Alisertib (MLN8237)

Alisertib (MLN8237)は一種の選択性オーロラ(Aurora )A阻害剤で、無細胞試験でIC50値が1.2 nMです。Alisertib (MLN8237)はオーロラAに作用する選択性はオーロラ Bに作用する選択性より200倍以上が高くなります。臨床3期。

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Alisertib (MLN8237) 化学構造
分子量: 518.92

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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)は一種の選択性オーロラ(Aurora )A阻害剤で、無細胞試験でIC50値が1.2 nMです。Alisertib (MLN8237)はオーロラAに作用する選択性はオーロラ Bに作用する選択性より200倍以上が高くなります。臨床3期。
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 Moi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLXOmg4OC53IN88US=> NXO0dYhCPzJiaB?= NUmyd3VUTE2VTx?= NEPyPGlKSzVyPUCuNFQh|ryP M2[0bVI3OTN4Nki0
LS174T MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGwMlUh|ryP Mn7rO|IhcA>? M2GxVWROW09? NEDPeo9KSzVyPUCuNFUh|ryP M322bFI3OTN4Nki0
T84 NUXCZoNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPCSGQxNjVizszN NF;CRo84OiCq MlTISG1UVw>? NWfldGZ6UUN3ME2wMlA6KM7:TR?= MmW1NlYyOzZ4OES=
LS180 NFnTS3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLyXWZjOC53IN88US=> M2WyTFczKGh? MoDWSG1UVw>? MlviTWM2OD1zIN88US=> NEPUeY0zPjF|Nk[4OC=>
SW948 NWfB[5hZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjuRnVROC53IN88US=> NEjCSG04OiCq MYTEUXNQ NGXFW4FKSzVyPUGg{txO NXLVW5ZjOjZzM{[2PFQ>
HCT15 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIq0bokxNjVizszN M4my[|czKGh? MXrEUXNQ MknKTWM2ODxyLkSg{txO NFjvUGozPjF|Nk[4OC=>
DLD-1 NUK4PIpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFflUnAxNjVizszN MnrkO|IhcA>? M2[yPGROW09? MXTJR|UxRDBwODFOwG0> MVqyOlE{PjZ6NB?=
MIP-101 MnP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYX2bGtXOC53IN88US=> NUfKSWg4PzJiaB?= M1fhTGROW09? NWWzZ5dbUUN3ME2xJO69VQ>? M4X6XFI3OTN4Nki0
SNU1544 M3TOU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUGwMlUh|ryP MWe3NkBp MoP1SG1UVw>? Ml31TWM2OD1zIN88US=> NUjXOFVqOjZzM{[2PFQ>
OCI-Ly10 NFroeHREgXSxdH;4bYMhSXO|YYm= M4\t[FczKGh? NFHPbYJFVVOR NEPzOXdKSzVyPUCuNFU5KM7:TR?= M3jaT|I2QDd6M{Ox
SU-DHL2 NEDmTHhEgXSxdH;4bYMhSXO|YYm= MYS3NkBp MkLLSG1UVw>? NYX0UGNkUUN3ME2wMlAyKM7:TR?= MkfJNlU5Pzh|M{G=
OCI-LY7 Mly4R5l1d3SxeHnjJGF{e2G7 NFzOU3A4OiCq NEjQNG9FVVOR Mn7JTWM2OD1yLkC4NUDPxE1? NWrY[JkyOjV6N{izN|E>
SU-DHL6 NULieYtwS3m2b4TvfIlkKEG|c3H5 NITxcWs4OiCq MXHEUXNQ MorhTWM2OD1yLkS4NkDPxE1? NH\zNnczPTh5OEOzNS=>
Jeko-1 M3OyXmN6fG:2b4jpZ{BCe3OjeR?= NFXwW2Y4OiCq NY\ReWtVTE2VTx?= NViyTFJtUUN3ME2wMlAzQSEQvF2= Mlz0NlU5Pzh|M{G=
JVM-2 NGjXd4xEgXSxdH;4bYMhSXO|YYm= M3XmU|czKGh? MX7EUXNQ MofrTWM2OD1yLkCxJO69VQ>? MXSyOVg4QDN|MR?=
Rec-1 M1LpbWN6fG:2b4jpZ{BCe3OjeR?= M{LRTlczKGh? M1;YcmROW09? NITtNm1KSzVyPUCuNFg4KM7:TR?= NF\seWIzPTh5OEOzNS=>
Z-138 NVfYSGYxS3m2b4TvfIlkKEG|c3H5 NWnifZppPzJiaB?= M{TtOGROW09? Mnf2TWM2OD1yLkCxN{DPxE1? M1;0cFI2QDd6M{Ox
H9 MXPDfZRwfG:6aXOgRZN{[Xl? MXy3NkBp MVnEUXNQ MnvUTWM2OD1yLk[g{txO MX:yOVg4QDN|MR?=
HH NFntNnhEgXSxdH;4bYMhSXO|YYm= NIrweIc4OiCq M1Pp[2ROW09? MnfDTWM2OD1yLkeg{txO MYCyOVg4QDN|MR?=
DND41 M2fTeGN6fG:2b4jpZ{BCe3OjeR?= M2L4OVczKGh? MmK1SG1UVw>? M{TFc2lEPTB;MD6xJO69VQ>? NF7xeXIzPTh5OEOzNS=>
CCL119 NHruTlhEgXSxdH;4bYMhSXO|YYm= MkTaO|IhcA>? M{jkXWROW09? NFrhTYlKSzVyPUCuNFYzKM7:TR?= NGDBV|MzPTh5OEOzNS=>
J.Cam 1.6 MorNR5l1d3SxeHnjJGF{e2G7 MnnrO|IhcA>? NFzZXnVFVVOR M2nSRmlEPTB;MD6xNFUh|ryP NX:yd5hkOjV6N{izN|E>
Sup-T1 M3G1O2N6fG:2b4jpZ{BCe3OjeR?= M4PtOVczKGh? NIe4[IVFVVOR MXXJR|UxRTJwMUSyJO69VQ>? NWXuSYhnOjV6N{izN|E>
Tib 152 M{frdWN6fG:2b4jpZ{BCe3OjeR?= NVr3U4V4PzJiaB?= MWrEUXNQ M{j2cGlEPTB;MD64JO69VQ>? M3vGelI2QDd6M{Ox
MCF7 MnLaSpVv[3Srb36gRZN{[Xl? NUDK[HlYPSEQvF2= NWHoTHRYOjRiaB?= Mm\pSG1UVw>? NF3leZJKdmS3Y3XzJGczN01iYYLy[ZN1 M3XkblI2QDN2NECx
MDA-MB-231 NHS5coxHfW6ldHnvckBCe3OjeR?= NGri[nQ2KM7:TR?= MV:yOEBp NInZNYZFVVOR NXPPZ5dqUW6mdXPld{BIOy:PIHHydoV{fA>? NH70c4ozPTh|NESwNS=>
MCF7 MVTGeY5kfGmxbjDBd5NigQ>? NV3pW|BZPSEQvF2= NF3TN2czPCCq Ml\rSG1UVw>? MVTE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ NYjxR3lbOjV6M{S0NFE>
MCF7 MnrySpVv[3Srb36gRZN{[Xl? NX;PZZVRPSEQvF2= NHXzUVYzPCCq NF;4bplFVVOR NH;p[GpF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NImwXmYzPTh|NESwNS=>
MCF7 M4fGfWZ2dmO2aX;uJGF{e2G7 NX3tR494PSEQvF2= Mlr1NlQhcA>? NG[xclJFVVOR MX\E[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz NEDLO3kzPTh|NESwNS=>
MCF7 NVHvO4kxTnWwY4Tpc44hSXO|YYm= MnHOOUDPxE1? MXWyOEBp M3jHPWROW09? MnvFTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> NEj5bXMzPTh|NESwNS=>
MCF7 NIS5OJpHfW6ldHnvckBCe3OjeR?= MkXROUDPxE1? M1\melI1KGh? M1q2dGROW09? NFnsWGtKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= M2L6blI2QDN2NECx
MDA-MB-231 NUHNdHI{TnWwY4Tpc44hSXO|YYm= M2fR[|Uh|ryP M3fPS|I1KGh? MULEUXNQ M4THeWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsyN0OGQ{K= MV[yOVg{PDRyMR?=
MDA-MB-231 MmrqSpVv[3Srb36gRZN{[Xl? NFLLNmEyKM7:TR?= NIjXOo8zPCCq MY\EUXNQ MWnJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=> NWHMNGUzOjV6M{S0NFE>
MDA-MB-231 MknYSpVv[3Srb36gRZN{[Xl? NXvWVXV5PSEQvF2= NX3EcnZUOjRiaB?= MVvEUXNQ Ml3qSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIHP5Z4xqdiCEMR?= Mn[1NlU5OzR2MEG=
