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 M2K4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHmNE42KM7:TR?= MVO3NkBp M2DmPWROW09? M3nDfWlEPTB;MD6wOEDPxE1? MWiyOlE{PjZ6NB?=
LS174T MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;oNE42KM7:TR?= NITNb2I4OiCq M2fLbmROW09? NYrROWU5UUN3ME2wMlA2KM7:TR?= M322WVI3OTN4Nki0
T84 M4nZ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nNWVAvPSEQvF2= MnXsO|IhcA>? Mmm5SG1UVw>? MUnJR|UxRTBwMEmg{txO M2XCT|I3OTN4Nki0
LS180 NWr0UnlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\TV|AvPSEQvF2= NVewb2dCPzJiaB?= MlfGSG1UVw>? NV7IV|B3UUN3ME2xJO69VQ>? NUDCc41iOjZzM{[2PFQ>
SW948 NGjOU4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXyXW1QOC53IN88US=> MUW3NkBp NGO3[oRFVVOR NVLDPFJqUUN3ME2xJO69VQ>? M1rhNFI3OTN4Nki0
HCT15 NEDMdFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWwMlUh|ryP NV:1TY16PzJiaB?= Mmn1SG1UVw>? MoC5TWM2ODxyLkSg{txO MXqyOlE{PjZ6NB?=
DLD-1 M3XkPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LOXVAvPSEQvF2= NXzub5ozPzJiaB?= MYTEUXNQ MWPJR|UxRDBwODFOwG0> MYKyOlE{PjZ6NB?=
MIP-101 M2LYRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XQ[lAvPSEQvF2= MkXMO|IhcA>? NGLGTFZFVVOR MmjhTWM2OD1zIN88US=> MWGyOlE{PjZ6NB?=
SNU1544 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLxZ|YxNjVizszN NIfYXZo4OiCq NGnIe49FVVOR NWfUTWp6UUN3ME2xJO69VQ>? NGjXRXgzPjF|Nk[4OC=>
OCI-Ly10 M3PseWN6fG:2b4jpZ{BCe3OjeR?= MUm3NkBp MVfEUXNQ NWjGPYxSUUN3ME2wMlA2QCEQvF2= M4jQUVI2QDd6M{Ox
SU-DHL2 MofyR5l1d3SxeHnjJGF{e2G7 NX3TbJZjPzJiaB?= NWDJcGprTE2VTx?= M3XBc2lEPTB;MD6wNUDPxE1? M2r1TlI2QDd6M{Ox
OCI-LY7 M2DRdWN6fG:2b4jpZ{BCe3OjeR?= NX\CWm1kPzJiaB?= MmqwSG1UVw>? NFrae3VKSzVyPUCuNFgyKM7:TR?= MXiyOVg4QDN|MR?=
SU-DHL6 NI\EfJNEgXSxdH;4bYMhSXO|YYm= MlnXO|IhcA>? NYK3fHpxTE2VTx?= MYfJR|UxRTBwNEiyJO69VQ>? NX\jSpN7OjV6N{izN|E>
Jeko-1 MnjWR5l1d3SxeHnjJGF{e2G7 NHHLT3Q4OiCq MVLEUXNQ NIDrdo1KSzVyPUCuNFI6KM7:TR?= M1H4flI2QDd6M{Ox
JVM-2 Ml:1R5l1d3SxeHnjJGF{e2G7 M2\LbVczKGh? MkDzSG1UVw>? M1rlcGlEPTB;MD6wNUDPxE1? Mmi3NlU5Pzh|M{G=
Rec-1 M1PafWN6fG:2b4jpZ{BCe3OjeR?= NGjXcGc4OiCq MlewSG1UVw>? MXzJR|UxRTBwMEi3JO69VQ>? MljhNlU5Pzh|M{G=
Z-138 NX[2OWFJS3m2b4TvfIlkKEG|c3H5 MnzxO|IhcA>? NXjo[IRUTE2VTx?= Mmj6TWM2OD1yLkCxN{DPxE1? MX:yOVg4QDN|MR?=
H9 MlHDR5l1d3SxeHnjJGF{e2G7 MUK3NkBp NYX5bJdLTE2VTx?= M{C1S2lEPTB;MD62JO69VQ>? Mmi1NlU5Pzh|M{G=
