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 M3HOTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[wMlUh|ryP MVm3NkBp NYrYUZFwTE2VTx?= NX3XXJpuUUN3ME2wMlA1KM7:TR?= M2XNU|I3OTN4Nki0
LS174T M1HxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfpNE42KM7:TR?= MknpO|IhcA>? NE\KZpJFVVOR NXXocnFEUUN3ME2wMlA2KM7:TR?= MVuyOlE{PjZ6NB?=
T84 Ml;vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HTcVAvPSEQvF2= MnTWO|IhcA>? MXnEUXNQ NVnac5RqUUN3ME2wMlA6KM7:TR?= M3nRWlI3OTN4Nki0
LS180 MmDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPNZVhiOC53IN88US=> NFT1dXM4OiCq M4W0NWROW09? M4DoTmlEPTB;MTFOwG0> M{j1NFI3OTN4Nki0
SW948 NUj4Zm9qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[yendUOC53IN88US=> MYO3NkBp M1[1fWROW09? M4\YdmlEPTB;MTFOwG0> NXnIUFJvOjZzM{[2PFQ>
HCT15 MkPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:4VFVQOC53IN88US=> NUC0VXRmPzJiaB?= M1i2WWROW09? MWfJR|UxRDBwNDFOwG0> NWmyVYw4OjZzM{[2PFQ>
DLD-1 M4XQOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDCNE42KM7:TR?= MkHFO|IhcA>? M4fPU2ROW09? NGPsSVhKSzVyPECuPEDPxE1? Moe3NlYyOzZ4OES=
MIP-101 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[wMlUh|ryP MmLqO|IhcA>? M1TPOmROW09? Ml;rTWM2OD1zIN88US=> MmPqNlYyOzZ4OES=
SNU1544 NXjXbYxlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDGNE42KM7:TR?= NF;2fIg4OiCq M1rMdmROW09? NWPqSoJnUUN3ME2xJO69VQ>? M3vRUlI3OTN4Nki0
OCI-Ly10 MXnDfZRwfG:6aXOgRZN{[Xl? MYO3NkBp NWj1PVN1TE2VTx?= M1LuVWlEPTB;MD6wOVgh|ryP MXSyOVg4QDN|MR?=
SU-DHL2 M2W4TmN6fG:2b4jpZ{BCe3OjeR?= M2P0O|czKGh? NXqyVZFiTE2VTx?= MVTJR|UxRTBwMEGg{txO NHrTPVkzPTh5OEOzNS=>
OCI-LY7 MlzMR5l1d3SxeHnjJGF{e2G7 M3\SbVczKGh? NG\4ZZBFVVOR NG\2WZBKSzVyPUCuNFgyKM7:TR?= NE\4TWkzPTh5OEOzNS=>
SU-DHL6 NXH1PGxHS3m2b4TvfIlkKEG|c3H5 NUn3OGVEPzJiaB?= NXH6d4Z7TE2VTx?= MVrJR|UxRTBwNEiyJO69VQ>? NE\4S|EzPTh5OEOzNS=>
Jeko-1 MkXNR5l1d3SxeHnjJGF{e2G7 NFrxSII4OiCq NH75XoNFVVOR M{PxXGlEPTB;MD6wNlkh|ryP M{fMcVI2QDd6M{Ox
JVM-2 M3nvTmN6fG:2b4jpZ{BCe3OjeR?= MXy3NkBp NFjN[lJFVVOR NGjtfnVKSzVyPUCuNFEh|ryP NGL2VGczPTh5OEOzNS=>
Rec-1 MlfMR5l1d3SxeHnjJGF{e2G7 NFXUfVM4OiCq NVHPdWdVTE2VTx?= Mn3UTWM2OD1yLkC4O{DPxE1? NX\UXIl[OjV6N{izN|E>
Z-138 MWLDfZRwfG:6aXOgRZN{[Xl? M2nhTVczKGh? M2PmdWROW09? M{TDPWlEPTB;MD6wNVMh|ryP MnvmNlU5Pzh|M{G=
H9 MoTVR5l1d3SxeHnjJGF{e2G7 MWS3NkBp NGfzbFZFVVOR NEX4VYVKSzVyPUCuOkDPxE1? M2rqe|I2QDd6M{Ox
