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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電話番号: + 81 3-5632-9610mail@cosmobio.co.jp

Alisertib (MLN8237) 化学構造
分子量: 518.92

高品質保証

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カスタマーフィードバック(10)

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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 M1fwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\KeFA3OC53IN88US=> M3zjbFczKGh? NXXn[XVxTE2VTx?= NHTiUmZKSzVyPUCuNFQh|ryP MV:yOlE{PjZ6NB?=
LS174T NF7DXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOwMlUh|ryP MkHUO|IhcA>? NEn4XYVFVVOR MnjOTWM2OD1yLkC1JO69VQ>? MmPTNlYyOzZ4OES=
T84 NXnK[nFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXwepVpOC53IN88US=> NUjFSJNRPzJiaB?= MYPEUXNQ Mk\GTWM2OD1yLkC5JO69VQ>? MYSyOlE{PjZ6NB?=
LS180 NUXWV3gzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnBTmlCOC53IN88US=> MUe3NkBp NV22W3ZuTE2VTx?= M2n4OWlEPTB;MTFOwG0> MWqyOlE{PjZ6NB?=
SW948 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILBU3QxNjVizszN NYXpNIwzPzJiaB?= NF7BVpRFVVOR MY\JR|UxRTFizszN NXm4UGdYOjZzM{[2PFQ>
HCT15 NFfneWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\JOZcxNjVizszN M372NVczKGh? NVLtdnBETE2VTx?= M{Lp[mlEPTB:MD60JO69VQ>? MWGyOlE{PjZ6NB?=
DLD-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDVXoQxNjVizszN NWn1e5YxPzJiaB?= Mm\mSG1UVw>? MW\JR|UxRDBwODFOwG0> Mn;MNlYyOzZ4OES=
MIP-101 MmTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHGNE42KM7:TR?= NG\mfIE4OiCq MXnEUXNQ MU\JR|UxRTFizszN NXrXcFR2OjZzM{[2PFQ>
SNU1544 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jNfVAvPSEQvF2= NELVbFI4OiCq M3rlOWROW09? NHPyXVNKSzVyPUGg{txO MWSyOlE{PjZ6NB?=
OCI-Ly10 M2jLPGN6fG:2b4jpZ{BCe3OjeR?= Mke0O|IhcA>? Mle0SG1UVw>? M3LSVGlEPTB;MD6wOVgh|ryP NXvaPW0zOjV6N{izN|E>
SU-DHL2 NY\wZW5TS3m2b4TvfIlkKEG|c3H5 NGXhSpo4OiCq NWTFVpZuTE2VTx?= M{ixTWlEPTB;MD6wNUDPxE1? M4C2fFI2QDd6M{Ox
OCI-LY7 NHzt[I9EgXSxdH;4bYMhSXO|YYm= NYTKUmRyPzJiaB?= MmTpSG1UVw>? M1PqZ2lEPTB;MD6wPFEh|ryP Mle2NlU5Pzh|M{G=
SU-DHL6 M{[5dmN6fG:2b4jpZ{BCe3OjeR?= MUW3NkBp MVXEUXNQ NIX2SW9KSzVyPUCuOFgzKM7:TR?= MVOyOVg4QDN|MR?=
Jeko-1 Moj1R5l1d3SxeHnjJGF{e2G7 M4HlPFczKGh? NUPPXnBzTE2VTx?= NYKz[WRjUUN3ME2wMlAzQSEQvF2= MlP1NlU5Pzh|M{G=
JVM-2 NXryeW1oS3m2b4TvfIlkKEG|c3H5 M2LkU|czKGh? NFXYWXFFVVOR NGH3R3RKSzVyPUCuNFEh|ryP MYmyOVg4QDN|MR?=
