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 M2XjRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTLfG0xNjVizszN MX63NkBp MmnxSG1UVw>? MV;JR|UxRTBwMESg{txO NIPZNpYzPjF|Nk[4OC=>
LS174T MlnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTKNE42KM7:TR?= NFX4ZYE4OiCq M3XsbWROW09? MlvpTWM2OD1yLkC1JO69VQ>? M3nOWVI3OTN4Nki0
T84 NGfvTJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKwMlUh|ryP MXe3NkBp NXvIUpNVTE2VTx?= MVfJR|UxRTBwMEmg{txO NGf3WG0zPjF|Nk[4OC=>
LS180 NEPUcFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4n4XFAvPSEQvF2= Mm\wO|IhcA>? MonRSG1UVw>? M{LiTWlEPTB;MTFOwG0> NVPnNYx7OjZzM{[2PFQ>
SW948 M1zGWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fzcFAvPSEQvF2= MWi3NkBp NVz6WoRPTE2VTx?= MoDWTWM2OD1zIN88US=> M4nKeFI3OTN4Nki0
HCT15 MnfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTWNE42KM7:TR?= NITCbGk4OiCq NGHNeIlFVVOR NX3SUFhNUUN3MEywMlQh|ryP MXyyOlE{PjZ6NB?=
DLD-1 NF33WXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImyVmoxNjVizszN MXK3NkBp MXXEUXNQ MXPJR|UxRDBwODFOwG0> Mo\jNlYyOzZ4OES=
MIP-101 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDYNE42KM7:TR?= M1LPTlczKGh? M17XWGROW09? MnXFTWM2OD1zIN88US=> MVeyOlE{PjZ6NB?=
SNU1544 M4jHemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\CNE42KM7:TR?= NWKyfFM3PzJiaB?= M13Qe2ROW09? M3nVXGlEPTB;MTFOwG0> NFPNV4MzPjF|Nk[4OC=>
OCI-Ly10 MYrDfZRwfG:6aXOgRZN{[Xl? MWi3NkBp NIrKR2lFVVOR NVfGclI1UUN3ME2wMlA2QCEQvF2= NF;RNmszPTh5OEOzNS=>
SU-DHL2 NWPnTnd[S3m2b4TvfIlkKEG|c3H5 M2Wwe|czKGh? M4ixPWROW09? NXnYTWlQUUN3ME2wMlAyKM7:TR?= NGTyRZgzPTh5OEOzNS=>
OCI-LY7 NYnXdYJ{S3m2b4TvfIlkKEG|c3H5 MVG3NkBp MmH1SG1UVw>? NXnpd2ZVUUN3ME2wMlA5OSEQvF2= M3S1flI2QDd6M{Ox
SU-DHL6 MlXBR5l1d3SxeHnjJGF{e2G7 NIfOcXc4OiCq MWnEUXNQ MWXJR|UxRTBwNEiyJO69VQ>? MnrrNlU5Pzh|M{G=
Jeko-1 NGPGOo1EgXSxdH;4bYMhSXO|YYm= MoO0O|IhcA>? M2TVRWROW09? MWDJR|UxRTBwMEK5JO69VQ>? MXeyOVg4QDN|MR?=
JVM-2 M4S2SWN6fG:2b4jpZ{BCe3OjeR?= NELX[Yk4OiCq MXnEUXNQ MXfJR|UxRTBwMEGg{txO MX6yOVg4QDN|MR?=
Rec-1 M4fZSWN6fG:2b4jpZ{BCe3OjeR?= MXq3NkBp MkLJSG1UVw>? Ml33TWM2OD1yLkC4O{DPxE1? MXSyOVg4QDN|MR?=
Z-138 MnjnR5l1d3SxeHnjJGF{e2G7 NVPvVZFkPzJiaB?= NF7NNYdFVVOR M4DWPWlEPTB;MD6wNVMh|ryP NFXXTpQzPTh5OEOzNS=>
H9 NVPUcYpbS3m2b4TvfIlkKEG|c3H5 NHn6Vlc4OiCq NGW3dZlFVVOR NYnFPZJjUUN3ME2wMlYh|ryP NX\xcItTOjV6N{izN|E>