HH NG\Kb2hEgXSxdH;4bYMhSXO|YYm= MVS3NkBp M3npd2ROW09? Mk\tTWM2OD1yLkeg{txO NUn0NlV5OjV6N{izN|E>
DND41 MknhR5l1d3SxeHnjJGF{e2G7 NIrXO5c4OiCq NIrqN41FVVOR NYSyWIFEUUN3ME2wMlEh|ryP MWKyOVg4QDN|MR?=
CCL119 NXvZXJdQS3m2b4TvfIlkKEG|c3H5 M4PVe|czKGh? M37VcGROW09? MV3JR|UxRTBwME[yJO69VQ>? NYrwSVZROjV6N{izN|E>
J.Cam 1.6 M1XWSWN6fG:2b4jpZ{BCe3OjeR?= MmrsO|IhcA>? Mn;tSG1UVw>? MlTLTWM2OD1yLkGwOUDPxE1? NIPseJUzPTh5OEOzNS=>
Sup-T1 NH73cZBEgXSxdH;4bYMhSXO|YYm= NHXwW2g4OiCq MnPMSG1UVw>? NHTJOpJKSzVyPUKuNVQzKM7:TR?= MlzYNlU5Pzh|M{G=
Tib 152 NWe3Xop1S3m2b4TvfIlkKEG|c3H5 M17NSFczKGh? NWPaSZN1TE2VTx?= M2nWSmlEPTB;MD64JO69VQ>? M1r2bFI2QDd6M{Ox
MCF7 MkD0SpVv[3Srb36gRZN{[Xl? MlP4OUDPxE1? M33nPFI1KGh? M{D2fmROW09? NYnUVpYxUW6mdXPld{BIOi:PIHHydoV{fA>? M2XaT|I2QDN2NECx
MDA-MB-231 NGLOSVdHfW6ldHnvckBCe3OjeR?= NVniflVPPSEQvF2= MoWyNlQhcA>? M1LkRWROW09? NHzyfYdKdmS3Y3XzJGc{N01iYYLy[ZN1 MWKyOVg{PDRyMR?=
MCF7 NXzYTIU4TnWwY4Tpc44hSXO|YYm= MlewOUDPxE1? MWWyOEBp MWLEUXNQ MWDE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ NEHXcnozPTh|NESwNS=>
MCF7 NU\U[WM3TnWwY4Tpc44hSXO|YYm= NF7XTJk2KM7:TR?= MmfVNlQhcA>? MlPNSG1UVw>? M2qwWWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz NH7DTXozPTh|NESwNS=>
MCF7 NYPLNIZ5TnWwY4Tpc44hSXO|YYm= MkPNOUDPxE1? NFL5U4MzPCCq NFm4W2hFVVOR Mnj1SIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIHP5Z4xqdiCEMR?= NWi1WHdFOjV6M{S0NFE>
MCF7 NGLRfHRHfW6ldHnvckBCe3OjeR?= NULXOGNwPSEQvF2= MV:yOEBp Ml:0SG1UVw>? MkW3TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> M1uyclI2QDN2NECx
MCF7 NVXXTpZNTnWwY4Tpc44hSXO|YYm= MkDPOUDPxE1? NU\SepBnOjRiaB?= M{DvSmROW09? NWPRTlVFUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzPyCNaYCx NY\1cZNFOjV6M{S0NFE>
MDA-MB-231 MVfGeY5kfGmxbjDBd5NigQ>? NWDkNIRTPSEQvF2= NFLnfpMzPCCq MWXEUXNQ NIrTNGRF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy MmPyNlU5OzR2MEG=
MDA-MB-231 M3u5NWZ2dmO2aX;uJGF{e2G7 M1vsVVEh|ryP NV[0fIRlOjRiaB?= MXvEUXNQ NHzVRZNKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NWXjd25oOjV6M{S0NFE>
MDA-MB-231 NXi4doc2TnWwY4Tpc44hSXO|YYm= NE[3[242KM7:TR?= MX6yOEBp NUnQd5hzTE2VTx?= M4XEOGRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= MUmyOVg{PDRyMR?=
MDA-MB-231 MoPzSpVv[3Srb36gRZN{[Xl? M2rzTVUh|ryP NUHyZlF5OjRiaB?= NFfB[GJFVVOR NWTuXoxJUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? M2C5ZVI2QDN2NECx
MDA-MB-231 NXvqdpNFTnWwY4Tpc44hSXO|YYm= MmPQOUDPxE1? Mki3NlQhcA>? Mn3TSG1UVw>? M2rTe2lv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= NFrEUIozPTh|NESwNS=>