Rec-1 M{O2ZmN6fG:2b4jpZ{BCe3OjeR?= MX[3NkBp M3vCSmROW09? NF6xVGlKSzVyPUCuNFg4KM7:TR?= M4HKSlI2QDd6M{Ox
Z-138 NEDITllEgXSxdH;4bYMhSXO|YYm= MV:3NkBp MUXEUXNQ MmfDTWM2OD1yLkCxN{DPxE1? MnrHNlU5Pzh|M{G=
H9 MXPDfZRwfG:6aXOgRZN{[Xl? MXq3NkBp M33FWWROW09? M{nrbmlEPTB;MD62JO69VQ>? NWXJPFVUOjV6N{izN|E>
HH NV;0PYlPS3m2b4TvfIlkKEG|c3H5 MX:3NkBp MWjEUXNQ M3Hs[mlEPTB;MD63JO69VQ>? MnvvNlU5Pzh|M{G=
DND41 NVHBNVF3S3m2b4TvfIlkKEG|c3H5 MmrpO|IhcA>? NHfOSmZFVVOR MV3JR|UxRTBwMTFOwG0> MYKyOVg4QDN|MR?=
CCL119 NUPTUXhlS3m2b4TvfIlkKEG|c3H5 MXS3NkBp Mly2SG1UVw>? NWD6b3RNUUN3ME2wMlA3OiEQvF2= MVmyOVg4QDN|MR?=
J.Cam 1.6 NFrPfHZEgXSxdH;4bYMhSXO|YYm= MmD0O|IhcA>? M1K5[WROW09? M1zaZmlEPTB;MD6xNFUh|ryP NHPReGEzPTh5OEOzNS=>
Sup-T1 MkDIR5l1d3SxeHnjJGF{e2G7 NF\sNXQ4OiCq Ml7GSG1UVw>? MYrJR|UxRTJwMUSyJO69VQ>? Mly5NlU5Pzh|M{G=
Tib 152 MlG3R5l1d3SxeHnjJGF{e2G7 NVWyc3hRPzJiaB?= Mln1SG1UVw>? NYK0bZFtUUN3ME2wMlgh|ryP M{DJO|I2QDd6M{Ox
MCF7 MYHGeY5kfGmxbjDBd5NigQ>? NYDKPWZ2PSEQvF2= NHKyc3gzPCCq NIjtVJpFVVOR MYrJcoR2[2W|IFeyM20h[XK{ZYP0 MV[yOVg{PDRyMR?=
MDA-MB-231 M{i0NmZ2dmO2aX;uJGF{e2G7 MWm1JO69VQ>? MmjiNlQhcA>? NXWySpN2TE2VTx?= M4rrb2lv\HWlZYOgS|MwVSCjcoLld5Q> M4rmXFI2QDN2NECx
MCF7 NXHLU2hoTnWwY4Tpc44hSXO|YYm= M{HSdVUh|ryP M1yye|I1KGh? NFjvV|hFVVOR NXu3ZYFnTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzFxQ1TDNi=> Mn76NlU5OzR2MEG=
MCF7 M{\Lc2Z2dmO2aX;uJGF{e2G7 NEixdnI2KM7:TR?= NInRN44zPCCq NWrYVWxtTE2VTx?= NFTLflJF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NG\RcGUzPTh|NESwNS=>
MCF7 NUHJ[GJjTnWwY4Tpc44hSXO|YYm= NWK2XYFCPSEQvF2= MWOyOEBp NYPMWWZUTE2VTx?= M362T2Rm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= MX:yOVg{PDRyMR?=
MCF7 M2HmVGZ2dmO2aX;uJGF{e2G7 MlPqOUDPxE1? M3ftXFI1KGh? NELqdnRFVVOR NFjI[|NKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFIyKFejZkGvR4lxOQ>? M4rXXFI2QDN2NECx
MCF7 M2LrS2Z2dmO2aX;uJGF{e2G7 M1fIZ|Uh|ryP MUiyOEBp MoTGSG1UVw>? MofxTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz MYGyOVg{PDRyMR?=
MDA-MB-231 MUHGeY5kfGmxbjDBd5NigQ>? Mn\jOUDPxE1? M4\xVFI1KGh? MWjEUXNQ NGTMTWxF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy MmH0NlU5OzR2MEG=
MDA-MB-231 NXLwSIxSTnWwY4Tpc44hSXO|YYm= NWLiUHZZOSEQvF2= MoHNNlQhcA>? MknsSG1UVw>? NVHxc|JEUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? NEXzc5ozPTh|NESwNS=>
