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 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOwMlUh|ryP M{jRWVczKGh? MnjHSG1UVw>? M1GwT2lEPTB;MD6wOEDPxE1? NWXmZWVKOjZzM{[2PFQ>
LS174T NI[3TohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1S3Z|AvPSEQvF2= MoTiO|IhcA>? Mof1SG1UVw>? NI\C[mpKSzVyPUCuNFUh|ryP MX:yOlE{PjZ6NB?=
T84 NEHiWFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED4VVQxNjVizszN MX23NkBp NEHUc5JFVVOR MmD3TWM2OD1yLkC5JO69VQ>? MonHNlYyOzZ4OES=
LS180 M3nxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnW5NE42KM7:TR?= NFPMTW44OiCq M3O5RWROW09? NELiXVZKSzVyPUGg{txO MUKyOlE{PjZ6NB?=
SW948 M1XIcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Dqb|AvPSEQvF2= NYDld|ZyPzJiaB?= NYfNd45ETE2VTx?= NGXvT3dKSzVyPUGg{txO MlLHNlYyOzZ4OES=
HCT15 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKwMlUh|ryP M1r6VVczKGh? NEfVW2dFVVOR M4rocmlEPTB:MD60JO69VQ>? MnP6NlYyOzZ4OES=
DLD-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;5NE42KM7:TR?= MXe3NkBp MYDEUXNQ M{HyZmlEPTB:MD64JO69VQ>? M1HqfVI3OTN4Nki0
MIP-101 MmK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvob5cxNjVizszN M2TKZVczKGh? MVrEUXNQ NF7lOndKSzVyPUGg{txO M{TsWFI3OTN4Nki0
SNU1544 NH;GNWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnwXnExNjVizszN MWK3NkBp NFLlOIlFVVOR NGHHS2JKSzVyPUGg{txO M4nXNVI3OTN4Nki0
OCI-Ly10 MX;DfZRwfG:6aXOgRZN{[Xl? MkHRO|IhcA>? MX\EUXNQ MXrJR|UxRTBwMEW4JO69VQ>? M{XlNFI2QDd6M{Ox
SU-DHL2 MVHDfZRwfG:6aXOgRZN{[Xl? MYK3NkBp NYDRVYlVTE2VTx?= MUTJR|UxRTBwMEGg{txO M4C2O|I2QDd6M{Ox
OCI-LY7 MnHvR5l1d3SxeHnjJGF{e2G7 M1PwclczKGh? MYfEUXNQ NVK5XnVvUUN3ME2wMlA5OSEQvF2= NULYeGtuOjV6N{izN|E>
SU-DHL6 NIXzO2lEgXSxdH;4bYMhSXO|YYm= NH3jWpQ4OiCq MUTEUXNQ MkL1TWM2OD1yLkS4NkDPxE1? NWey[ncyOjV6N{izN|E>
Jeko-1 Mlj3R5l1d3SxeHnjJGF{e2G7 NIfIRoo4OiCq NV;IT4tjTE2VTx?= M1HHR2lEPTB;MD6wNlkh|ryP MYiyOVg4QDN|MR?=
JVM-2 Mn3xR5l1d3SxeHnjJGF{e2G7 Mm\wO|IhcA>? NXXPdXRlTE2VTx?= NWWySoh6UUN3ME2wMlAyKM7:TR?= MViyOVg4QDN|MR?=
Rec-1 NYjiV5BjS3m2b4TvfIlkKEG|c3H5 NGXZUHM4OiCq MkTzSG1UVw>? M1HaOWlEPTB;MD6wPFch|ryP NYnvdoNiOjV6N{izN|E>
Z-138 MV7DfZRwfG:6aXOgRZN{[Xl? MnnyO|IhcA>? Mk\lSG1UVw>? MXjJR|UxRTBwMEGzJO69VQ>? NHHIZXEzPTh5OEOzNS=>
H9 MmPiR5l1d3SxeHnjJGF{e2G7 MlzSO|IhcA>? Mmf2SG1UVw>? NHHRRpFKSzVyPUCuOkDPxE1? MWSyOVg4QDN|MR?=
HH M3e5R2N6fG:2b4jpZ{BCe3OjeR?= MWO3NkBp MVjEUXNQ MoPVTWM2OD1yLkeg{txO NHz2WpYzPTh5OEOzNS=>