MDA-MB-231 M3TpU2Z2dmO2aX;uJGF{e2G7 NIS4XXE2KM7:TR?= MXOyOEBp NHfFVWRFVVOR M4XyNGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwOVM> NU\1dXNMOjV6M{S0NFE>
MCF7 MoWwRZBweHSxc3nzJGF{e2G7 MkXOOUDPxE1? M2HObVI1KGh? M2\oSWROW09? MWLJcoR2[2W|IHHwc5B1d3SrYzDk[YF1cA>? NXjxSItOOjV6M{S0NFE>
MDA-MB-231 M1zpVGFxd3C2b4Ppd{BCe3OjeR?= NIniUHY2KM7:TR?= NIrFbY0zPCCq NHzOboRFVVOR NIjNdnhKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= MonMNlU5OzR2MEG=
MCF7 M4XWfGZ2dmO2aX;uJGF{e2G7 MV:xJO69VQ>? Ml;YO|IhcA>? Mn3KSG1UVw>? M2nWeGlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= MUCyOVg{PDRyMR?=
MDA-MB-231 NEnKUI5HfW6ldHnvckBCe3OjeR?= M1\4[lEh|ryP M4XnSFczKGh? MoP2SG1UVw>? M2fmSGlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= M3[0WFI2QDN2NECx
U-2 OS MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXP5dHltPTBizszN NVXx[plsOjRiaB?= NXe5ZnRrTE2VTx?= NX76[IM{UUN3ME2xOk43KM7:TR?= MnfFNlU4QTJ6MUG=
MG-63 MoPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS1NEDPxE1? MWiyOEBp M1jPfGROW09? M{TIW2lEPTB;OT61JO69VQ>? MkWxNlU4QTJ6MUG=
U-2 OS MmnCRZBweHSxc3nzJGF{e2G7 M{nTe|Uh|ryP M2rOW|I1KGh? NVPicI5yTE2VTx?= MkDaTY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> MVeyOVc6OjhzMR?=
MG-63 NIr4S3ZCeG:ydH;zbZMhSXO|YYm= M4TrU|Uh|ryP M4f6[|I1KGh? MXjEUXNQ NVP6NZRUUW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>? M1LqeVI2Pzl{OEGx
U-2 OS NYDLU2ZnTnWwY4Tpc44hSXO|YYm= Mn[wOUDPxE1? NFvBV2IzPCCq MWPEUXNQ NGDXPJFRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? MXOyOVc6OjhzMR?=
MG-63 NHnGUZFHfW6ldHnvckBCe3OjeR?= MVK1JO69VQ>? MknlNlQhcA>? NHLhWItFVVOR NHnFPHVRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? M2XmeFI2Pzl{OEGx
PANC-1 NITxNWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVm1NEDPxE1? M{jMe|I1KGh? NGLM[3lFVVOR M2\jc2lEPTB;Nz6xJO69VQ>? M4XC[lI2PjN{MkK1
BxPC-3 NW\Mc3N[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nPdFUxKM7:TR?= NFm1cpQzPCCq Ml\RSG1UVw>? MW\JR|UxRTZwODFOwG0> M2nUXVI2PjN{MkK1
PANC-1 NX7yOpNsTnWwY4Tpc44hSXO|YYm= M2jJO|Uh|ryP NIfoZXczPCCq NILp[49FVVOR MXzJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> NFvy[pozPTZ|MkKyOS=>
BxPC-3 M2T6eWZ2dmO2aX;uJGF{e2G7 MXK1JO69VQ>? MmDLNlQhcA>? M2[2dWROW09? NFXiOY9KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NWjTeWh[OjV4M{KyNlU>