HH MmjGR5l1d3SxeHnjJGF{e2G7 MU[3NkBp M{\hSWROW09? MWPJR|UxRTBwNzFOwG0> MoqzNlU5Pzh|M{G=
DND41 Mke4R5l1d3SxeHnjJGF{e2G7 M2e1VFczKGh? M3nBUmROW09? MkCzTWM2OD1yLkGg{txO NI\MeVAzPTh5OEOzNS=>
CCL119 NVfBfmZkS3m2b4TvfIlkKEG|c3H5 MlzPO|IhcA>? MYTEUXNQ NVvEcFRFUUN3ME2wMlA3OiEQvF2= MoTpNlU5Pzh|M{G=
J.Cam 1.6 MV;DfZRwfG:6aXOgRZN{[Xl? MXe3NkBp M1;INWROW09? M4SyRWlEPTB;MD6xNFUh|ryP NHf6doUzPTh5OEOzNS=>
Sup-T1 MmH0R5l1d3SxeHnjJGF{e2G7 NIDHTWo4OiCq MoK1SG1UVw>? Mn3yTWM2OD1{LkG0NkDPxE1? MoXYNlU5Pzh|M{G=
Tib 152 NWTBWoROS3m2b4TvfIlkKEG|c3H5 MYW3NkBp NEn4XHZFVVOR MY\JR|UxRTBwODFOwG0> MojWNlU5Pzh|M{G=
MCF7 M4DLbGZ2dmO2aX;uJGF{e2G7 MorhOUDPxE1? MoDUNlQhcA>? MnX6SG1UVw>? MWHJcoR2[2W|IFeyM20h[XK{ZYP0 MkHMNlU5OzR2MEG=
MDA-MB-231 MXfGeY5kfGmxbjDBd5NigQ>? MV[1JO69VQ>? NYDLbIsxOjRiaB?= NEXPd5JFVVOR NVXjeo1lUW6mdXPld{BIOy:PIHHydoV{fA>? MlzTNlU5OzR2MEG=
MCF7 M3zBemZ2dmO2aX;uJGF{e2G7 M3TVT|Uh|ryP Ml:0NlQhcA>? NVXYcnF5TE2VTx?= Mmr1SIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|EwS0SFMh?= M1v6cFI2QDN2NECx
MCF7 MVfGeY5kfGmxbjDBd5NigQ>? MUO1JO69VQ>? Mn3pNlQhcA>? M3;XWmROW09? NXTLWZNrTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? NGjiOYEzPTh|NESwNS=>
MCF7 M2X1PGZ2dmO2aX;uJGF{e2G7 M1nSUVUh|ryP NInKSHkzPCCq MlLRSG1UVw>? NXn1bJhETGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> MX6yOVg{PDRyMR?=
MCF7 M2i0RWZ2dmO2aX;uJGF{e2G7 NFmw[pI2KM7:TR?= MV2yOEBp Mof6SG1UVw>? M3PV[mlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlEhX2GoMT;DbZAy M1fuNVI2QDN2NECx
MCF7 MoTtSpVv[3Srb36gRZN{[Xl? MV61JO69VQ>? M2q4W|I1KGh? M362[2ROW09? M1jYWGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= M3S1c|I2QDN2NECx
MDA-MB-231 M{TBVmZ2dmO2aX;uJGF{e2G7 NX[zemo4PSEQvF2= NHP0UmkzPCCq NILOTIpFVVOR MX\E[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ MYeyOVg{PDRyMR?=
MDA-MB-231 MUjGeY5kfGmxbjDBd5NigQ>? NU\ZTXVrOSEQvF2= NIPheWMzPCCq MUPEUXNQ MnewTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|I> NVjtPXhtOjV6M{S0NFE>
MDA-MB-231 M3S0fmZ2dmO2aX;uJGF{e2G7 NXrNc5RiPSEQvF2= M1fvTlI1KGh? NILTSVhFVVOR M1rweGRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= MV[yOVg{PDRyMR?=
MDA-MB-231 M2nobGZ2dmO2aX;uJGF{e2G7 M4XvdlUh|ryP M4HhO|I1KGh? NF;WNpJFVVOR MkjtTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> NFfZV3EzPTh|NESwNS=>
