{4yPiEQvF2= NV;nOW4zQTZiaB?= MV3EUXNQ MoOzTWM2OD1yLkGxPVgh|ryP M1m2[lI{PDB|NkOz
UM-UC-3 M3zwSWFxd3C2b4Ppd{BCe3OjeR?= MV[zMlE3KM7:TR?= NXTaXGh4QTZiaB?= M4rmXWROW09? MoXFTWM2OD1yLkC0OFkh|ryP MYCyN|QxOzZ|Mx?=
OVCAR-5 NWrjcW5LTnWwY4Tpc44hSXO|YYm= Mo\GOVAhdk1? NFm4Ro9KdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MV2yN|M{PDN{Nx?=
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RS4-11 NFvpSlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1v0eVExKM7:TR?= NFHK[nU6PiCq NIjGW5lKSzVyPUCuNFE5KM7:TR?= MV2yNFExQDN|OB?=
MOLT-4 NW\B[HU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvONVAh|ryP MXG5OkBp Mo\zTWM2OD1yLkCyOkDPxE1? MYeyNFExQDN|OB?=
CCRF-CEM M3m0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoThNVAh|ryP NGfaNIM6PiCq Mn3iTWM2OD1yLkC5OEDPxE1? NGS3clgzODFyOEOzPC=>
Kasumi-1 M1i3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq4[ZAyOCEQvF2= NIq5RVc6PiCq MoDtTWM2OD1yLkGwN{DPxE1? NVjReFlNOjBzMEizN|g>
Karpas-299 MojRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUCxNEDPxE1? MYK5OkBp MYXJR|UxRTBwMEO4JO69VQ>? Mo\iNlAyODh|M{i=
Ramos-RA1 NH75PIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M125[VExKM7:TR?= NW\pWm41QTZiaB?= MmXLTWM2OD1yLkGyO{DPxE1? M4rzXFIxOTB6M{O4

... 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID