Alisertib (MLN8237) 化学構造
分子量: 518.92

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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 NF\JTVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGwMlUh|ryP NHTjfFY4OiCq Mm\TSG1UVw>? NHXGUWpKSzVyPUCuNFQh|ryP NIS3N4gzPjF|Nk[4OC=>
LS174T NXKwRoJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUWwVW0yOC53IN88US=> M1\tT|czKGh? M2PQTmROW09? MmLWTWM2OD1yLkC1JO69VQ>? Ml3MNlYyOzZ4OES=
T84 MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[wMlUh|ryP NHrEU2U4OiCq MlXoSG1UVw>? NEXqeWhKSzVyPUCuNFkh|ryP MYCyOlE{PjZ6NB?=
LS180 NHfTd2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XlelAvPSEQvF2= NYPGepZ6PzJiaB?= MoHhSG1UVw>? NFjMd5dKSzVyPUGg{txO MXOyOlE{PjZ6NB?=
SW948 M2WzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDxUZI3OC53IN88US=> MVq3NkBp M2TXUmROW09? MnnNTWM2OD1zIN88US=> NH\ycGQzPjF|Nk[4OC=>
HCT15 NIPxd4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvVb4QxNjVizszN MUG3NkBp MoiySG1UVw>? NY\2[IxGUUN3MEywMlQh|ryP NWLCfohOOjZzM{[2PFQ>
DLD-1 MnjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTWNE42KM7:TR?= M3\3[VczKGh? Mn3SSG1UVw>? M2juRWlEPTB:MD64JO69VQ>? Mn:1NlYyOzZ4OES=
MIP-101 NWSweoVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKwMlUh|ryP NV:z[5ljPzJiaB?= MV3EUXNQ NF3ORllKSzVyPUGg{txO NFTRXmEzPjF|Nk[4OC=>
SNU1544 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPjTXYxNjVizszN NHX6SWQ4OiCq MoO1SG1UVw>? NWCxXJdGUUN3ME2xJO69VQ>? MV:yOlE{PjZ6NB?=
OCI-Ly10 NFPrNpBEgXSxdH;4bYMhSXO|YYm= MnzCO|IhcA>? M4S1Z2ROW09? MlXwTWM2OD1yLkC1PEDPxE1? M4Hud|I2QDd6M{Ox
SU-DHL2 MVnDfZRwfG:6aXOgRZN{[Xl? NVPMdZk3PzJiaB?= NX7tc2tiTE2VTx?= NU[4clN6UUN3ME2wMlAyKM7:TR?= NInOeZIzPTh5OEOzNS=>
OCI-LY7 NGTZfYJEgXSxdH;4bYMhSXO|YYm= Mn;GO|IhcA>? MnPUSG1UVw>? MXrJR|UxRTBwMEixJO69VQ>? MoLFNlU5Pzh|M{G=
SU-DHL6 M2r1Z2N6fG:2b4jpZ{BCe3OjeR?= NFX0cIk4OiCq NUjtOJk4TE2VTx?= M1T5OmlEPTB;MD60PFIh|ryP M4XhTlI2QDd6M{Ox
Jeko-1 MYTDfZRwfG:6aXOgRZN{[Xl? MVK3NkBp M2Pae2ROW09? NVfo[241UUN3ME2wMlAzQSEQvF2= M4HqNVI2QDd6M{Ox
JVM-2 M1H1bGN6fG:2b4jpZ{BCe3OjeR?= NV7YUnBvPzJiaB?= NIq4OZVFVVOR MXjJR|UxRTBwMEGg{txO MXuyOVg4QDN|MR?=
Rec-1 MlOxR5l1d3SxeHnjJGF{e2G7 NFvGO|A4OiCq NUXZRXhtTE2VTx?= NGHvSWVKSzVyPUCuNFg4KM7:TR?= M{\s[FI2QDd6M{Ox
Z-138 NVTZd5A1S3m2b4TvfIlkKEG|c3H5 NU\YNZNbPzJiaB?= MXrEUXNQ MYDJR|UxRTBwMEGzJO69VQ>? NX3nPWxFOjV6N{izN|E>
