Alisertib (MLN8237) 化学構造
分子量: 518.92

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Quality Control & MSDS

製品説明

  • Compare Aurora Kinase Inhibitors
    Aurora Kinase製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Alisertib (MLN8237)は、1.2nMのIC50による選択的なオーロラA阻害剤です。
ターゲット Aurora A
IC50 1.2 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HCT116 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2wMlUh|ryP NGrFVFk4OiCq NWTvUmxlTE2VTx?= NFzyZm1KSzVyPUCuNFQh|ryP MXGyOlE{PjZ6NB?=
LS174T MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVe4fFd1OC53IN88US=> MofNO|IhcA>? Mn7oSG1UVw>? NHPiSGlKSzVyPUCuNFUh|ryP MYSyOlE{PjZ6NB?=
T84 NUDGZ403T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDZUJpKOC53IN88US=> Moq2O|IhcA>? M2rpO2ROW09? MorHTWM2OD1yLkC5JO69VQ>? NHHSWlEzPjF|Nk[4OC=>
LS180 NUDEeGdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LhN|AvPSEQvF2= NIfhSJg4OiCq NHO5PWFFVVOR NHrTUnVKSzVyPUGg{txO NInDPXQzPjF|Nk[4OC=>
SW948 NEG0XYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmwMlUh|ryP NFjvUY44OiCq MnHzSG1UVw>? MX7JR|UxRTFizszN NGHBZYUzPjF|Nk[4OC=>
HCT15 NUPTZo9bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX1dYN3OC53IN88US=> NWjUSGFwPzJiaB?= NETDcIxFVVOR NVrZ[pcyUUN3MEywMlQh|ryP NHXabIszPjF|Nk[4OC=>
DLD-1 NVLHfFVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWwMlUh|ryP MlvEO|IhcA>? MY\EUXNQ M3HJV2lEPTB:MD64JO69VQ>? NGPJUVkzPjF|Nk[4OC=>
MIP-101 NYXFOYhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKwMlUh|ryP M1TSOFczKGh? MX;EUXNQ NEDMWlFKSzVyPUGg{txO NUHZc|E4OjZzM{[2PFQ>
SNU1544 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i5T|AvPSEQvF2= NVvSXItrPzJiaB?= NWX4[lMyTE2VTx?= NHXPc2tKSzVyPUGg{txO MnPBNlYyOzZ4OES=
OCI-Ly10 MV;DfZRwfG:6aXOgRZN{[Xl? NF3PbpE4OiCq MXLEUXNQ NY\zbJBJUUN3ME2wMlA2QCEQvF2= NGnDUmszPTh5OEOzNS=>
SU-DHL2 MmLBR5l1d3SxeHnjJGF{e2G7 MkSzO|IhcA>? M{\v[2ROW09? MYPJR|UxRTBwMEGg{txO MYSyOVg4QDN|MR?=
OCI-LY7 MlzsR5l1d3SxeHnjJGF{e2G7 NXfVU3U3PzJiaB?= NWn5SoY5TE2VTx?= NXT3eVFkUUN3ME2wMlA5OSEQvF2= MoXXNlU5Pzh|M{G=
SU-DHL6 MmPxR5l1d3SxeHnjJGF{e2G7 NWrwfZJyPzJiaB?= MUDEUXNQ NXvt[ZBVUUN3ME2wMlQ5OiEQvF2= NH7BUHEzPTh5OEOzNS=>
Jeko-1 NU\ZXGZSS3m2b4TvfIlkKEG|c3H5 M1\NelczKGh? Mn\tSG1UVw>? NEjrVFdKSzVyPUCuNFI6KM7:TR?= M1XuXFI2QDd6M{Ox
JVM-2 MYDDfZRwfG:6aXOgRZN{[Xl? Mk\jO|IhcA>? NIL2XW5FVVOR NXq5WI06UUN3ME2wMlAyKM7:TR?= MUmyOVg4QDN|MR?=
Rec-1 NUfkV4JXS3m2b4TvfIlkKEG|c3H5 NUDycYhvPzJiaB?= M1G3dWROW09? MkntTWM2OD1yLkC4O{DPxE1? NGrKTHQzPTh5OEOzNS=>
Z-138 NVS5TFRsS3m2b4TvfIlkKEG|c3H5 M4O4TFczKGh? NUjifpJwTE2VTx?= Ml;tTWM2OD1yLkCxN{DPxE1? MXSyOVg4QDN|MR?=
H9 MV3DfZRwfG:6aXOgRZN{[Xl? NUL5emM1PzJiaB?= MUDEUXNQ MWHJR|UxRTBwNjFOwG0> MorZNlU5Pzh|M{G=
HH NUTkXpljS3m2b4TvfIlkKEG|c3H5 MXy3NkBp M4qw[2ROW09? MmLHTWM2OD1yLkeg{txO MVqyOVg4QDN|MR?=
DND41 MWfDfZRwfG:6aXOgRZN{[Xl? MlnZO|IhcA>? MYjEUXNQ MV;JR|UxRTBwMTFOwG0> MnXoNlU5Pzh|M{G=
CCL119 MnvmR5l1d3SxeHnjJGF{e2G7 M4D4NlczKGh? NGXjZXdFVVOR NEDvOG9KSzVyPUCuNFYzKM7:TR?= M1TrTVI2QDd6M{Ox