HH MlznR5l1d3SxeHnjJGF{e2G7 NIjzfWs4OiCq NUfGelFvTE2VTx?= M4faW2lEPTB;MD63JO69VQ>? MX6yOVg4QDN|MR?=
DND41 NH;SNFhEgXSxdH;4bYMhSXO|YYm= NF\nRlc4OiCq MULEUXNQ NYn2b|U2UUN3ME2wMlEh|ryP NGPtR2ozPTh5OEOzNS=>
CCL119 NIr5WY1EgXSxdH;4bYMhSXO|YYm= MX:3NkBp MmjwSG1UVw>? MVvJR|UxRTBwME[yJO69VQ>? NUjOSm02OjV6N{izN|E>
J.Cam 1.6 MVfDfZRwfG:6aXOgRZN{[Xl? M3jDN|czKGh? MnH4SG1UVw>? M3v1dGlEPTB;MD6xNFUh|ryP MlHlNlU5Pzh|M{G=
Sup-T1 MYjDfZRwfG:6aXOgRZN{[Xl? MYG3NkBp M2HJUmROW09? M3TzS2lEPTB;Mj6xOFIh|ryP NWO0e2lzOjV6N{izN|E>
Tib 152 MkezR5l1d3SxeHnjJGF{e2G7 M33DOFczKGh? M4TZXGROW09? MVrJR|UxRTBwODFOwG0> NFT3PYYzPTh5OEOzNS=>
MCF7 M2nKbWZ2dmO2aX;uJGF{e2G7 NHq2eFM2KM7:TR?= M13icVI1KGh? NXW4SWs1TE2VTx?= MXfJcoR2[2W|IFeyM20h[XK{ZYP0 MmHlNlU5OzR2MEG=
MDA-MB-231 NEjH[plHfW6ldHnvckBCe3OjeR?= Ml\JOUDPxE1? MV2yOEBp M3LRPWROW09? Mk[xTY5lfWOnczDHN{9OKGG{cnXzeC=> M3PxfFI2QDN2NECx
MCF7 NYTCdFBZTnWwY4Tpc44hSXO|YYm= NIjNOlU2KM7:TR?= MkTuNlQhcA>? Mn2zSG1UVw>? MW\E[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ NVO1ZpQyOjV6M{S0NFE>
MCF7 Mlf5SpVv[3Srb36gRZN{[Xl? M2L1PFUh|ryP NV7FPGR2OjRiaB?= MUjEUXNQ NELsWZZF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NYTUco17OjV6M{S0NFE>
MCF7 M12xeGZ2dmO2aX;uJGF{e2G7 NFzZXJA2KM7:TR?= MUKyOEBp MoXXSG1UVw>? MVTE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz MX[yOVg{PDRyMR?=
MCF7 M3rJUWZ2dmO2aX;uJGF{e2G7 NF7BOI42KM7:TR?= NH20SG4zPCCq NYe3UlFCTE2VTx?= MnS2TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> NFT1fnkzPTh|NESwNS=>
MCF7 NF\ZfodHfW6ldHnvckBCe3OjeR?= NX;IdGpHPSEQvF2= M2CybVI1KGh? MoG0SG1UVw>? MnXYTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz MViyOVg{PDRyMR?=
MDA-MB-231 MVzGeY5kfGmxbjDBd5NigQ>? MluwOUDPxE1? NHXPWVQzPCCq M3LzR2ROW09? MnLmSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|EwS0SFMh?= NUDxdVdiOjV6M{S0NFE>
MDA-MB-231 NVS2b|R7TnWwY4Tpc44hSXO|YYm= NH\HVncyKM7:TR?= Mln6NlQhcA>? MkLCSG1UVw>? NGrmZldKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? MV[yOVg{PDRyMR?=
MDA-MB-231 NIeyfWVHfW6ldHnvckBCe3OjeR?= NFj1O2s2KM7:TR?= MYSyOEBp M4D4emROW09? NYrHZlB[TGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> MlvvNlU5OzR2MEG=
MDA-MB-231 MY\GeY5kfGmxbjDBd5NigQ>? M{H6U|Uh|ryP MmLSNlQhcA>? M1XhWmROW09? NF;iNWZKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFIyKFejZkGvR4lxOQ>? NV;w[XJUOjV6M{S0NFE>