H9 Mmm0R5l1d3SxeHnjJGF{e2G7 MlW4O|IhcA>? NIDq[IFFVVOR NV7HVmxHUUN3ME2wMlYh|ryP Ml7ENlU5Pzh|M{G=
HH NYPPO|dzS3m2b4TvfIlkKEG|c3H5 M{PlOFczKGh? MljoSG1UVw>? NHfJXlVKSzVyPUCuO{DPxE1? M4LuVFI2QDd6M{Ox
DND41 NW\QOlI{S3m2b4TvfIlkKEG|c3H5 M2TzNlczKGh? MlnESG1UVw>? M3ToZmlEPTB;MD6xJO69VQ>? NFzrbW8zPTh5OEOzNS=>
CCL119 MYDDfZRwfG:6aXOgRZN{[Xl? MmWxO|IhcA>? MkjVSG1UVw>? Mk\3TWM2OD1yLkC2NkDPxE1? NV;xeJBpOjV6N{izN|E>
J.Cam 1.6 MkjoR5l1d3SxeHnjJGF{e2G7 NITrSHE4OiCq M2\sSGROW09? NF3Eb5VKSzVyPUCuNVA2KM7:TR?= MXeyOVg4QDN|MR?=
Sup-T1 NWTidVFNS3m2b4TvfIlkKEG|c3H5 M3zMXFczKGh? M3ThemROW09? MkW4TWM2OD1{LkG0NkDPxE1? M1;vb|I2QDd6M{Ox
Tib 152 NGfLWplEgXSxdH;4bYMhSXO|YYm= MVO3NkBp NFXIVZBFVVOR MV;JR|UxRTBwODFOwG0> MmT1NlU5Pzh|M{G=
MCF7 M1\zOWZ2dmO2aX;uJGF{e2G7 MXO1JO69VQ>? NFjpNIczPCCq NUfPVYs1TE2VTx?= M1HYO2lv\HWlZYOgS|IwVSCjcoLld5Q> MYSyOVg{PDRyMR?=
MDA-MB-231 M{C5XGZ2dmO2aX;uJGF{e2G7 MoDiOUDPxE1? MoTDNlQhcA>? M{POcWROW09? MULJcoR2[2W|IFezM20h[XK{ZYP0 MoLyNlU5OzR2MEG=
MCF7 MWHGeY5kfGmxbjDBd5NigQ>? MVi1JO69VQ>? M3nCd|I1KGh? NFzNPHJFVVOR MXrE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ NUDGTW9zOjV6M{S0NFE>
MCF7 NWDmXmF{TnWwY4Tpc44hSXO|YYm= Ml7FOUDPxE1? MV:yOEBp MUDEUXNQ NWXodGVOTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? NETPSGczPTh|NESwNS=>
MCF7 M37PO2Z2dmO2aX;uJGF{e2G7 M2DBN|Uh|ryP MXWyOEBp MmnCSG1UVw>? NXznOlZQTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> Mnj1NlU5OzR2MEG=
MCF7 MUfGeY5kfGmxbjDBd5NigQ>? NEDqT3E2KM7:TR?= M1f1fFI1KGh? M13MS2ROW09? MWXJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> NIH1PI8zPTh|NESwNS=>
MCF7 NXfiWVhCTnWwY4Tpc44hSXO|YYm= MmewOUDPxE1? NUHTeWNWOjRiaB?= NIDBPZhFVVOR NILWZ3dKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= M2XQZlI2QDN2NECx
MDA-MB-231 MXnGeY5kfGmxbjDBd5NigQ>? NUexVItmPSEQvF2= NETQXXAzPCCq MnS4SG1UVw>? MXfE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ M{LBUFI2QDN2NECx
MDA-MB-231 MU\GeY5kfGmxbjDBd5NigQ>? MXexJO69VQ>? M37rRVI1KGh? NYfJ[4ZHTE2VTx?= NWTxd|lrUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? NYi4TJc3OjV6M{S0NFE>
MDA-MB-231 NEXhdHNHfW6ldHnvckBCe3OjeR?= NFKyVIg2KM7:TR?= MnvzNlQhcA>? M33COWROW09? MYDE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz MnnrNlU5OzR2MEG=