J.Cam 1.6 Mo[xR5l1d3SxeHnjJGF{e2G7 M1j3XVczKGh? NXfvT496TE2VTx?= NY\oZVhSUUN3ME2wMlExPSEQvF2= NGjWW3ozPTh5OEOzNS=>
Sup-T1 M{PKcGN6fG:2b4jpZ{BCe3OjeR?= Mly5O|IhcA>? NEHCNGVFVVOR NVfTUFlVUUN3ME2yMlE1OiEQvF2= Mme4NlU5Pzh|M{G=
Tib 152 M1;odmN6fG:2b4jpZ{BCe3OjeR?= MV:3NkBp MkG5SG1UVw>? M1HRTWlEPTB;MD64JO69VQ>? NHH3TpczPTh5OEOzNS=>
MCF7 NVS1[XZiTnWwY4Tpc44hSXO|YYm= MlLBOUDPxE1? M{fnV|I1KGh? NEXjZ|RFVVOR NI\JcllKdmS3Y3XzJGczN01iYYLy[ZN1 Ml\MNlU5OzR2MEG=
MDA-MB-231 M2TwS2Z2dmO2aX;uJGF{e2G7 M4TQTlUh|ryP Ml\yNlQhcA>? MmroSG1UVw>? NUG0NI1QUW6mdXPld{BIOy:PIHHydoV{fA>? MWGyOVg{PDRyMR?=
MCF7 M1mwe2Z2dmO2aX;uJGF{e2G7 NWLl[|MzPSEQvF2= NGTmZ2szPCCq MVnEUXNQ M4\zNGRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsyN0OGQ{K= M3mycFI2QDN2NECx
MCF7 M3;vOGZ2dmO2aX;uJGF{e2G7 MV:1JO69VQ>? M4rwVVI1KGh? MVzEUXNQ NH7kXoFF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NFLTRVkzPTh|NESwNS=>
MCF7 MoXJSpVv[3Srb36gRZN{[Xl? Mm[xOUDPxE1? NHi0cnEzPCCq NFPFb5VFVVOR M{\o[WRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= NXjENYN2OjV6M{S0NFE>
MCF7 Mn3nSpVv[3Srb36gRZN{[Xl? NYnGe|U6PSEQvF2= M2XDSlI1KGh? MmPHSG1UVw>? MUjJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> NF;aUYIzPTh|NESwNS=>
MCF7 NV3ScollTnWwY4Tpc44hSXO|YYm= MlH4OUDPxE1? NWGyeWZLOjRiaB?= MlPLSG1UVw>? NGnRcodKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= NHywXW0zPTh|NESwNS=>
MDA-MB-231 MWHGeY5kfGmxbjDBd5NigQ>? M{j5UVUh|ryP MnTUNlQhcA>? NF30dYhFVVOR Ml7JSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|EwS0SFMh?= NIjJWoUzPTh|NESwNS=>
MDA-MB-231 MlHUSpVv[3Srb36gRZN{[Xl? MWixJO69VQ>? MXuyOEBp MUjEUXNQ Ml;tTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|I> M1XCZ|I2QDN2NECx
MDA-MB-231 NECySJFHfW6ldHnvckBCe3OjeR?= MoqwOUDPxE1? MnTNNlQhcA>? M4OxSGROW09? NXzyc5hpTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> Mk\kNlU5OzR2MEG=
MDA-MB-231 NF7PVmpHfW6ldHnvckBCe3OjeR?= NEHrTlU2KM7:TR?= NH20dnAzPCCq NHyxZo1FVVOR MYTJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> MmPGNlU5OzR2MEG=
MDA-MB-231 MYLGeY5kfGmxbjDBd5NigQ>? NGXXTZA2KM7:TR?= NE[5ZpYzPCCq MmDFSG1UVw>? MYfJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEK3JGtqeDF? MnrqNlU5OzR2MEG=
MDA-MB-231 MXPGeY5kfGmxbjDBd5NigQ>? NHvwNVg2KM7:TR?= MXGyOEBp NYfWNZJ6TE2VTx?= NVru[5pLUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJA2Ow>? MX:yOVg{PDRyMR?=
MCF7 NXvjUVRGSXCxcITvd4l{KEG|c3H5 MXK1JO69VQ>? NX:3[o1POjRiaB?= MoL3SG1UVw>? M2nSdGlv\HWlZYOgZZBweHSxdHnjJIRm[XSq NUjETnNGOjV6M{S0NFE>
MDA-MB-231 NFTXeXVCeG:ydH;zbZMhSXO|YYm= MkWxOUDPxE1? MVOyOEBp M2LBfGROW09? M4HiVGlv\HWlZYOgZZBweHSxdHnjJIRm[XSq MXKyOVg{PDRyMR?=
MCF7 NWnyepNwTnWwY4Tpc44hSXO|YYm= NYDKVFVDOSEQvF2= MXG3NkBp MX\EUXNQ NEPLUXFKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= NYjpXmxLOjV6M{S0NFE>
MDA-MB-231 M1LVemZ2dmO2aX;uJGF{e2G7 MoXWNUDPxE1? NHfHdmc4OiCq NIraOpNFVVOR NEPpcWNKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= M1vPRVI2QDN2NECx