DND41 NInjPFVEgXSxdH;4bYMhSXO|YYm= MkPVO|IhcA>? NV\obFZZTE2VTx?= M2rZWWlEPTB;MD6xJO69VQ>? MonHNlU5Pzh|M{G=
CCL119 M3XHXmN6fG:2b4jpZ{BCe3OjeR?= MlrmO|IhcA>? Ml3TSG1UVw>? M325dWlEPTB;MD6wOlIh|ryP NVznZ3hxOjV6N{izN|E>
J.Cam 1.6 M{LmW2N6fG:2b4jpZ{BCe3OjeR?= M1rSb|czKGh? NEi3NWVFVVOR MUnJR|UxRTBwMUC1JO69VQ>? MWWyOVg4QDN|MR?=
Sup-T1 MoDNR5l1d3SxeHnjJGF{e2G7 M125WlczKGh? MoT6SG1UVw>? MYLJR|UxRTJwMUSyJO69VQ>? NXjQc24yOjV6N{izN|E>
Tib 152 MnjjR5l1d3SxeHnjJGF{e2G7 M4DnXFczKGh? M1nxT2ROW09? NEHsb4FKSzVyPUCuPEDPxE1? MUSyOVg4QDN|MR?=
MCF7 NU\o[Wl6TnWwY4Tpc44hSXO|YYm= NYPGZopLPSEQvF2= NVHiNYdLOjRiaB?= NVrzWGZ[TE2VTx?= NGfSZpFKdmS3Y3XzJGczN01iYYLy[ZN1 M{DV[VI2QDN2NECx
MDA-MB-231 M1rSemZ2dmO2aX;uJGF{e2G7 M2PJTFUh|ryP M4fTZlI1KGh? NH7TU|JFVVOR NHrsSJVKdmS3Y3XzJGc{N01iYYLy[ZN1 NGLBVlIzPTh|NESwNS=>
MCF7 NELObHlHfW6ldHnvckBCe3OjeR?= NFvxWWg2KM7:TR?= MVKyOEBp MWDEUXNQ NYjTPFJITGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzFxQ1TDNi=> Mly0NlU5OzR2MEG=
MCF7 Mmq4SpVv[3Srb36gRZN{[Xl? MlGzOUDPxE1? MnvINlQhcA>? MkXwSG1UVw>? NWXCXo9RTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? MnLKNlU5OzR2MEG=
MCF7 Mmr6SpVv[3Srb36gRZN{[Xl? M1zqUVUh|ryP MlW4NlQhcA>? M1LndGROW09? M3W2PGRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= NHzxO4czPTh|NESwNS=>
MCF7 M2XTcGZ2dmO2aX;uJGF{e2G7 NIrDZ4s2KM7:TR?= MmPRNlQhcA>? NUXhfGt7TE2VTx?= MkexTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> MmLMNlU5OzR2MEG=
MCF7 NHrIZotHfW6ldHnvckBCe3OjeR?= MXq1JO69VQ>? NV70[W96OjRiaB?= MlXsSG1UVw>? NUPHSWltUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzPyCNaYCx M3XQ[lI2QDN2NECx
MDA-MB-231 NWXlSmFETnWwY4Tpc44hSXO|YYm= NX32NnZiPSEQvF2= MnXiNlQhcA>? NHPzWFhFVVOR NUPnWYNJTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzFxQ1TDNi=> MXiyOVg{PDRyMR?=
MDA-MB-231 NWqwOmxQTnWwY4Tpc44hSXO|YYm= MVWxJO69VQ>? M4HKV|I1KGh? MlrISG1UVw>? NGfCUW1KdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? MmHqNlU5OzR2MEG=
MDA-MB-231 MXXGeY5kfGmxbjDBd5NigQ>? M1XqcFUh|ryP NI\NU|AzPCCq NFfs[pBFVVOR NEjBb45F\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx MnXaNlU5OzR2MEG=
MDA-MB-231 MkTNSpVv[3Srb36gRZN{[Xl? MWC1JO69VQ>? MUmyOEBp MWnEUXNQ NV;MdWNmUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? MlLlNlU5OzR2MEG=
