Alisertib (MLN8237)

Catalog No.S1133

For research use only.

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.

Alisertib (MLN8237) Chemical Structure

CAS No. 1028486-01-2

Selleck's Alisertib (MLN8237) has been cited by 298 publications

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Other Aurora Kinase Products

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 NFPMVphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\DdJBOOC53IN88US=> NVvQO4ZbPzJiaB?= MlTwSG1UVw>? NXr4[lZsUUN3ME2wMlA1KM7:TR?= NUD3XWFTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xN|Y3QDRpPkK2NVM3Pjh2PD;hQi=>
LS174T M2r4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDqbZptOC53IN88US=> NYrIXZQyPzJiaB?= M1zoW2ROW09? Mn3kTWM2OD1yLkC1JO69VQ>? NULrTYdRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xN|Y3QDRpPkK2NVM3Pjh2PD;hQi=>
T84 NEi1[mlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUewMlUh|ryP NHL0TpI4OiCq NHvZWXBFVVOR NVe3TIZMUUN3ME2wMlA6KM7:TR?= NIfMWGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGzOlY5PCd-Mk[xN|Y3QDR:L3G+
LS180 M2PadWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILjUVYxNjVizszN NEH6Spk4OiCq NUH3O5lzTE2VTx?= NX3MbYIyUUN3ME2xJO69VQ>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF|Nk[4OEc,OjZzM{[2PFQ9N2F-
SW948 MnXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHG0TlIxNjVizszN M2fnS|czKGh? MXXEUXNQ NGLCcnFKSzVyPUGg{txO M3\lO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUO2Olg1Lz5{NkGzOlY5PDxxYU6=
HCT15 NVvXc44xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PTcFAvPSEQvF2= MVu3NkBp NGXOfItFVVOR NUK3TJhYUUN3MEywMlQh|ryP NF3GT2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGzOlY5PCd-Mk[xN|Y3QDR:L3G+
DLD-1 MkDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3joR|AvPSEQvF2= NGLLUnE4OiCq NVv1TpFITE2VTx?= Mn\6TWM2ODxyLkig{txO MkLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzM{[2PFQoRjJ4MUO2Olg1RC:jPh?=
MIP-101 NGfrOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDoNE42KM7:TR?= NET5XJQ4OiCq MoPVSG1UVw>? M3\WRmlEPTB;MTFOwG0> NWO2bXk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xN|Y3QDRpPkK2NVM3Pjh2PD;hQi=>
SNU1544 MmnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXFRlIxNjVizszN MmGzO|IhcA>? MnjTSG1UVw>? MVjJR|UxRTFizszN NE[y[ZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGzOlY5PCd-Mk[xN|Y3QDR:L3G+
OCI-Ly10 MmrLR5l1d3SxeHnjJGF{e2G7 M4X2OlczKGh? M1r5XGROW09? M2P6T2lEPTB;MD6wOVgh|ryP MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
SU-DHL2 NUn0WVRlS3m2b4TvfIlkKEG|c3H5 MlzTO|IhcA>? M1XNSGROW09? MW\JR|UxRTBwMEGg{txO MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
OCI-LY7 NWr5W4pNS3m2b4TvfIlkKEG|c3H5 M2LpO|czKGh? MmH3SG1UVw>? MVnJR|UxRTBwMEixJO69VQ>? NV\USmdpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4O|g{OzFpPkK1PFc5OzNzPD;hQi=>
SU-DHL6 M{LXSmN6fG:2b4jpZ{BCe3OjeR?= MnPLO|IhcA>? Mn\xSG1UVw>? MXXJR|UxRTBwNEiyJO69VQ>? NUXZZYhHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4O|g{OzFpPkK1PFc5OzNzPD;hQi=>
Jeko-1 NV\nT3dPS3m2b4TvfIlkKEG|c3H5 MkX4O|IhcA>? M{HvfWROW09? MX7JR|UxRTBwMEK5JO69VQ>? MoL5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