MDA-MB-231 MXrGeY5kfGmxbjDBd5NigQ>? MXO1JO69VQ>? MnjTNlQhcA>? Mnf4SG1UVw>? MV7JcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEK3JGtqeDF? NEjX[ZUzPTh|NESwNS=>
MDA-MB-231 M{LzSGZ2dmO2aX;uJGF{e2G7 M2jvWlUh|ryP Ml\VNlQhcA>? NFq5eohFVVOR MnLnTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIIC1Ny=> MX6yOVg{PDRyMR?=
MCF7 NYr0eVZ[SXCxcITvd4l{KEG|c3H5 MVe1JO69VQ>? MYqyOEBp MWrEUXNQ M{G1V2lv\HWlZYOgZZBweHSxdHnjJIRm[XSq MlztNlU5OzR2MEG=
MDA-MB-231 NIXwRXlCeG:ydH;zbZMhSXO|YYm= Mof0OUDPxE1? M37jflI1KGh? MVPEUXNQ MWTJcoR2[2W|IHHwc5B1d3SrYzDk[YF1cA>? NH73d2czPTh|NESwNS=>
MCF7 NWXI[JhtTnWwY4Tpc44hSXO|YYm= NHzXOlMyKM7:TR?= NYG1NnNIPzJiaB?= M4e5S2ROW09? NEjVR4ZKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= MXKyOVg{PDRyMR?=
MDA-MB-231 MlvnSpVv[3Srb36gRZN{[Xl? M2nlbFEh|ryP NICzeVg4OiCq MoHhSG1UVw>? NFnJSYFKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= MYCyOVg{PDRyMR?=
U-2 OS NVHLTG9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL3WWk2OCEQvF2= NV;zNGJbOjRiaB?= MlfzSG1UVw>? MV3JR|UxRTF4Lk[g{txO MofqNlU4QTJ6MUG=
MG-63 NHjiNItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUi1NEDPxE1? NH6xOXUzPCCq MXjEUXNQ M{jFNGlEPTB;OT61JO69VQ>? MYqyOVc6OjhzMR?=
U-2 OS NEXZSHlCeG:ydH;zbZMhSXO|YYm= NXTORmJTPSEQvF2= NFrjWFUzPCCq MYPEUXNQ NEjCbppKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp MVuyOVc6OjhzMR?=
MG-63 Mn3JRZBweHSxc3nzJGF{e2G7 MU[1JO69VQ>? NH71RWEzPCCq NYrseJlDTE2VTx?= NWXP[FVEUW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>? M3P3SlI2Pzl{OEGx
U-2 OS NYLZeIJjTnWwY4Tpc44hSXO|YYm= NFztbYY2KM7:TR?= M3KwcFI1KGh? NX3TSVNnTE2VTx?= MmfiVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MX:yOVc6OjhzMR?=
MG-63 MVvGeY5kfGmxbjDBd5NigQ>? M2L1OlUh|ryP NFm3[mszPCCq M3jFb2ROW09? NXzhdplzWHKxbX;0[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq M3vmXFI2Pzl{OEGx
PANC-1 M3qwe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoniOVAh|ryP MknzNlQhcA>? NVrIO3ZxTE2VTx?= NFfaN|VKSzVyPUeuNUDPxE1? NFvNfpQzPTZ|MkKyOS=>
BxPC-3 M4LlV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTQNJBtPTBizszN M{i2SVI1KGh? MkXtSG1UVw>? MoOwTWM2OD14Lkig{txO MmrDNlU3OzJ{MkW=
PANC-1 MWDGeY5kfGmxbjDBd5NigQ>? NX7reZN{PSEQvF2= M{TtT|I1KGh? NIOwc29FVVOR NHv4SYNKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NFTaZ|kzPTZ|MkKyOS=>