MDA-MB-231 MYTGeY5kfGmxbjDBd5NigQ>? NEfMWFA2KM7:TR?= MViyOEBp MYDEUXNQ MVfJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEK3JGtqeDF? Mn3FNlU5OzR2MEG=
MDA-MB-231 M{DTZWZ2dmO2aX;uJGF{e2G7 NUexZldqPSEQvF2= M2rZbFI1KGh? M13vcGROW09? MnSzTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIIC1Ny=> M333PVI2QDN2NECx
MCF7 M{W4Z2Fxd3C2b4Ppd{BCe3OjeR?= NYroeoFWPSEQvF2= MmnRNlQhcA>? MX7EUXNQ M2fs[Wlv\HWlZYOgZZBweHSxdHnjJIRm[XSq M2G2fVI2QDN2NECx
MDA-MB-231 MUnBdI9xfG:|aYOgRZN{[Xl? MUm1JO69VQ>? M4f1RVI1KGh? M1\3bmROW09? NHnGZ2dKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= MnzUNlU5OzR2MEG=
MCF7 MUTGeY5kfGmxbjDBd5NigQ>? NF7nXoMyKM7:TR?= M3O3OFczKGh? M{LRbGROW09? NYrpfWIzUW6mdXPld{BifXSxcHjh[4lkKGSnYYTo M{H2bFI2QDN2NECx
MDA-MB-231 NHnoeXdHfW6ldHnvckBCe3OjeR?= NUjvcpgzOSEQvF2= M4nnZlczKGh? MVvEUXNQ M3yydWlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= NV\4PIg2OjV6M{S0NFE>
U-2 OS NIjUO4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[1NEDPxE1? NYDjOZl7OjRiaB?= MYfEUXNQ NV:5SGcyUUN3ME2xOk43KM7:TR?= M1K1c|I2Pzl{OEGx
MG-63 M2ewbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLuNY1RPTBizszN NVjnTndkOjRiaB?= M3TPOGROW09? Ml;GTWM2OD17LkWg{txO NF;uToUzPTd7MkixNS=>
U-2 OS MV7BdI9xfG:|aYOgRZN{[Xl? NXTFbI9FPSEQvF2= Mn7qNlQhcA>? M{jucGROW09? M1LnXWlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> NHT0cHczPTd7MkixNS=>
MG-63 MX7BdI9xfG:|aYOgRZN{[Xl? Mlu0OUDPxE1? NVq3c2ROOjRiaB?= M2q4emROW09? MlThTY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> MmTINlU4QTJ6MUG=
U-2 OS MYPGeY5kfGmxbjDBd5NigQ>? Mny2OUDPxE1? MlzVNlQhcA>? MlvQSG1UVw>? MlHyVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp NXzvPHpnOjV5OUK4NVE>
MG-63 M37qXmZ2dmO2aX;uJGF{e2G7 MXS1JO69VQ>? Mo[yNlQhcA>? M13WU2ROW09? NU\QdFhsWHKxbX;0[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq Mlz2NlU4QTJ6MUG=
PANC-1 NGPFN3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFmzT5o2OCEQvF2= NFWxZoUzPCCq M2XScmROW09? M2L4[mlEPTB;Nz6xJO69VQ>? NYr6dZl1OjV4M{KyNlU>
BxPC-3 NULxfG1vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\Qfmk2OCEQvF2= MWCyOEBp MkPPSG1UVw>? M{f6PGlEPTB;Nj64JO69VQ>? M1nyOFI2PjN{MkK1
PANC-1 MYrGeY5kfGmxbjDBd5NigQ>? MofROUDPxE1? M4rXTVI1KGh? M2LkdmROW09? M3XTT2lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hTzJxTTDwbIF{\Q>? M3WzOlI2PjN{MkK1