JVM-2 MXXDfZRwfG:6aXOgRZN{[Xl? M{jzPVczKGh? MkHGSG1UVw>? MnfxTWM2OD1yLkCxJO69VQ>? MnvWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
Rec-1 MYDDfZRwfG:6aXOgRZN{[Xl? MVO3NkBp NY\DcWN6TE2VTx?= NVXESIV6UUN3ME2wMlA5PyEQvF2= MoHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
Z-138 NVHoVnhJS3m2b4TvfIlkKEG|c3H5 MmnGO|IhcA>? NYDiRpFmTE2VTx?= NGHWOolKSzVyPUCuNFE{KM7:TR?= M2PqfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEe4N|MyLz5{NUi3PFM{OTxxYU6=
H9 MWHDfZRwfG:6aXOgRZN{[Xl? NGfBcZY4OiCq MWPEUXNQ NV\4PZM4UUN3ME2wMlYh|ryP MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
HH MVjDfZRwfG:6aXOgRZN{[Xl? NEfFcYM4OiCq NFH3N3pFVVOR M3rtfGlEPTB;MD63JO69VQ>? NFf4RVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi3PFM{OSd-MkW4O|g{OzF:L3G+
DND41 NFvyWG1EgXSxdH;4bYMhSXO|YYm= M4f1RVczKGh? NGjNXXhFVVOR MUPJR|UxRTBwMTFOwG0> NWTudIlWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4O|g{OzFpPkK1PFc5OzNzPD;hQi=>
CCL119 NF73NJNEgXSxdH;4bYMhSXO|YYm= Ml3SO|IhcA>? M{PJb2ROW09? MVTJR|UxRTBwME[yJO69VQ>? Mn3UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
J.Cam 1.6 MXHDfZRwfG:6aXOgRZN{[Xl? Ml;oO|IhcA>? M2\XTWROW09? MnLjTWM2OD1yLkGwOUDPxE1? MkS0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
Sup-T1 NYXlXm91S3m2b4TvfIlkKEG|c3H5 M{[4NlczKGh? MljXSG1UVw>? M1XpcGlEPTB;Mj6xOFIh|ryP NIO4Tpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi3PFM{OSd-MkW4O|g{OzF:L3G+
Tib 152 MlXZR5l1d3SxeHnjJGF{e2G7 NYXWWINuPzJiaB?= MUHEUXNQ MYDJR|UxRTBwODFOwG0> M1TSOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEe4N|MyLz5{NUi3PFM{OTxxYU6=
MCF7 NULzc2hPTnWwY4Tpc44hSXO|YYm= NV\SOmdKPSEQvF2= NIXn[GYzPCCq M4rHTmROW09? M125NGlv\HWlZYOgS|IwVSCjcoLld5Q> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MDA-MB-231 NU\OPJZ2TnWwY4Tpc44hSXO|YYm= NGnEcYU2KM7:TR?= M1ToblI1KGh? NXzKc4hRTE2VTx?= NYf1WYVPUW6mdXPld{BIOy:PIHHydoV{fA>? NXS0cmxPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MCF7 NVLt[nA2TnWwY4Tpc44hSXO|YYm= M1HHUVUh|ryP M3HKdFI1KGh? M4jnUWROW09? MX7E[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MCF7 NIjXU3VHfW6ldHnvckBCe3OjeR?= NFXkc|c2KM7:TR?= NGDnWWIzPCCq MX3EUXNQ NW\r[mZiTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? NEjxeWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MCF7 M1XsZmZ2dmO2aX;uJGF{e2G7 NIHFZWw2KM7:TR?= M3\oNFI1KGh? MYXEUXNQ NVTiWWx{TGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> MmXmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{S0NFEoRjJ3OEO0OFAyRC:jPh?=
MCF7 M4DxfmZ2dmO2aX;uJGF{e2G7 NGTVbmM2KM7:TR?= M3PpTFI1KGh? NY\PeVF7TE2VTx?= MWDJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> NXi0R5YyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MCF7 MYrGeY5kfGmxbjDBd5NigQ>? M{O5dFUh|ryP M1vuVFI1KGh? NXTUT5MxTE2VTx?= M1fTfGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= NX3KUZBzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 NVL0[WJjTnWwY4Tpc44hSXO|YYm= NFS0WWQ2KM7:TR?= NG\MO28zPCCq MVLEUXNQ M3:3SGRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsyN0OGQ{K= NXHDfXlTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 M1PUW2Z2dmO2aX;uJGF{e2G7 NFHE[FAyKM7:TR?= MYiyOEBp Ml7FSG1UVw>? MnHsTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|I> NWrSUIpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 M1\2fGZ2dmO2aX;uJGF{e2G7 NWnNN5ZxPSEQvF2= Mn7rNlQhcA>? NWDLb4FrTE2VTx?