MDA-MB-231 NX\HO49UTnWwY4Tpc44hSXO|YYm= Ml[1OUDPxE1? M4jIOlI1KGh? MXLEUXNQ Mki4TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz NGP2OFkzPTh|NESwNS=>
MDA-MB-231 MX3GeY5kfGmxbjDBd5NigQ>? M2\xW|Uh|ryP NF;kdlUzPCCq NUHvR|ZOTE2VTx?= NY\lPWU2UW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJA2Ow>? Mn3mNlU5OzR2MEG=
MCF7 MnnxRZBweHSxc3nzJGF{e2G7 MYi1JO69VQ>? NYrjbXE1OjRiaB?= M4HJVWROW09? MXTJcoR2[2W|IHHwc5B1d3SrYzDk[YF1cA>? NIfCVnozPTh|NESwNS=>
MDA-MB-231 Mk\TRZBweHSxc3nzJGF{e2G7 MlvGOUDPxE1? MlnuNlQhcA>? NGSxR3pFVVOR NFj6[GZKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= MXKyOVg{PDRyMR?=
MCF7 NVW3UpZUTnWwY4Tpc44hSXO|YYm= MoD6NUDPxE1? M1zHXlczKGh? NXH1TXNwTE2VTx?= M13OW2lv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= M1TP[lI2QDN2NECx
MDA-MB-231 MV\GeY5kfGmxbjDBd5NigQ>? Mn[yNUDPxE1? MVi3NkBp MlrpSG1UVw>? Mo\wTY5lfWOnczDheZRweGijZ3njJIRm[XSq NGK4PG8zPTh|NESwNS=>
U-2 OS M2\hemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XoOVUxKM7:TR?= NUnjdldoOjRiaB?= NH\VeYFFVVOR MX3JR|UxRTF4Lk[g{txO Mo\2NlU4QTJ6MUG=
MG-63 MkmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:2TVUxKM7:TR?= MUOyOEBp M1yx[mROW09? NU\1[GdqUUN3ME25MlUh|ryP NHS1OHMzPTd7MkixNS=>
U-2 OS MWDBdI9xfG:|aYOgRZN{[Xl? MoPzOUDPxE1? NFXnNYMzPCCq MULEUXNQ MX7JcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo M3:yNlI2Pzl{OEGx
MG-63 M2q4cmFxd3C2b4Ppd{BCe3OjeR?= M3f5T|Uh|ryP NIriepczPCCq M1rlSWROW09? M3rEPGlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> MYKyOVc6OjhzMR?=
U-2 OS Mn\HSpVv[3Srb36gRZN{[Xl? NWfCflJZPSEQvF2= MVSyOEBp M{jmdWROW09? NW\LV4FtWHKxbX;0[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq NVfVXpJ[OjV5OUK4NVE>
MG-63 MX;GeY5kfGmxbjDBd5NigQ>? MX61JO69VQ>? NIq2e5QzPCCq NWPZSGxxTE2VTx?= NIfCS4hRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? NV[5O3ZLOjV5OUK4NVE>
PANC-1 MoTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWCzW2tvPTBizszN M4jETFI1KGh? MWfEUXNQ Ml70TWM2OD15LkGg{txO MlW4NlU3OzJ{MkW=
BxPC-3 NGrv[GVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjWTppOPTBizszN NUjQcHgzOjRiaB?= NX;FOWZ1TE2VTx?= MWLJR|UxRTZwODFOwG0> NFrNT40zPTZ|MkKyOS=>
PANC-1 NF:xPIdHfW6ldHnvckBCe3OjeR?= M{fjeVUh|ryP NHTy[nYzPCCq NYnzXoJWTE2VTx?= NGXZU3ZKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? MXuyOVY{OjJ{NR?=
BxPC-3 Ml\NSpVv[3Srb36gRZN{[Xl? MVm1JO69VQ>? M3PQ[FI1KGh? NInMfpVFVVOR NGTKR|RKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NUTSd2hiOjV4M{KyNlU>