MDA-MB-231 NV63WHFLTnWwY4Tpc44hSXO|YYm= NHX3fWo2KM7:TR?= NHziZo0zPCCq NHHnT2VFVVOR M3XMUWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlEhX2GoMT;DbZAy NXLKeFZDOjV6M{S0NFE>
MDA-MB-231 M2DET2Z2dmO2aX;uJGF{e2G7 MWC1JO69VQ>? NVfNTZprOjRiaB?= MXfEUXNQ MnnCTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz NXjQV2RjOjV6M{S0NFE>
MDA-MB-231 NXzyUFVwTnWwY4Tpc44hSXO|YYm= M3q4PVUh|ryP NHSzdnEzPCCq NIG4U4FFVVOR M{TYOWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwOVM> M17IRVI2QDN2NECx
MCF7 MUDBdI9xfG:|aYOgRZN{[Xl? MmT0OUDPxE1? MUGyOEBp MV7EUXNQ M2PHcmlv\HWlZYOgZZBweHSxdHnjJIRm[XSq NWnxRWFJOjV6M{S0NFE>
MDA-MB-231 MVvBdI9xfG:|aYOgRZN{[Xl? MUW1JO69VQ>? NUnMOIZyOjRiaB?= MVjEUXNQ M2nx[2lv\HWlZYOgZZBweHSxdHnjJIRm[XSq NY\vTGtwOjV6M{S0NFE>
MCF7 NYjWcG9wTnWwY4Tpc44hSXO|YYm= NGe5e44yKM7:TR?= MY[3NkBp NIXpOGdFVVOR MV\JcoR2[2W|IHH1eI9xcGGpaXOg[IVifGh? M1rBV|I2QDN2NECx
MDA-MB-231 NHPxfWdHfW6ldHnvckBCe3OjeR?= MVixJO69VQ>? MUi3NkBp Mki4SG1UVw>? M{DXcGlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= MmX3NlU5OzR2MEG=
U-2 OS NVL0RpFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\QPWY2OCEQvF2= NYrSfWhvOjRiaB?= NWrYPXdpTE2VTx?= NIrj[JBKSzVyPUG2MlYh|ryP M3;vVFI2Pzl{OEGx
MG-63 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TISFUxKM7:TR?= MYGyOEBp M1r1V2ROW09? NX7RdmZwUUN3ME25MlUh|ryP MVWyOVc6OjhzMR?=
U-2 OS M2jzdGFxd3C2b4Ppd{BCe3OjeR?= NILDPJE2KM7:TR?= M3i1dVI1KGh? MmDVSG1UVw>? M2HSRmlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> MWSyOVc6OjhzMR?=
MG-63 NIDmPWRCeG:ydH;zbZMhSXO|YYm= NUnEfWcyPSEQvF2= Mn3ENlQhcA>? NXHuN5U4TE2VTx?= MYPJcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo MlvDNlU4QTJ6MUG=
U-2 OS MmmzSpVv[3Srb36gRZN{[Xl? NXzQOGU2PSEQvF2= NIHNSowzPCCq NVnP[ZZrTE2VTx?= NHnHS2lRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? MmOwNlU4QTJ6MUG=
MG-63 MmO1SpVv[3Srb36gRZN{[Xl? NF72cm82KM7:TR?= M4nBdlI1KGh? NH\SdFhFVVOR MnLGVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp M1\pcFI2Pzl{OEGx
PANC-1 M3TT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33FdFUxKM7:TR?= MXmyOEBp NUn2ZVhRTE2VTx?= Mk\6TWM2OD15LkGg{txO NWXtUo9LOjV4M{KyNlU>
BxPC-3 M1PMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUG1NEDPxE1? NYfMPG43OjRiaB?= NHPSNIlFVVOR MoD4TWM2OD14Lkig{txO Mo[yNlU3OzJ{MkW=
PANC-1 Mme2SpVv[3Srb36gRZN{[Xl? MW[1JO69VQ>? MnvtNlQhcA>? NVPoO|Z5TE2VTx?= NVS1[lk6UW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBqdiCJMj;NJJBp[XOn NWSxPGtKOjV4M{KyNlU>