MDA-MB-231 M3rYXGZ2dmO2aX;uJGF{e2G7 NHz1SFE2KM7:TR?= NGe4emQzPCCq NUezcIsxTE2VTx?= NFXsbVJKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFIyKFejZkGvR4lxOQ>? MW[yOVg{PDRyMR?=
MDA-MB-231 NUXE[FJ1TnWwY4Tpc44hSXO|YYm= NU\MSmI1PSEQvF2= MVGyOEBp M4D1WmROW09? NFPBT5hKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= MXmyOVg{PDRyMR?=
MDA-MB-231 MUXGeY5kfGmxbjDBd5NigQ>? M3rJN|Uh|ryP NX7mUZlYOjRiaB?= NUDL[phqTE2VTx?= M3[1U2lv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwOVM> MYCyOVg{PDRyMR?=
MCF7 MVvBdI9xfG:|aYOgRZN{[Xl? NF\Fe4Q2KM7:TR?= M1;rTVI1KGh? MWXEUXNQ Mkn4TY5lfWOnczDhdI9xfG:2aXOg[IVifGh? NFGyTFMzPTh|NESwNS=>
MDA-MB-231 NH7RflNCeG:ydH;zbZMhSXO|YYm= NWXwc4lQPSEQvF2= NX3qS|gzOjRiaB?= NVS4Smx3TE2VTx?= NYCzNmVTUW6mdXPld{BieG:ydH;0bYMh\GWjdHi= NVnWU3htOjV6M{S0NFE>
MCF7 M2fSfmZ2dmO2aX;uJGF{e2G7 MmPGNUDPxE1? NVHDWmo3PzJiaB?= NGnDS2pFVVOR NGC4U4RKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= NV6xbpVYOjV6M{S0NFE>
MDA-MB-231 MlfZSpVv[3Srb36gRZN{[Xl? MWKxJO69VQ>? NGXVXVA4OiCq M{\xWGROW09? MmLPTY5lfWOnczDheZRweGijZ3njJIRm[XSq MlezNlU5OzR2MEG=
U-2 OS M1zLVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DIT|UxKM7:TR?= MVmyOEBp MWjEUXNQ NYewdJIxUUN3ME2xOk43KM7:TR?= MkHpNlU4QTJ6MUG=
MG-63 NY\0N4dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkCxOVAh|ryP MVGyOEBp NXjRdFJiTE2VTx?= MkjWTWM2OD17LkWg{txO MV:yOVc6OjhzMR?=
U-2 OS NIXFUI5CeG:ydH;zbZMhSXO|YYm= MVW1JO69VQ>? NUnLd4ljOjRiaB?= M2jjSmROW09? Mlu4TY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> NUPkXlVYOjV5OUK4NVE>
MG-63 MVPBdI9xfG:|aYOgRZN{[Xl? MWm1JO69VQ>? NIT5N2szPCCq MofjSG1UVw>? MlSyTY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> MoHhNlU4QTJ6MUG=
U-2 OS NHn1T2FHfW6ldHnvckBCe3OjeR?= NV;XO5g5PSEQvF2= NH\xeG8zPCCq MYDEUXNQ NH\1O5ZRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? NXfmRZFHOjV5OUK4NVE>
MG-63 MmixSpVv[3Srb36gRZN{[Xl? NYLmXIJvPSEQvF2= M3H4U|I1KGh? NILDbpRFVVOR NGjVcVBRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? NEGwboozPTd7MkixNS=>
PANC-1 M1LX[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;BZos2OCEQvF2= NUfUNYFYOjRiaB?= MYLEUXNQ MX;JR|UxRTdwMTFOwG0> NIPUdW8zPTZ|MkKyOS=>
BxPC-3 M{nBPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVu1NEDPxE1? NUfJPXY3OjRiaB?= NHvGVpNFVVOR MY\JR|UxRTZwODFOwG0> NGXnPHAzPTZ|MkKyOS=>
PANC-1 MlH5SpVv[3Srb36gRZN{[Xl? MX21JO69VQ>? MWKyOEBp NFrwZ4hFVVOR M3\qPWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hTzJxTTDwbIF{\Q>? MVSyOVY{OjJ{NR?=