PANC-1 NYToSmJtTnWwY4Tpc44hSXO|YYm= MlTOOUDPxE1? Mke5NlQhcA>? NFnnNmZFVVOR NYXsd3o1UW6mdXPld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? MYmyOVY{OjJ{NR?=
BxPC-3 MVnGeY5kfGmxbjDBd5NigQ>? MXe1JO69VQ>? NXPOfVFxOjRiaB?= MXXEUXNQ NYjnXmJIUW6mdXPld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? Mn7ENlU3OzJ{MkW=
SKOV3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjuVm4yODBizszN MkDuNlQhcA>? M33F[mROW09? M3Lje2lEPTB;MkCuOFgh|ryP MUSyOVYzPDd3MB?=
OVCAR4 NXH3OpR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDHVJcyODBizszN M1q4V|I1KGh? NWTHRok4TE2VTx?= M3vzcGlEPTB;MkKuNVMh|ryP MX2yOVYzPDd3MB?=
SKOV3 NFq0SItHfW6ldHnvckBCe3OjeR?= M1XrNVUh|ryP MWG3NkBp M4H1TWROW09? Mn;yTY5lfWOnczDHNk9OKGG{cnXzeC=> NYjDO3dyOjV4MkS3OVA>
OVCAR4 M{Sxc2Z2dmO2aX;uJGF{e2G7 MnO2OUDPxE1? MYW3NkBp Mm\ZSG1UVw>? M1fNbGlv\HWlZYOgS|IwVSCjcoLld5Q> MoHaNlU3OjR5NUC=
SKOV3 M4LFb2Fxd3C2b4Ppd{BCe3OjeR?= M2\QdVUh|ryP Ml7VNlQhcA>? MlLXSG1UVw>? NGHzXHhKdmS3Y3XzJIFxd3C2b4Ppdy=> MX:yOVYzPDd3MB?=
OVCAR4 Mn;yRZBweHSxc3nzJGF{e2G7 NGO5TVY2KM7:TR?= MoSwNlQhcA>? MU\EUXNQ M{ToRWlv\HWlZYOgZZBweHSxc3nz M320UFI2PjJ2N{Ww
AGS M3qxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPncoh{OjVizszN NFLOPVYzPCCq MU\EUXNQ M2[0dWlEPTB;MUmuNFkh|ryP Mly2NlU3ODl7MkO=
NCI-N78 MlPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXBNlUh|ryP NYnQcJVwOjRiaB?= NWnsWWtqTE2VTx?= M3PNdmlEPTB;Mk[uN|Mh|ryP M3G2dFI2PjB7OUKz
AGS NEfle2RCeG:ydH;zbZMhSXO|YYm= MonTOUDPxE1? NHrUfIozPCCq MULEUXNQ MVvJcoR2[2W|IHHwc5B1d3Orcx?= NEP1ZoszPTZyOUmyNy=>
NCI-N78 NIfqRoNCeG:ydH;zbZMhSXO|YYm= NU[yXVUzPSEQvF2= NX;MUo1tOjRiaB?= MYHEUXNQ NHmwbHRKdmS3Y3XzJIFxd3C2b4Ppdy=> MYWyOVYxQTl{Mx?=
AGS NUS1ZXJ6TnWwY4Tpc44hSXO|YYm= NEnxfJg2KM7:TR?= NI\leIozPCCq NWf2UYhCTE2VTx?= MVvJcoR2[2W|IITo[UBifXSxcHjh[5k> NIrFXHkzPTZyOUmyNy=>
NCI-N78 NH7ydZZHfW6ldHnvckBCe3OjeR?= MnjZOUDPxE1? M1jqRlI1KGh? NWnHepR{TE2VTx?= M4P4fGlv\HWlZYOgeIhmKGG3dH;wbIFogQ>? MV:yOVYxQTl{Mx?=
HSC-3 NVvyfXNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXexJO69VQ>? M2nZOVQ5KGh? NEXRPJdKSzVyPUCuOVQh|ryP M1u5[lI2OzZ4MUSz
GB30 MljYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1q2cFEh|ryP MWG3JIQ> NYD3PGhiTE2VTx?= MXzJR|UxRTBwMEGxJO69VQ>? MVGyOVExPjR{OB?=
GB9 NWPxcJduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS2NUDPxE1? MYS3JIQ> M{Lmb2ROW09? MkD4TWM2OD1yLkCyOEDPxE1? M3rEXFI2OTB4NEK4