U-2 OS NHHQZYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvaOVAh|ryP MYmyOEBp NXzKPIp{TE2VTx?= MX\JR|UxRTF4Lk[g{txO M4j5W|I2Pzl{OEGx
MG-63 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PUfVUxKM7:TR?= NEjmUIwzPCCq MlvDSG1UVw>? MWjJR|UxRTlwNTFOwG0> NFy1WXkzPTd7MkixNS=>
U-2 OS NGLpZWtCeG:ydH;zbZMhSXO|YYm= NUfhUVZbPSEQvF2= M3L5[VI1KGh? M3TkUWROW09? MWHJcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo NIC2[ngzPTd7MkixNS=>
MG-63 M2e4cmFxd3C2b4Ppd{BCe3OjeR?= MV61JO69VQ>? M1ywVFI1KGh? NWrSfo9pTE2VTx?= M1TrPWlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> NWrGN2hMOjV5OUK4NVE>
U-2 OS MmrUSpVv[3Srb36gRZN{[Xl? MX:1JO69VQ>? MUmyOEBp NG\2T2ZFVVOR MkfaVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MVKyOVc6OjhzMR?=
MG-63 NYjtPVJOTnWwY4Tpc44hSXO|YYm= M2f3cFUh|ryP NXPHd4NxOjRiaB?= NG\jRVFFVVOR MmflVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp NYjJe5JlOjV5OUK4NVE>
PANC-1 NUPnXpFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln1OVAh|ryP NGK2VYYzPCCq NFrieIxFVVOR MljjTWM2OD15LkGg{txO NF\IcXczPTZ|MkKyOS=>
BxPC-3 MnLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnye417PTBizszN M33xe|I1KGh? Ml3rSG1UVw>? NV\zeZU5UUN3ME22Mlgh|ryP NGTiOVUzPTZ|MkKyOS=>
PANC-1 M3[xbGZ2dmO2aX;uJGF{e2G7 NV;JR5VZPSEQvF2= MUCyOEBp Mk\sSG1UVw>? MmXUTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDpckBIOi:PIIDoZZNm NInNWm4zPTZ|MkKyOS=>
BxPC-3 NXzKW4xwTnWwY4Tpc44hSXO|YYm= NUC5So1CPSEQvF2= NVm5NWR5OjRiaB?= MlfBSG1UVw>? NHi3UZVKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? MXGyOVY{OjJ{NR?=
PANC-1 MkHNSpVv[3Srb36gRZN{[Xl? NIO1fpE2KM7:TR?= NVjKbVZ2OjRiaB?= MnSwSG1UVw>? MnyyTY5lfWOnczDheZRweGijZ3njJINmdGxiZHXheIg> NVTZZplwOjV4M{KyNlU>
BxPC-3 NWP6T3lOTnWwY4Tpc44hSXO|YYm= NWf3dWg6PSEQvF2= MUeyOEBp MXvEUXNQ NF\oUHpKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? NEWzSJQzPTZ|MkKyOS=>
SKOV3 NHX5[|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVixNFAh|ryP M2S5V|I1KGh? MYPEUXNQ NHvmXY1KSzVyPUKwMlQ5KM7:TR?= M3v0ZVI2PjJ2N{Ww
OVCAR4 NInJe5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rJSFExOCEQvF2= MWKyOEBp NWnlfXVWTE2VTx?= MWTJR|UxRTJ{LkGzJO69VQ>? NHXWbWUzPTZ{NEe1NC=>
SKOV3 M{m0[2Z2dmO2aX;uJGF{e2G7 M1ToVFUh|ryP MYO3NkBp NV\3dFVuTE2VTx?= M1PFdWlv\HWlZYOgS|IwVSCjcoLld5Q> NXjKXox1OjV4MkS3OVA>
OVCAR4 MX;GeY5kfGmxbjDBd5NigQ>? NEjPc5I2KM7:TR?= M1nENlczKGh? M3\3cmROW09? NEKzZ3hKdmS3Y3XzJGczN01iYYLy[ZN1 NFLjNJgzPTZ{NEe1NC=>
SKOV3 NIC2OYlCeG:ydH;zbZMhSXO|YYm= M1XmPFUh|ryP M3G1S|I1KGh? M1:2TmROW09? NV3MS3J5UW6mdXPld{BieG:ydH;zbZM> NETIfpczPTZ{NEe1NC=>
OVCAR4 MWTBdI9xfG:|aYOgRZN{[Xl? NVLvZ|c2PSEQvF2= MoXmNlQhcA>? MoToSG1UVw>? NG\CbVFKdmS3Y3XzJIFxd3C2b4Ppdy=> M2[2clI2PjJ2N{Ww
AGS MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;qXnozPSEQvF2= M4G4UVI1KGh? MW\EUXNQ MknYTWM2OD1zOT6wPUDPxE1? MnLwNlU3ODl7MkO=
NCI-N78 NULNNINWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSyOUDPxE1? Mn3SNlQhcA>? MVfEUXNQ NHv0eoJKSzVyPUK2MlM{KM7:TR?= MUKyOVYxQTl{Mx?=