MDA-MB-231 NELOOFdHfW6ldHnvckBCe3OjeR?= NHTzOIg2KM7:TR?= MVyyOEBp NHHYWmRFVVOR M4PySmRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= MUmyOVg{PDRyMR?=
MDA-MB-231 M1jQW2Z2dmO2aX;uJGF{e2G7 MlvxOUDPxE1? M1zoOVI1KGh? MVrEUXNQ MX;JcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> NYDQdIxrOjV6M{S0NFE>
MDA-MB-231 NVLUcFRiTnWwY4Tpc44hSXO|YYm= MXe1JO69VQ>? M3nZV|I1KGh? NVjNVGtDTE2VTx?= NHzSNItKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= NH[5Z|QzPTh|NESwNS=>
MDA-MB-231 NX;re3BJTnWwY4Tpc44hSXO|YYm= NHfDOpo2KM7:TR?= M2\Id|I1KGh? NG\Md3pFVVOR M1zvdWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwOVM> NWX6c5c1OjV6M{S0NFE>
MCF7 MnnRRZBweHSxc3nzJGF{e2G7 NITKZ4k2KM7:TR?= M2HB[VI1KGh? NWTI[Gx6TE2VTx?= NIPWe2xKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= MYSyOVg{PDRyMR?=
MDA-MB-231 Mn76RZBweHSxc3nzJGF{e2G7 NU\5N5Z5PSEQvF2= NVm4eG05OjRiaB?= NX\KfGhLTE2VTx?= M1ywU2lv\HWlZYOgZZBweHSxdHnjJIRm[XSq MnrDNlU5OzR2MEG=
MCF7 MoLnSpVv[3Srb36gRZN{[Xl? NVv4TVhoOSEQvF2= MlvPO|IhcA>? MmqzSG1UVw>? MlHUTY5lfWOnczDheZRweGijZ3njJIRm[XSq M4PwSlI2QDN2NECx
MDA-MB-231 MVzGeY5kfGmxbjDBd5NigQ>? NFm0dYIyKM7:TR?= MW[3NkBp NHrN[YpFVVOR NEPMRopKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= M{m3fVI2QDN2NECx
U-2 OS NVjuPIlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXHOVAh|ryP MkTvNlQhcA>? M2LicmROW09? MkjtTWM2OD1zNj62JO69VQ>? M1f3U|I2Pzl{OEGx
MG-63 NYrEZmRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHJS5M3PTBizszN NVLQO4JsOjRiaB?= Mn;6SG1UVw>? Mn3kTWM2OD17LkWg{txO M2X4UFI2Pzl{OEGx
U-2 OS NF20SFVCeG:ydH;zbZMhSXO|YYm= MojSOUDPxE1? NH7OfJkzPCCq Ml72SG1UVw>? MU\JcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo NEOxcoEzPTd7MkixNS=>
MG-63 MXXBdI9xfG:|aYOgRZN{[Xl? NVrjNHpSPSEQvF2= NV\FTINqOjRiaB?= MVTEUXNQ NGrLbFVKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp NW\uWplzOjV5OUK4NVE>
U-2 OS NEXz[plHfW6ldHnvckBCe3OjeR?= MkT0OUDPxE1? NV;FNG1WOjRiaB?= NYn5[m81TE2VTx?= MkjyVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp NWqwSI9GOjV5OUK4NVE>
MG-63 MUDGeY5kfGmxbjDBd5NigQ>? MYW1JO69VQ>? NFO0ZngzPCCq MVrEUXNQ MVTQdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> MYiyOVc6OjhzMR?=
PANC-1 NYLVOJJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH2wToo2OCEQvF2= NWOwNZJXOjRiaB?= M2KzRWROW09? NUfyOGt1UUN3ME23MlEh|ryP NHjwTYkzPTZ|MkKyOS=>
BxPC-3 NXq5d4x4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHxOVAh|ryP M2D4NlI1KGh? Mm\qSG1UVw>? MWHJR|UxRTZwODFOwG0> NEjuS|kzPTZ|MkKyOS=>