= NILnfmNF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MDA-MB-231 Ml\VSpVv[3Srb36gRZN{[Xl? NFzUXJA2KM7:TR?= NUCyUnBrOjRiaB?= NIDlWpdFVVOR MXHJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MDA-MB-231 MoHYSpVv[3Srb36gRZN{[Xl? NHXkd|I2KM7:TR?= MUSyOEBp NWj0NHFRTE2VTx?= MV;JcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEK3JGtqeDF? NHr3epg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MDA-MB-231 NITDUXdHfW6ldHnvckBCe3OjeR?= M1jUT|Uh|ryP NX7SdmVCOjRiaB?= NH;uZlZFVVOR M{PNbWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwOVM> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MCF7 NXn4NFJ5SXCxcITvd4l{KEG|c3H5 NECzNW82KM7:TR?= MkSyNlQhcA>? MmPiSG1UVw>? M3nRfWlv\HWlZYOgZZBweHSxdHnjJIRm[XSq NGHUeXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MDA-MB-231 MVXBdI9xfG:|aYOgRZN{[Xl? NGL6N2c2KM7:TR?= MWGyOEBp MXTEUXNQ NFXjXGhKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MCF7 NW[0ZnFVTnWwY4Tpc44hSXO|YYm= NHH3bngyKM7:TR?= MWS3NkBp NVnFOG8zTE2VTx?= NWn0bpc1UW6mdXPld{BifXSxcHjh[4lkKGSnYYTo MnvqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{S0NFEoRjJ3OEO0OFAyRC:jPh?=
MDA-MB-231 M4fOVmZ2dmO2aX;uJGF{e2G7 NVXhb2lUOSEQvF2= NGX3RVc4OiCq M{XZNWROW09? M2HWcmlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= NVvJUnlZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
U-2 OS MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLLO5U2OCEQvF2= NEn4U|QzPCCq M{HMbGROW09? M4HNb2lEPTB;MU[uOkDPxE1? M2jKPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{myPFEyLz5{NUe5NlgyOTxxYU6=
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SK-N-MC MXLxTHRUKGG|c3H5 M3PtWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? NVLNdIZtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 NEO4bJlyUFSVIHHzd4F6 NHyxdGhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{ MnOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MVrxTHRUKGG|c3H5 M1zEd5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot p-AURKA(T288) / p-EIF4E(S209) / c-Myc ; phospho-Aurora A / Aurora B ; H3S10P / H3K27me2 / H3K27me3 / H3K9me2 / H3AcK / H4K16Ac 28073841 22863010 29477140
Growth inhibition assay Cell viability 25632225
Immunofluorescence acetylated α-tubulin / γ-tubulin ; E-cadherin / β-catenin / vimentin / p-SMAD5 ; Centrin-2 / tubulin ; phospho-Aurora A(T288) 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[2]
  • Animal Models: Severe combined immune-deficient (SCID) mice inoculated subcutaneously with MM1.S cells
  • Dosages: ~30 mg/kg/day
  • Administration: Orally

Solubility (25°C)

In vitro

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.

6mg/mL

Chemical Information

Molecular Weight 518.92
Formula

C27H20ClFN4O4

CAS No. 1028486-01-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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 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 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 Completed 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
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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.

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