BxPC-3 NX3WXlB1TnWwY4Tpc44hSXO|YYm= Mm\pOUDPxE1? NEm3W|gzPCCq NIfzbIZFVVOR NFrQVY1KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NETqVlczPTZ|MkKyOS=>
PANC-1 MnOySpVv[3Srb36gRZN{[Xl? M3jTelUh|ryP M4KzSFI1KGh? NGjqZXhFVVOR M1PlTGlv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp NFfT[GszPTZ|MkKyOS=>
BxPC-3 NH3Rd4FHfW6ldHnvckBCe3OjeR?= NXj1fGQyPSEQvF2= MWKyOEBp M2PPN2ROW09? M{TGcWlv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MXKyOVY{OjJ{NR?=
SKOV3 NEjNWIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;XWFExOCEQvF2= M4j3fFI1KGh? NV7reJBSTE2VTx?= Mo\CTWM2OD1{MD60PEDPxE1? NX34WpIxOjV4MkS3OVA>
OVCAR4 NFrkfm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXmxNFAh|ryP M2L1UVI1KGh? M4PHeWROW09? M33mV2lEPTB;MkKuNVMh|ryP M2XZdFI2PjJ2N{Ww
SKOV3 MkLqSpVv[3Srb36gRZN{[Xl? NXrmd|lbPSEQvF2= M2\wSFczKGh? M3rnXmROW09? MUfJcoR2[2W|IFeyM20h[XK{ZYP0 Mk\ENlU3OjR5NUC=
OVCAR4 MV3GeY5kfGmxbjDBd5NigQ>? M2jrWFUh|ryP M1LrZVczKGh? NGTXdXpFVVOR MU\JcoR2[2W|IFeyM20h[XK{ZYP0 M4\mflI2PjJ2N{Ww
SKOV3 MUnBdI9xfG:|aYOgRZN{[Xl? MYC1JO69VQ>? NVy0SIp5OjRiaB?= MkPMSG1UVw>? MmjMTY5lfWOnczDhdI9xfG:|aYO= MX6yOVYzPDd3MB?=
OVCAR4 M3TQfmFxd3C2b4Ppd{BCe3OjeR?= NXH1bGc3PSEQvF2= MoXENlQhcA>? MWHEUXNQ M4D4b2lv\HWlZYOgZZBweHSxc3nz MX6yOVYzPDd3MB?=
AGS MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv5XFMzPSEQvF2= M13vOlI1KGh? MkfnSG1UVw>? NVXLblVJUUN3ME2xPU4xQSEQvF2= MoDHNlU3ODl7MkO=
NCI-N78 MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnNdVczPSEQvF2= M3LIO|I1KGh? M3y4dWROW09? MnLuTWM2OD1{Nj6zN{DPxE1? NHTOO|UzPTZyOUmyNy=>
AGS NWLXOXpuSXCxcITvd4l{KEG|c3H5 NV75UIhJPSEQvF2= NUe3[GhjOjRiaB?= NYn3[W1uTE2VTx?= NFLN[GhKdmS3Y3XzJIFxd3C2b4Ppdy=> MXWyOVYxQTl{Mx?=
NCI-N78 NFTKfY5CeG:ydH;zbZMhSXO|YYm= MVq1JO69VQ>? MVyyOEBp MoT4SG1UVw>? NIj3R5FKdmS3Y3XzJIFxd3C2b4Ppdy=> NWKwTIttOjV4MEm5NlM>
AGS NXrYfZlkTnWwY4Tpc44hSXO|YYm= MnXXOUDPxE1? M4XreFI1KGh? M2PCWGROW09? NYrOO2NWUW6mdXPld{B1cGViYYX0c5Bp[We7 M1PxfFI2PjB7OUKz
NCI-N78 M1vSV2Z2dmO2aX;uJGF{e2G7 MVG1JO69VQ>? MUWyOEBp MljrSG1UVw>? M3jCOmlv\HWlZYOgeIhmKGG3dH;wbIFogQ>? M3XR[FI2PjB7OUKz
HSC-3 M3LpbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LXR|Eh|ryP NGnQU241QCCq NFPyS4JKSzVyPUCuOVQh|ryP M1LZdFI2OzZ4MUSz
GB30 NFvXbnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXKxJO69VQ>? NI\wUo84KGR? MoSwSG1UVw>? Mnq3TWM2OD1yLkCxNUDPxE1? M3XKXVI2OTB4NEK4