AGS NYH4NXZDSXCxcITvd4l{KEG|c3H5 MnqyOUDPxE1? MlG4NlQhcA>? MWPEUXNQ NXznNmFOUW6mdXPld{BieG:ydH;zbZM> MlK0NlU3ODl7MkO=
NCI-N78 NFvjZYNCeG:ydH;zbZMhSXO|YYm= NVnIb2MxPSEQvF2= MVGyOEBp MVjEUXNQ NGjiV|RKdmS3Y3XzJIFxd3C2b4Ppdy=> Mlq4NlU3ODl7MkO=
AGS MWnGeY5kfGmxbjDBd5NigQ>? NIXHN|c2KM7:TR?= NXToWGxQOjRiaB?= NUi4dIRoTE2VTx?= MnS1TY5lfWOnczD0bIUh[XW2b4DoZYd6 MUOyOVYxQTl{Mx?=
NCI-N78 NVLLT2hPTnWwY4Tpc44hSXO|YYm= Mn\nOUDPxE1? NGfUW5kzPCCq NGGxemRFVVOR NWjKO|UxUW6mdXPld{B1cGViYYX0c5Bp[We7 M33LNlI2PjB7OUKz
HSC-3 Mn\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPkVXRJOSEQvF2= NEHEWoc1QCCq M4C1NGlEPTB;MD61OEDPxE1? NXfiZYM5OjV|Nk[xOFM>
GB30 MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYmxJO69VQ>? M2fXRlch\A>? NG\GZ4ZFVVOR Mnm4TWM2OD1yLkCxNUDPxE1? MnnZNlUyODZ2Mki=
GB9 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[1NUDPxE1? MXe3JIQ> M2f3[GROW09? M1HyR2lEPTB;MD6wNlQh|ryP NE\GSZYzPTFyNkSyPC=>
GB169 NF\tUHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M131SlEh|ryP NUH5WXk{PyCm MVnEUXNQ NVO4UlBjUUN3ME2wMlA{OiEQvF2= MYiyOVExPjR{OB?=
T24 NV;wVGduTnWwY4Tpc44hSXO|YYm= MX2xJO69VQ>? MmDxOFghcA>? M4Wxe2ROW09? M3HzeGlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NIC4U5YzOzRyM{[zNy=>
RT4 NH\PNHlHfW6ldHnvckBCe3OjeR?= NETSfm0yKM7:TR?= MWK0PEBp M1viZ2ROW09? NGHaNVBKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M1exSFI{PDB|NkOz
UM-UC-3 NHPOTJNHfW6ldHnvckBCe3OjeR?= NEP4bW0yKM7:TR?= MXq0PEBp Ml3SSG1UVw>? NV:zOY1QUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NVTP[25qOjN2MEO2N|M>
T24 MoOzRZBweHSxc3nzJGF{e2G7 MUCzMlE3KM7:TR?= MoPsPVYhcA>? Mn3DSG1UVw>? M1\TWGlEPTB;MD6wN|A3KM7:TR?= MkLGNlM1ODN4M{O=
RT4 M1fKS2Fxd3C2b4Ppd{BCe3OjeR?= M3H4PVMvOTZizszN Mo\xPVYhcA>? NE\k[4NFVVOR MWHJR|UxRTBwMUG5PEDPxE1? NUj0coRuOjN2MEO2N|M>
UM-UC-3 NYnOe29zSXCxcITvd4l{KEG|c3H5 M3uzU|MvOTZizszN NFPFN5c6PiCq M1;vWmROW09? M1PrbmlEPTB;MD6wOFQ6KM7:TR?= Mn\mNlM1ODN4M{O=
OVCAR-5 NX;nToRQTnWwY4Tpc44hSXO|YYm= M3ztNVUxKG6P NUHTd2hJUW6qaXLpeJMh[2WubDDtbYdz[XSrb36= MUOyN|M{PDN{Nx?=
SKOV3ip2 M1\kNmZ2dmO2aX;uJGF{e2G7 MXK1NEBvVQ>? MXHJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? MoLvNlM{OzR|Mke=
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MOLT-4 MlzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HTdVExKM7:TR?= NGTFdJA6PiCq NGDRepBKSzVyPUCuNFI3KM7:TR?= MmS5NlAyODh|M{i=
CCRF-CEM MoPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmxNEDPxE1? NELuR4Q6PiCq M3XPRmlEPTB;MD6wPVQh|ryP NYHleItEOjBzMEizN|g>
Kasumi-1 M2nBbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXexNEDPxE1? MV:5OkBp NYe0R4hyUUN3ME2wMlExOyEQvF2= MmDGNlAyODh|M{i=
Karpas-299 NH3ocpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHHNVAh|ryP MXS5OkBp Mo\yTWM2OD1yLkCzPEDPxE1? NIDhe5YzODFyOEOzPC=>
Ramos-RA1 M1nNSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPidZV[OTBizszN NHrTZ|g6PiCq NXXXfFdQUUN3ME2wMlEzPyEQvF2= Mor3NlAyODh|M{i=