PANC-1 MXjGeY5kfGmxbjDBd5NigQ>? Mmm2OUDPxE1? M4jIXVI1KGh? M3nkPWROW09? M1TG[2lv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MWiyOVY{OjJ{NR?=
BxPC-3 NHrROWlHfW6ldHnvckBCe3OjeR?= NGL4OIQ2KM7:TR?= NUnNTlh5OjRiaB?= MUfEUXNQ NY[2OGh6UW6mdXPld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? M1zLb|I2PjN{MkK1
SKOV3 NGD2U2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUSzSJpMOTByIN88US=> NEfa[GUzPCCq M{XZXWROW09? NUHpUIFpUUN3ME2yNE41QCEQvF2= M4\rSVI2PjJ2N{Ww
OVCAR4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf6[olpOTByIN88US=> MUKyOEBp MW\EUXNQ MXnJR|UxRTJ{LkGzJO69VQ>? M2\relI2PjJ2N{Ww
SKOV3 M2\nRWZ2dmO2aX;uJGF{e2G7 NX;ZXJBmPSEQvF2= M3T5UFczKGh? NGrjR4pFVVOR NHTYPZdKdmS3Y3XzJGczN01iYYLy[ZN1 MU[yOVYzPDd3MB?=
OVCAR4 M2iwU2Z2dmO2aX;uJGF{e2G7 Mlu1OUDPxE1? M3fHTVczKGh? MVHEUXNQ NVzBdm85UW6mdXPld{BIOi:PIHHydoV{fA>? MlvyNlU3OjR5NUC=
SKOV3 NXz2PGZZSXCxcITvd4l{KEG|c3H5 M2O4[FUh|ryP NH36T3czPCCq NVX2dGQyTE2VTx?= M3PkXmlv\HWlZYOgZZBweHSxc3nz NIO2WYYzPTZ{NEe1NC=>
OVCAR4 M3qyRWFxd3C2b4Ppd{BCe3OjeR?= MVu1JO69VQ>? MlvaNlQhcA>? MWDEUXNQ M1zhTmlv\HWlZYOgZZBweHSxc3nz MUOyOVYzPDd3MB?=
AGS M13PZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITwNYIzPSEQvF2= MYCyOEBp NHv0T4tFVVOR M3fBUWlEPTB;MUmuNFkh|ryP NIjLZ5YzPTZyOUmyNy=>
NCI-N78 NVjWd4pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:zem0zPSEQvF2= MknpNlQhcA>? NXrCc|dtTE2VTx?= M2HrU2lEPTB;Mk[uN|Mh|ryP NVj4VI5NOjV4MEm5NlM>
AGS NHXuN29CeG:ydH;zbZMhSXO|YYm= Mmi3OUDPxE1? NH\hfnQzPCCq M4LLSWROW09? NXLuWndSUW6mdXPld{BieG:ydH;zbZM> M1:zXFI2PjB7OUKz
NCI-N78 NG\seFBCeG:ydH;zbZMhSXO|YYm= NE\CcHM2KM7:TR?= MnrlNlQhcA>? NXHYUnFOTE2VTx?= M3[4Xmlv\HWlZYOgZZBweHSxc3nz M1z2d|I2PjB7OUKz
AGS MYPGeY5kfGmxbjDBd5NigQ>? MV61JO69VQ>? NFvXT4kzPCCq NVLa[FRPTE2VTx?= MXTJcoR2[2W|IITo[UBifXSxcHjh[5k> MY[yOVYxQTl{Mx?=
NCI-N78 MVXGeY5kfGmxbjDBd5NigQ>? NVHWdG1VPSEQvF2= NYryU2JxOjRiaB?= MYjEUXNQ Mm[wTY5lfWOnczD0bIUh[XW2b4DoZYd6 MmPiNlU3ODl7MkO=
HSC-3 M3zze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULtOoNbOSEQvF2= MYq0PEBp MlLYTWM2OD1yLkW0JO69VQ>? Mle3NlU{PjZzNEO=
GB30 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NET4fWQyKM7:TR?= NFr3SHg4KGR? M3m4XWROW09? MnPSTWM2OD1yLkCxNUDPxE1? M4q0dVI2OTB4NEK4
GB9 NHPQWoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHNNXIyKM7:TR?= NGHSbGc4KGR? M{nxdmROW09? M1mwbmlEPTB;MD6wNlQh|ryP Ml3mNlUyODZ2Mki=