BxPC-3 MWHGeY5kfGmxbjDBd5NigQ>? NVfqOm86PSEQvF2= NYDGZ5ZVOjRiaB?= NWnt[ZduTE2VTx?= MWnJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> MmnQNlU3OzJ{MkW=
PANC-1 Ml72SpVv[3Srb36gRZN{[Xl? NVT4XHF4PSEQvF2= M2\yUVI1KGh? MUfEUXNQ NUTjNIxVUW6mdXPld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? NGnOPJYzPTZ|MkKyOS=>
BxPC-3 MlTtSpVv[3Srb36gRZN{[Xl? MXm1JO69VQ>? Ml3tNlQhcA>? NYTm[ZhITE2VTx?= NIntbpJKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? NXzGV4ZOOjV4M{KyNlU>
SKOV3 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4CwW|ExOCEQvF2= MlSzNlQhcA>? NVLBNllkTE2VTx?= M3LhXmlEPTB;MkCuOFgh|ryP MojjNlU3OjR5NUC=
OVCAR4 NWD5WGQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWixNFAh|ryP MYCyOEBp MVXEUXNQ NYX6ZlJbUUN3ME2yNk4yOyEQvF2= MWqyOVYzPDd3MB?=
SKOV3 MXzGeY5kfGmxbjDBd5NigQ>? MUO1JO69VQ>? MkjWO|IhcA>? MUnEUXNQ NXT4eWRFUW6mdXPld{BIOi:PIHHydoV{fA>? NGrB[G0zPTZ{NEe1NC=>
OVCAR4 M3OwW2Z2dmO2aX;uJGF{e2G7 NXzuXJBLPSEQvF2= NWO2OJd4PzJiaB?= NIrBZY5FVVOR MmXvTY5lfWOnczDHNk9OKGG{cnXzeC=> NVvXWWN[OjV4MkS3OVA>
SKOV3 MUPBdI9xfG:|aYOgRZN{[Xl? NWCwcoRyPSEQvF2= MYSyOEBp NXfCbIRLTE2VTx?= NXTWcW9WUW6mdXPld{BieG:ydH;zbZM> NFv3RmgzPTZ{NEe1NC=>
OVCAR4 NIf5RphCeG:ydH;zbZMhSXO|YYm= MkDDOUDPxE1? MmHXNlQhcA>? NHTyR3ZFVVOR MoLsTY5lfWOnczDhdI9xfG:|aYO= MkHVNlU3OjR5NUC=
AGS M4DQ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDIbpZ{OjVizszN NGTIb28zPCCq MkK0SG1UVw>? NHTKVotKSzVyPUG5MlA6KM7:TR?= MonTNlU3ODl7MkO=
NCI-N78 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLjNlUh|ryP MmnJNlQhcA>? NGLJb2ZFVVOR MlqzTWM2OD1{Nj6zN{DPxE1? MoCwNlU3ODl7MkO=
AGS Mn\VRZBweHSxc3nzJGF{e2G7 M3PsdVUh|ryP NIXPPY8zPCCq M3n3bGROW09? Ml\RTY5lfWOnczDhdI9xfG:|aYO= MUiyOVYxQTl{Mx?=
NCI-N78 NY\pRolFSXCxcITvd4l{KEG|c3H5 M1X3UlUh|ryP NGLYWYIzPCCq NUn6XlgyTE2VTx?= MXfJcoR2[2W|IHHwc5B1d3Orcx?= MkjONlU3ODl7MkO=
AGS NU\Z[ZFqTnWwY4Tpc44hSXO|YYm= M2LtN|Uh|ryP NUTLZWExOjRiaB?= MkDSSG1UVw>? NVzRZoZjUW6mdXPld{B1cGViYYX0c5Bp[We7 NHfXUmQzPTZyOUmyNy=>
NCI-N78 MYDGeY5kfGmxbjDBd5NigQ>? MnzoOUDPxE1? MmfwNlQhcA>? M{fNT2ROW09? M1zlR2lv\HWlZYOgeIhmKGG3dH;wbIFogQ>? M{n6O|I2PjB7OUKz
HSC-3 NGLsRVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjtclgyKM7:TR?= NIrY[og1QCCq NFTa[2hKSzVyPUCuOVQh|ryP MlL4NlU{PjZzNEO=
GB30 MmrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILlSlYyKM7:TR?= NV3QWXBYPyCm MUjEUXNQ Mnm3TWM2OD1yLkCxNUDPxE1? NYLWVIZtOjVzME[0Nlg>