GB169 NUjtNVE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWeybVA3OSEQvF2= NE\2[YE4KGR? MV3EUXNQ MorHTWM2OD1yLkCzNkDPxE1? M2XH[VI2OTB4NEK4
T24 MmnPSpVv[3Srb36gRZN{[Xl? MnXyNUDPxE1? NXf5eIRQPDhiaB?= MnviSG1UVw>? Ml3jTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MknENlM1ODN4M{O=
RT4 MV7GeY5kfGmxbjDBd5NigQ>? M2Pr[FEh|ryP NVi3[|hSPDhiaB?= NH\DVmZFVVOR NF;aZ4tKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NFjBRowzOzRyM{[zNy=>
UM-UC-3 NHrSUohHfW6ldHnvckBCe3OjeR?= M2XiOFEh|ryP Mk\vOFghcA>? MVnEUXNQ NIXqbW9KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NV3scHFDOjN2MEO2N|M>
T24 NGi1U3ZCeG:ydH;zbZMhSXO|YYm= Ml3QN{4yPiEQvF2= MmXmPVYhcA>? M2n0RWROW09? NEfMS25KSzVyPUCuNFMxPiEQvF2= NI[2[ZgzOzRyM{[zNy=>
RT4 MXjBdI9xfG:|aYOgRZN{[Xl? NVTXU3JzOy5zNjFOwG0> NWjqRWlxQTZiaB?= NXnBTXM1TE2VTx?= M{LWXWlEPTB;MD6xNVk5KM7:TR?= M{nIUFI{PDB|NkOz
UM-UC-3 NYfGPYg{SXCxcITvd4l{KEG|c3H5 M1nxb|MvOTZizszN NGHWbY06PiCq MkPWSG1UVw>? NXfOOG5YUUN3ME2wMlA1PDlizszN MlHaNlM1ODN4M{O=
OVCAR-5 NVLwO|B4TnWwY4Tpc44hSXO|YYm= MkjuOVAhdk1? NWL4bIVDUW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NH\RPIczOzN|NEOyOy=>
SKOV3ip2 NXr6OHFxTnWwY4Tpc44hSXO|YYm= MWm1NEBvVQ>? MWPJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NWO4SGZXOjN|M{SzNlc>
S462 M{TQSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j3eVExOCEQvF2= MUC3NkBp NFTIVWhFVVOR NEfzfHFCfHSnboXheIV{KGOnbHyg[5Jwf3Sq NWjVUoJtOjN|MkixNVQ>
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CCRF-CEM NWXuSJZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{WwXVExKM7:TR?= NUCzOZRJQTZiaB?= NVTaTpl7UUN3ME2wMlA6PCEQvF2= M{C3bVIxOTB6M{O4
Kasumi-1 NUTuUYtXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjMfYR5OTBizszN NFHPUYQ6PiCq M1HvSWlEPTB;MD6xNFMh|ryP NYXtdYxXOjBzMEizN|g>
Karpas-299 M2X3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PrR|ExKM7:TR?= MlzwPVYhcA>? M1HCPWlEPTB;MD6wN|gh|ryP NE[xOnAzODFyOEOzPC=>
Ramos-RA1 NXrlRZNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TvNlExKM7:TR?= NFnFW4U6PiCq M2H0ZmlEPTB;MD6xNlch|ryP NVzxcZZXOjBzMEizN|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 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-

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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