BxPC-3 NUTjTIFCTnWwY4Tpc44hSXO|YYm= NEWxV3I2KM7:TR?= NGi3TmUzPCCq MY\EUXNQ NFz4N|JKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NFXEVXgzPTZ|MkKyOS=>
PANC-1 NGTQdWpHfW6ldHnvckBCe3OjeR?= NF\3NlE2KM7:TR?= M1vpV|I1KGh? MWPEUXNQ NF;Mb25KdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? MlfRNlU3OzJ{MkW=
BxPC-3 NGTweHlHfW6ldHnvckBCe3OjeR?= MoPKOUDPxE1? MWGyOEBp M1r6emROW09? NICxdYVKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? M3zNRVI2PjN{MkK1
SKOV3 Mn7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\V[|VrOTByIN88US=> MWGyOEBp NHnXUopFVVOR MlzjTWM2OD1{MD60PEDPxE1? MUeyOVYzPDd3MB?=
OVCAR4 M2HkdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P3ZVExOCEQvF2= MV6yOEBp MmW5SG1UVw>? NVPPTXkyUUN3ME2yNk4yOyEQvF2= M3vKOVI2PjJ2N{Ww
SKOV3 MoDjSpVv[3Srb36gRZN{[Xl? MlHhOUDPxE1? NXziU49SPzJiaB?= NYHk[owyTE2VTx?= MmPGTY5lfWOnczDHNk9OKGG{cnXzeC=> Mn;HNlU3OjR5NUC=
OVCAR4 M{LXRmZ2dmO2aX;uJGF{e2G7 M{DwTFUh|ryP NGTS[nk4OiCq NEnxOGlFVVOR Moq4TY5lfWOnczDHNk9OKGG{cnXzeC=> MYeyOVYzPDd3MB?=
SKOV3 NFjRRZlCeG:ydH;zbZMhSXO|YYm= NV24XGNoPSEQvF2= MV[yOEBp NYDobmFVTE2VTx?= M2X1[mlv\HWlZYOgZZBweHSxc3nz NYXHcXA2OjV4MkS3OVA>
OVCAR4 NG\1WW9CeG:ydH;zbZMhSXO|YYm= NFX4W3E2KM7:TR?= NISxN3czPCCq NYC1V4pJTE2VTx?= MYfJcoR2[2W|IHHwc5B1d3Orcx?= MnXaNlU3OjR5NUC=
AGS MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37RNlI2KM7:TR?= NHj1[HUzPCCq MUXEUXNQ NHHk[XJKSzVyPUG5MlA6KM7:TR?= MYOyOVYxQTl{Mx?=
NCI-N78 NFnBbVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP0bWFEOjVizszN M3\G[VI1KGh? NX7uZml6TE2VTx?= Mm\CTWM2OD1{Nj6zN{DPxE1? NUjKdXM1OjV4MEm5NlM>
AGS NG[4ZWZCeG:ydH;zbZMhSXO|YYm= MV[1JO69VQ>? Mnu2NlQhcA>? MlHwSG1UVw>? NUPweZJHUW6mdXPld{BieG:ydH;zbZM> Mlj2NlU3ODl7MkO=
NCI-N78 MlTVRZBweHSxc3nzJGF{e2G7 M{jPU|Uh|ryP MUCyOEBp MYDEUXNQ MlnzTY5lfWOnczDhdI9xfG:|aYO= Mn;sNlU3ODl7MkO=
AGS MkjsSpVv[3Srb36gRZN{[Xl? NHnnOYs2KM7:TR?= M4DrZlI1KGh? Ml3BSG1UVw>? NIf6OVJKdmS3Y3XzJJRp\SCjdYTvdIhi\3l? MoPyNlU3ODl7MkO=
NCI-N78 NH\HelVHfW6ldHnvckBCe3OjeR?= M3PTb|Uh|ryP NWrIVGwzOjRiaB?= NWe5OJhMTE2VTx?= MYDJcoR2[2W|IITo[UBifXSxcHjh[5k> M3HtXFI2PjB7OUKz
HSC-3 MmflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWxJO69VQ>? NHuze2Y1QCCq NHHNd41KSzVyPUCuOVQh|ryP M2T5[|I2OzZ4MUSz
GB30 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv2NUDPxE1? MV[3JIQ> NWHXUXB{TE2VTx?= M4TSTWlEPTB;MD6wNVEh|ryP M37SSlI2OTB4NEK4