GB169 NVzGW3k2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXK5cWdZOSEQvF2= MV63JIQ> M1XV[GROW09? NV3wNGxwUUN3ME2wMlA{OiEQvF2= NFLtT5QzPTFyNkSyPC=>
T24 NUHSZoZNTnWwY4Tpc44hSXO|YYm= M4DXNlEh|ryP NFXxOXY1QCCq NXu4NVB7TE2VTx?= NGW4SFJKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M2HBOlI{PDB|NkOz
RT4 NGLObWNHfW6ldHnvckBCe3OjeR?= MXexJO69VQ>? MVe0PEBp NGPwRVdFVVOR MUfJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NWCydngzOjN2MEO2N|M>
UM-UC-3 NXvWeZM6TnWwY4Tpc44hSXO|YYm= NGn6TmQyKM7:TR?= NXP4PVRbPDhiaB?= M3fiTGROW09? NIfRW5lKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M3XUTFI{PDB|NkOz
T24 M4PYVmFxd3C2b4Ppd{BCe3OjeR?= NXLDZpFDOy5zNjFOwG0> MXy5OkBp NFG0eFRFVVOR M1TnTmlEPTB;MD6wN|A3KM7:TR?= NHLNZ|EzOzRyM{[zNy=>
RT4 NYjxfHVsSXCxcITvd4l{KEG|c3H5 NYKzNII4Oy5zNjFOwG0> MVu5OkBp M2rMd2ROW09? Ml2wTWM2OD1yLkGxPVgh|ryP M1;XelI{PDB|NkOz
UM-UC-3 NW\rRlNoSXCxcITvd4l{KEG|c3H5 NWHxZYtzOy5zNjFOwG0> MonnPVYhcA>? NFP1NYRFVVOR M1jhdWlEPTB;MD6wOFQ6KM7:TR?= MWOyN|QxOzZ|Mx?=
OVCAR-5 MnzxSpVv[3Srb36gRZN{[Xl? Mo\LOVAhdk1? MUXJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? M{W2TFI{OzN2M{K3
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RS4-11 MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETyRXIyOCEQvF2= NF;3ZYs6PiCq NILKTmhKSzVyPUCuNFE5KM7:TR?= MkKzNlAyODh|M{i=
MOLT-4 NXz0PXJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\FPXlzOTBizszN NUKxZ4x2QTZiaB?= NH3FPXhKSzVyPUCuNFI3KM7:TR?= M2HqWFIxOTB6M{O4
CCRF-CEM NFXBb5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfLNVAh|ryP M3XSfFk3KGh? M4jj[2lEPTB;MD6wPVQh|ryP MXeyNFExQDN|OB?=
Kasumi-1 NEDDV4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\uN|ExKM7:TR?= M3PPTlk3KGh? NFXmZmRKSzVyPUCuNVA{KM7:TR?= MmXsNlAyODh|M{i=
Karpas-299 NGPUTotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;BZpFIOTBizszN MkPwPVYhcA>? M1Tqe2lEPTB;MD6wN|gh|ryP MofKNlAyODh|M{i=
Ramos-RA1 MkTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3mzPFExKM7:TR?= NIjheYs6PiCq M37yPGlEPTB;MD6xNlch|ryP NG[xTXEzODFyOEOzPC=>

... 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
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*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
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    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.

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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