GB9 NF[zXGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4riTFEh|ryP NFnTTWo4KGR? M1u5d2ROW09? NFvR[GlKSzVyPUCuNFI1KM7:TR?= NEL2cW4zPTFyNkSyPC=>
GB169 Ml7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PwTFEh|ryP NFPZbZM4KGR? MmHySG1UVw>? MlzsTWM2OD1yLkCzNkDPxE1? MX6yOVExPjR{OB?=
T24 MnXsSpVv[3Srb36gRZN{[Xl? NXe3WIhEOSEQvF2= MWi0PEBp NEnMUVZFVVOR MXXJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NHS0NVczOzRyM{[zNy=>
RT4 MY\GeY5kfGmxbjDBd5NigQ>? NFjhOYUyKM7:TR?= M13UdFQ5KGh? NHOwdpZFVVOR Ml;6TY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NVe0PYNtOjN2MEO2N|M>
UM-UC-3 NXTJ[4R{TnWwY4Tpc44hSXO|YYm= NFfPV5IyKM7:TR?= NF7pZ|M1QCCq M4jJb2ROW09? M13FSGlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M3y4UlI{PDB|NkOz
T24 NYDXNYJ{SXCxcITvd4l{KEG|c3H5 NYHLbGVMOy5zNjFOwG0> Mm\qPVYhcA>? MVLEUXNQ MknFTWM2OD1yLkCzNFYh|ryP NI\qZXgzOzRyM{[zNy=>
RT4 MorNRZBweHSxc3nzJGF{e2G7 NWTYRY1qOy5zNjFOwG0> M3TacVk3KGh? MXrEUXNQ NWXMVolnUUN3ME2wMlEyQThizszN MWmyN|QxOzZ|Mx?=
UM-UC-3 MUjBdI9xfG:|aYOgRZN{[Xl? NEHqTIo{NjF4IN88US=> M4ez[|k3KGh? NHXJbItFVVOR MlTBTWM2OD1yLkC0OFkh|ryP MoLQNlM1ODN4M{O=
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COG-LL-317 MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD0NVAh|ryP M4PDNVk3KGh? M13oS2lEPTB;MD6wOFch|ryP NHXPRnIzODFyOEOzPC=>
RS4-11 NWLwfmM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLjNVAh|ryP NFrFUFA6PiCq NV;6TZFYUUN3ME2wMlAyQCEQvF2= M2Xw[|IxOTB6M{O4
MOLT-4 Mm\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkKwNVAh|ryP M4HIflk3KGh? MlPmTWM2OD1yLkCyOkDPxE1? MVSyNFExQDN|OB?=
CCRF-CEM MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKxNEDPxE1? MlnzPVYhcA>? NFH6UoZKSzVyPUCuNFk1KM7:TR?= M3HPO|IxOTB6M{O4
Kasumi-1 NImzUnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:xNEDPxE1? NYTrNIloQTZiaB?= NHX1SmhKSzVyPUCuNVA{KM7:TR?= NXrzNlBWOjBzMEizN|g>
Karpas-299 NWn2ZopnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLkXFMyOCEQvF2= NV;UU|h4QTZiaB?= NUjsd5diUUN3ME2wMlA{QCEQvF2= NFvmTmEzODFyOEOzPC=>
Ramos-RA1 M1HJUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrGNVAh|ryP NVn5N5RyQTZiaB?= NH;MSWNKSzVyPUCuNVI4KM7:TR?= NVn0PFV4OjBzMEizN|g>

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 27 mg/mL (52.03 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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-

文献中の引用 (46)

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.

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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