GB9 M2nXV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUWxJO69VQ>? Mn[xO{Bl M1TLXGROW09? Mk\uTWM2OD1yLkCyOEDPxE1? NX3LbGhrOjVzME[0Nlg>
GB169 NV\CVlhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml21NUDPxE1? MlLxO{Bl NUDDc2p2TE2VTx?= NEfqTWpKSzVyPUCuNFMzKM7:TR?= MVqyOVExPjR{OB?=
T24 MmO1SpVv[3Srb36gRZN{[Xl? MnfxNUDPxE1? M1LDOFQ5KGh? M3Wzb2ROW09? MVrJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MUKyN|QxOzZ|Mx?=
RT4 NYfVe2ZuTnWwY4Tpc44hSXO|YYm= MoLaNUDPxE1? NELGWWE1QCCq NV;GVFhyTE2VTx?= M3LzOWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MkH6NlM1ODN4M{O=
UM-UC-3 M{\l[mZ2dmO2aX;uJGF{e2G7 MXOxJO69VQ>? MlqwOFghcA>? M2G0TmROW09? M1\remlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M2\pWFI{PDB|NkOz
T24 NX3meFZ5SXCxcITvd4l{KEG|c3H5 NXXUU5JyOy5zNjFOwG0> NGO0b|c6PiCq MkHnSG1UVw>? Mn[5TWM2OD1yLkCzNFYh|ryP NWr2emdnOjN2MEO2N|M>
RT4 Ml;nRZBweHSxc3nzJGF{e2G7 NIrwWYk{NjF4IN88US=> MWm5OkBp NGDrbJBFVVOR M2HROWlEPTB;MD6xNVk5KM7:TR?= M3;yeFI{PDB|NkOz
UM-UC-3 NF\MWmFCeG:ydH;zbZMhSXO|YYm= NXv1cVN{Oy5zNjFOwG0> NV;q[GRUQTZiaB?= M{fZcGROW09? MUHJR|UxRTBwMES0PUDPxE1? MlLVNlM1ODN4M{O=
OVCAR-5 Mn76SpVv[3Srb36gRZN{[Xl? NH35OZA2OCCwTR?= NU\3d4FPUW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NXfIVHhuOjN|M{SzNlc>
SKOV3ip2 Mn:4SpVv[3Srb36gRZN{[Xl? NETmfVU2OCCwTR?= NHe1UHdKdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MX:yN|M{PDN{Nx?=
S462 NH;wZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSxNFAh|ryP MVe3NkBp M2TVVmROW09? Mk\DRZR1\W63YYTld{Bk\WyuIHfyc5d1cA>? MnHZNlM{OjhzMUS=
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CCRF-CEM M1;vemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnVNVAh|ryP MXe5OkBp NVXqdZlCUUN3ME2wMlA6PCEQvF2= NFXZZWYzODFyOEOzPC=>
Kasumi-1 NEm1RnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDCNVAh|ryP Mo\qPVYhcA>? MXTJR|UxRTBwMUCzJO69VQ>? MXqyNFExQDN|OB?=
Karpas-299 NX7TNGtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHkdm9XOTBizszN NYjxfXN6QTZiaB?= MV3JR|UxRTBwMEO4JO69VQ>? MonkNlAyODh|M{i=
Ramos-RA1 NUflUHN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUWxNEDPxE1? MWm5OkBp Mn3jTWM2OD1yLkGyO{DPxE1? M3jiZ|IxOTB6M{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.

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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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