PANC-1 NHHHZ2xHfW6ldHnvckBCe3OjeR?= NWjnVlJFPSEQvF2= MXiyOEBp NHS1R3BFVVOR MXzJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> MoDaNlU3OzJ{MkW=
BxPC-3 NYG4ZW1YTnWwY4Tpc44hSXO|YYm= MoHWOUDPxE1? NETsTHozPCCq NFjFcJlFVVOR MU\JcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> NFjqSo0zPTZ|MkKyOS=>
PANC-1 MknxSpVv[3Srb36gRZN{[Xl? NUH2Z5JpPSEQvF2= MVqyOEBp MWnEUXNQ MWHJcoR2[2W|IHH1eI9xcGGpaXOgZ4VtdCCmZXH0bC=> M3XHWFI2PjN{MkK1
BxPC-3 M{e2[GZ2dmO2aX;uJGF{e2G7 MmmzOUDPxE1? MXKyOEBp NUPI[|g4TE2VTx?= MUnJcoR2[2W|IHH1eI9xcGGpaXOgZ4VtdCCmZXH0bC=> Ml:zNlU3OzJ{MkW=
SKOV3 NV\TNHU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkS5NVAxKM7:TR?= MlmzNlQhcA>? M4L5S2ROW09? M4j4[WlEPTB;MkCuOFgh|ryP NGXwcpMzPTZ{NEe1NC=>
OVCAR4 M2O4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\XNVAxKM7:TR?= NX;STZZFOjRiaB?= MlnjSG1UVw>? NEfwW2FKSzVyPUKyMlE{KM7:TR?= MXGyOVYzPDd3MB?=
SKOV3 NFfHV2hHfW6ldHnvckBCe3OjeR?= NHTw[XI2KM7:TR?= NXLQUFBWPzJiaB?= NELOcnlFVVOR NXO4NVJsUW6mdXPld{BIOi:PIHHydoV{fA>? MmHqNlU3OjR5NUC=
OVCAR4 M1nD[mZ2dmO2aX;uJGF{e2G7 M3LJNlUh|ryP NHLzVI44OiCq MorHSG1UVw>? MUHJcoR2[2W|IFeyM20h[XK{ZYP0 MViyOVYzPDd3MB?=
SKOV3 MlfhRZBweHSxc3nzJGF{e2G7 MWm1JO69VQ>? MUOyOEBp MnnsSG1UVw>? MUfJcoR2[2W|IHHwc5B1d3Orcx?= M{j4WFI2PjJ2N{Ww
OVCAR4 M162d2Fxd3C2b4Ppd{BCe3OjeR?= MVi1JO69VQ>? NU\t[281OjRiaB?= NVizd49DTE2VTx?= MkPmTY5lfWOnczDhdI9xfG:|aYO= NHnBTWMzPTZ{NEe1NC=>
AGS MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojnNlUh|ryP MmXkNlQhcA>? MYHEUXNQ NHXPWm5KSzVyPUG5MlA6KM7:TR?= NUHEcYR{OjV4MEm5NlM>
NCI-N78 NE\5XVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLSNlUh|ryP MoLINlQhcA>? M4TFTGROW09? NYn2NJJZUUN3ME2yOk4{OyEQvF2= MkS0NlU3ODl7MkO=
AGS NWLsenJkSXCxcITvd4l{KEG|c3H5 M3XLe|Uh|ryP MUWyOEBp NUnyR4pzTE2VTx?= NUXXd4Y1UW6mdXPld{BieG:ydH;zbZM> M1\MXVI2PjB7OUKz
NCI-N78 NGn3[JJCeG:ydH;zbZMhSXO|YYm= NHLSbYk2KM7:TR?= NF2yW4wzPCCq M33ISGROW09? M4H0N2lv\HWlZYOgZZBweHSxc3nz NFfNbXIzPTZyOUmyNy=>
AGS NWnNdJI4TnWwY4Tpc44hSXO|YYm= NWTIbGdJPSEQvF2= MmrENlQhcA>? NHPRWFRFVVOR NUX4Tm5oUW6mdXPld{B1cGViYYX0c5Bp[We7 NILHTlAzPTZyOUmyNy=>
NCI-N78 NYPaNVluTnWwY4Tpc44hSXO|YYm= M4C2dFUh|ryP NFXjO5QzPCCq MYPEUXNQ MWrJcoR2[2W|IITo[UBifXSxcHjh[5k> NHX4O2QzPTZyOUmyNy=>
HSC-3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\KZYhWOSEQvF2= M1Hub|Q5KGh? NHTKRXNKSzVyPUCuOVQh|ryP NHLMWm8zPTN4NkG0Ny=>