BxPC-3 MXrGeY5kfGmxbjDBd5NigQ>? NHL1OWE2KM7:TR?= MUSyOEBp NGPLTotFVVOR M{\v[Glv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hTzJxTTDwbIF{\Q>? M{PVUFI2PjN{MkK1
PANC-1 MmHuSpVv[3Srb36gRZN{[Xl? M3:zclUh|ryP MXeyOEBp MnfSSG1UVw>? MoHoTY5lfWOnczDheZRweGijZ3njJINmdGxiZHXheIg> MXmyOVY{OjJ{NR?=
BxPC-3 MXXGeY5kfGmxbjDBd5NigQ>? M1\3R|Uh|ryP MkLRNlQhcA>? MmraSG1UVw>? NGLCZ5VKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? MX[yOVY{OjJ{NR?=
SKOV3 NGi2bpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDOSYwyODBizszN MnnuNlQhcA>? NIW3b3RFVVOR NWizWVFyUUN3ME2yNE41QCEQvF2= M2f3SVI2PjJ2N{Ww
OVCAR4 Ml7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTpcJUyODBizszN M2nzb|I1KGh? NVXzfHhRTE2VTx?= M2\IOWlEPTB;MkKuNVMh|ryP NHf1c3QzPTZ{NEe1NC=>
SKOV3 NXrCc3dvTnWwY4Tpc44hSXO|YYm= M2\qelUh|ryP MmjKO|IhcA>? NV30[Y1jTE2VTx?= MnTrTY5lfWOnczDHNk9OKGG{cnXzeC=> M{XNcFI2PjJ2N{Ww
OVCAR4 MX\GeY5kfGmxbjDBd5NigQ>? NXm0R5A{PSEQvF2= NITFVHE4OiCq M1iyemROW09? NFzQSIZKdmS3Y3XzJGczN01iYYLy[ZN1 Ml\JNlU3OjR5NUC=
SKOV3 M4XWbWFxd3C2b4Ppd{BCe3OjeR?= NYXHNXl4PSEQvF2= NWHDS5loOjRiaB?= M3WxUWROW09? M3LpUmlv\HWlZYOgZZBweHSxc3nz NWDhV25WOjV4MkS3OVA>
OVCAR4 MYjBdI9xfG:|aYOgRZN{[Xl? MXq1JO69VQ>? NYP3PFNJOjRiaB?= M1LqRWROW09? NInKT5lKdmS3Y3XzJIFxd3C2b4Ppdy=> NYrkVoY5OjV4MkS3OVA>
AGS NYT3eYZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfYcWszPSEQvF2= M{nsXlI1KGh? NX7GVoNKTE2VTx?= M4HWUWlEPTB;MUmuNFkh|ryP MUKyOVYxQTl{Mx?=
NCI-N78 M3fxO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnPNlUh|ryP M2DTclI1KGh? NEf6c2lFVVOR Mo\wTWM2OD1{Nj6zN{DPxE1? NWDVSldnOjV4MEm5NlM>
AGS MkTDRZBweHSxc3nzJGF{e2G7 MknzOUDPxE1? MV:yOEBp MmXWSG1UVw>? M33OWWlv\HWlZYOgZZBweHSxc3nz NVW1OYxxOjV4MEm5NlM>
NCI-N78 MknnRZBweHSxc3nzJGF{e2G7 M{HzNVUh|ryP MnHrNlQhcA>? NV\EVFNpTE2VTx?= NEfIZ5hKdmS3Y3XzJIFxd3C2b4Ppdy=> NYHyUpZGOjV4MEm5NlM>
AGS M3LicGZ2dmO2aX;uJGF{e2G7 MUm1JO69VQ>? NHHubmczPCCq M13ZOWROW09? MnrDTY5lfWOnczD0bIUh[XW2b4DoZYd6 M12xZlI2PjB7OUKz
NCI-N78 NUXGSGM4TnWwY4Tpc44hSXO|YYm= M3\GTVUh|ryP Mki5NlQhcA>? M33KSWROW09? NYHJXZBlUW6mdXPld{B1cGViYYX0c5Bp[We7 MXWyOVYxQTl{Mx?=
HSC-3 NU\PdZdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLyNlMyKM7:TR?= Mn;JOFghcA>? MX7JR|UxRTBwNUSg{txO MVeyOVM3PjF2Mx?=