GB9 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fuRlEh|ryP MXS3JIQ> NHywfmNFVVOR MkHNTWM2OD1yLkCyOEDPxE1? M{XhT|I2OTB4NEK4
GB169 NIPNclNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mny2NUDPxE1? NInzfHY4KGR? Mn;USG1UVw>? NFHTd3dKSzVyPUCuNFMzKM7:TR?= MWKyOVExPjR{OB?=
T24 Mn\SSpVv[3Srb36gRZN{[Xl? NVPST3pmOSEQvF2= MYS0PEBp M33JUGROW09? MmPRTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NUDjSIVwOjN2MEO2N|M>
RT4 MljPSpVv[3Srb36gRZN{[Xl? NWHMWmdnOSEQvF2= NH33dos1QCCq NGPsS2RFVVOR MmfGTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MkDtNlM1ODN4M{O=
UM-UC-3 MmO5SpVv[3Srb36gRZN{[Xl? NFrSNpIyKM7:TR?= NUK5dI1iPDhiaB?= M3PBXmROW09? M3nmXWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MVyyN|QxOzZ|Mx?=
T24 MYTBdI9xfG:|aYOgRZN{[Xl? MV:zMlE3KM7:TR?= M1XkfVk3KGh? NFSwfI1FVVOR M3i3OGlEPTB;MD6wN|A3KM7:TR?= NFj5VG0zOzRyM{[zNy=>
RT4 M4\HeWFxd3C2b4Ppd{BCe3OjeR?= NWLzcZY2Oy5zNjFOwG0> Mk\nPVYhcA>? NEjQeZNFVVOR MXjJR|UxRTBwMUG5PEDPxE1? MUeyN|QxOzZ|Mx?=
UM-UC-3 NFjRW3pCeG:ydH;zbZMhSXO|YYm= M3zhUFMvOTZizszN NX:1THp2QTZiaB?= M2fEVGROW09? NEDBe4JKSzVyPUCuNFQ1QSEQvF2= MV6yN|QxOzZ|Mx?=
OVCAR-5 M3T1bmZ2dmO2aX;uJGF{e2G7 M2rDNFUxKG6P M2rYSGlvcGmkaYTzJINmdGxibXnndoF1cW:w MoTaNlM{OzR|Mke=
SKOV3ip2 MXLGeY5kfGmxbjDBd5NigQ>? MojjOVAhdk1? Mk[wTY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? NYL0VFdQOjN|M{SzNlc>
S462 NUDpdpFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTxSGRXOTByIN88US=> NXTrc2NMPzJiaB?= NYLHSmRjTE2VTx?= NUjQWndZSXS2ZX71ZZRmeyClZXzsJIdzd3e2aB?= MoPPNlM{OjhzMUS=
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CCRF-CEM NXzBcGtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC3d5B5OTBizszN NELjOFY6PiCq NFX5T49KSzVyPUCuNFk1KM7:TR?= NXjaSWlzOjBzMEizN|g>
Kasumi-1 M1zwTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrnNVAh|ryP NEfTVo46PiCq MUnJR|UxRTBwMUCzJO69VQ>? NFruSIIzODFyOEOzPC=>
Karpas-299 M1e5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGm3RpcyOCEQvF2= MnTiPVYhcA>? MV7JR|UxRTBwMEO4JO69VQ>? MXqyNFExQDN|OB?=
Ramos-RA1 NWf2[Y52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTHNVAh|ryP MWi5OkBp M{TRXGlEPTB;MD6xNlch|ryP M4e5eFIxOTB6M{O4

... 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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