GB30 M4nWWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqxJO69VQ>? NYX5emVMPyCm MojhSG1UVw>? NXjuUIZGUUN3ME2wMlAyOSEQvF2= NGOwVnQzPTFyNkSyPC=>
GB9 NGLCNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTDbpN7OSEQvF2= NGqwTYQ4KGR? MVrEUXNQ M37Ke2lEPTB;MD6wNlQh|ryP NYW5fJV[OjVzME[0Nlg>
GB169 NH\IXINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqxJO69VQ>? NX3pUYptPyCm NWTXWlYxTE2VTx?= MXzJR|UxRTBwMEOyJO69VQ>? NWTYbGNROjVzME[0Nlg>
T24 M1SxOWZ2dmO2aX;uJGF{e2G7 MVSxJO69VQ>? MXG0PEBp MUXEUXNQ NGf4SWhKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MYeyN|QxOzZ|Mx?=
RT4 M1TremZ2dmO2aX;uJGF{e2G7 NFLnXGgyKM7:TR?= NHLoO3k1QCCq M1;YT2ROW09? M2HyWWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NHq5XHAzOzRyM{[zNy=>
UM-UC-3 MXzGeY5kfGmxbjDBd5NigQ>? MUWxJO69VQ>? MYe0PEBp MU\EUXNQ M3G1eWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NF7Jd|kzOzRyM{[zNy=>
T24 M2K5R2Fxd3C2b4Ppd{BCe3OjeR?= NFvsT48{NjF4IN88US=> MnvIPVYhcA>? NULB[5JlTE2VTx?= NVvSfI9IUUN3ME2wMlA{ODZizszN NUfHZZBxOjN2MEO2N|M>
RT4 M4nsTWFxd3C2b4Ppd{BCe3OjeR?= NH;mVow{NjF4IN88US=> NE\OTWQ6PiCq NXvEUXJ3TE2VTx?= NYnheHhoUUN3ME2wMlEyQThizszN NH\3SowzOzRyM{[zNy=>
UM-UC-3 NVLlSoRiSXCxcITvd4l{KEG|c3H5 MXizMlE3KM7:TR?= NV[3UFlQQTZiaB?= NV;ObXV3TE2VTx?= NUXPZ|hIUUN3ME2wMlA1PDlizszN NEfOfZgzOzRyM{[zNy=>
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RS4-11 NHP4PHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmruNVAh|ryP MV65OkBp NXrzT404UUN3ME2wMlAyQCEQvF2= MWKyNFExQDN|OB?=
MOLT-4 NH;4[5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[xNEDPxE1? NFHqSJY6PiCq NIDpTpRKSzVyPUCuNFI3KM7:TR?= M3rZTlIxOTB6M{O4
CCRF-CEM NXTFUHJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX76flBIOTBizszN MWK5OkBp M3vTTWlEPTB;MD6wPVQh|ryP MUeyNFExQDN|OB?=
Kasumi-1 NH\uWohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1y0Z|ExKM7:TR?= MYm5OkBp MkniTWM2OD1yLkGwN{DPxE1? M334RVIxOTB6M{O4
Karpas-299 NFrHUJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTNN4RCOTBizszN NVn6ZXRDQTZiaB?= M2LvRWlEPTB;MD6wN|gh|ryP MVOyNFExQDN|OB?=
Ramos-RA1 NYrr[3dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHIOYgyOCEQvF2= M1Pm[Vk3KGh? NEDNSJBKSzVyPUCuNVI4KM7:TR?= NUm2dHR5OjBzMEizN|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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