GB30 NGLqb2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\yNUDPxE1? NGrzVFQ4KGR? MXLEUXNQ M3v3ZWlEPTB;MD6wNVEh|ryP NXTweWdsOjVzME[0Nlg>
GB9 NXzEVJdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy5dmEyKM7:TR?= MlXoO{Bl NVexWY1UTE2VTx?= NX:ydIViUUN3ME2wMlAzPCEQvF2= M{nUT|I2OTB4NEK4
GB169 MlPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXsNUDPxE1? NET4Vo44KGR? NELzXFhFVVOR MX;JR|UxRTBwMEOyJO69VQ>? NHnDPWszPTFyNkSyPC=>
T24 M2XvcGZ2dmO2aX;uJGF{e2G7 MmHtNUDPxE1? NIP5cYw1QCCq NVPQfo1oTE2VTx?= MXXJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NUXoWXVGOjN2MEO2N|M>
RT4 M{fkWmZ2dmO2aX;uJGF{e2G7 MV2xJO69VQ>? MV[0PEBp M4\ROWROW09? NWfUXmZ1UW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NFr5blEzOzRyM{[zNy=>
UM-UC-3 M3fjZWZ2dmO2aX;uJGF{e2G7 NGrSOXcyKM7:TR?= MWW0PEBp M1PTeWROW09? MXnJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NVvqeJdYOjN2MEO2N|M>
T24 M2Pk[WFxd3C2b4Ppd{BCe3OjeR?= NFjxZog{NjF4IN88US=> NEPpVHg6PiCq MV;EUXNQ NHi5cZRKSzVyPUCuNFMxPiEQvF2= MUSyN|QxOzZ|Mx?=
RT4 NIH4S|RCeG:ydH;zbZMhSXO|YYm= M3rNXlMvOTZizszN MXm5OkBp M{XMfGROW09? MVLJR|UxRTBwMUG5PEDPxE1? Ml3ENlM1ODN4M{O=
UM-UC-3 MXHBdI9xfG:|aYOgRZN{[Xl? M4LUPVMvOTZizszN NEf2PZc6PiCq MYTEUXNQ M4\0[mlEPTB;MD6wOFQ6KM7:TR?= MmrLNlM1ODN4M{O=
OVCAR-5 M1KweWZ2dmO2aX;uJGF{e2G7 Mnm1OVAhdk1? NVnkTpNJUW6qaXLpeJMh[2WubDDtbYdz[XSrb36= MWCyN|M{PDN{Nx?=
SKOV3ip2 Mn;OSpVv[3Srb36gRZN{[Xl? MmDlOVAhdk1? MXXJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? MoK1NlM{OzR|Mke=
S462 M3jKXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnWyNVAxKM7:TR?= M3TwcFczKGh? Ml;BSG1UVw>? MnG5RZR1\W63YYTld{Bk\WyuIHfyc5d1cA>? M1f2OlI{OzJ6MUG0
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CCRF-CEM NWfH[2RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;2PVZ1OTBizszN NH7QXpY6PiCq MkLSTWM2OD1yLkC5OEDPxE1? MkLxNlAyODh|M{i=
Kasumi-1 NFqzUohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PWN|ExKM7:TR?= MXi5OkBp MlvMTWM2OD1yLkGwN{DPxE1? NG\KVIQzODFyOEOzPC=>
Karpas-299 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTYNVAh|ryP NXjCU3NPQTZiaB?= MYnJR|UxRTBwMEO4JO69VQ>? M3LqdFIxOTB6M{O4
Ramos-RA1 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rzZlExKM7:TR?= Mmf6PVYhcA>? MX\JR|UxRTBwMUK3JO69VQ>? NXHiWmxnOjBzMEizN|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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