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 A Phase II study of MLN8237 for treatment of patients with ovarian, fallopian tube, or peritoneal carcinoma has been completed.
特集 First orally available inhibitor of Aurora A.

プロトコル (参考用のみ)

キナーゼアッセイ: [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.

細胞アッセイ: [2]

細胞株 MM1.S, MM.1R, LR5, RPMI 8226, DOX40, OPM1, OPM2, INA6, and U266
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 24, 48, and 72 hours
実験の流れ 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.

動物実験: [2]

動物モデル Severe combined immune-deficient (SCID) mice inoculated subcutaneously with MM1.S cells
製剤 Formulated in 10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate
投薬量 ~30 mg/kg/day
投与方法 Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Alisertib (MLN8237) SDF
分子量 518.92
化学式

C27H20ClFN4O4

CAS No. 1028486-01-2
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 27 mg/mL (52.03 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 15% Captisol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 Benzoic acid, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-

カスタマーフィードバック (10)


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Rating
Source Cell Stem Cell, 2012, 11, 179-94. Alisertib (MLN8237) purchased from Selleck
Method qPCR
Cell Lines CCE cells
Concentrations 1 uM
Incubation Time 48 h
Results Treatment with the Aurka-specific chemical inhibitor MLN8237 suppressed pluripotency TF expression and decreased fluorescence in the NG4 Nanog-GFP reporter line.

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Rating
Source EMBO J, 2012, 30, 906-19. Alisertib (MLN8237) purchased from Selleck
Method immunofluorescence
Cell Lines HEK293 cells
Concentrations 0.3 μM
Incubation Time 40 min
Results Incubation of cells with the Aurora-A kinase inhibitor MLN8237 (0.3 μM) induced a change in the localisation of endogenous TACC3 and clathrin from the mitotic spindle to the cytoplasm.

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Rating
Source J Cell Biol, 2010, 191, 1315-32. Alisertib (MLN8237) purchased from Selleck
Method DAPI staining
Cell Lines HeLa cells
Concentrations 10/20 nM
Incubation Time 15 min/24 h
Results Depletion of PPP6C resulted in a twofold increase in the pT288 form of Aurora A at prometaphase and metaphase spindles compared with control cells, and addition of 10 nM MLN8237 reversed this increase (Fig. A). Importantly, this partial Aurora A inhibition with 10 nM MLN8237 also reduced the micronucleation seen in PPP6C-depleted cells from 40 to 5% (Fig. B).

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Rating
Source EMBO reports , 2010, 11, 977-984. Alisertib (MLN8237) purchased from Selleck
Method Immunoprecipitation, MS/MS analysis
Cell Lines HeLa cells
Concentrations 0.5 µM
Incubation Time 1 h
Results This phosphopeptide was absent in interphase cells and strongly reduced in mitotic cells treated with the inhibitor.

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Rating
Source EMBO Mol Med, 2013, 5(1), 149-66. Alisertib (MLN8237) purchased from Selleck
Method Immunofluorescence co-staining
Cell Lines Hs294T xenograft
Concentrations 30 mg/kg
Incubation Time 28 days
Results To extend its findings in vivo, we examined senescence (SA-b-Gal staining), DNA damage (53BP1), NF-kB activity (IkB-a) and the SASP (IL-6) in an Hs294T xenograft tumour after MLN 8237 treatment. Tumour tissues treated with MLN8237 were b-galactosidase-positive (blue), 53BP1 (red) was increased.

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Rating
Source Oncogene, 2014, 33, 3550-60. Alisertib (MLN8237) purchased from Selleck
Method Western blot, time-lapse microscopy, flow cytometry
Cell Lines HeLa cells
Concentrations 6-1000 nM
Incubation Time 2 h,8 h,24 h,48 h
Results Alisertib inhibits AURKA and AURKB in a concentration-dependent manner.

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Rating
Source ACS Chem Biol , 2010, 5, 563-576. Alisertib (MLN8237) purchased from Selleck
Method Duplicate radiometric assays
Cell Lines
Concentrations 0.1-1000 nM
Incubation Time
Results These clinical stage compounds MLN8237 and MLN8254, which exhibit subtly different chemistry, display similar potency towards Aurora A in vitro.

Click to enlarge
Rating
Source ACS Chem Biol , 2010, 5, 563-576. Alisertib (MLN8237) purchased from Selleck
Method Colony assays
Cell Lines WT Aurora A-expressing cells
Concentrations 30 nM
Incubation Time 8 d
Results We find that a T217D/W277E double mutant does not induce cellular resistance to MLN8054 or MLN8237 in cells

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Rating
Source J Biol Chem, 2012, 287, 27670-81. Alisertib (MLN8237) purchased from Selleck
Method Immunofluorescence Microscopy
Cell Lines HeLa cells
Concentrations 100 nM
Incubation Time 2 h
Results The fluorescence intensity of the pT210 signal in the spindle poles was markedly decreasedin Fry-depleted cells. Exposure to MLN8237, a specific inhibitor of Aurora A, also abrogated the pT210 signal in the spindle poles.

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Rating
Source Mol Cancer, 2011, 10, 131. Alisertib (MLN8237) purchased from Selleck
Method immunofluorescence
Cell Lines U2OS cells
Concentrations 20/50 nM
Incubation Time 4 h
Results MLN8237 treatment lasted 4 hours and yielded the induction of spindle abnormalities. Spindles with multiple poles represented 15-20 % of all PM/Ms in M LN8237-treated cultures, comparable to the occurrence in Aurora-Ai cultures. When MON was added, Eg5 was inhibited, and the generation of spindles with fragmented poles in MLN8237-treated cultures was abolished, with a parallel increase in mono polar figures.

文献中の引用 (45)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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