Alisertib (MLN8237) 化学構造
分子量: 518.92

高品質保証

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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 NXnYU|ViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrXU4QxNjVizszN Mm\PO|IhcA>? NVP6XoJsTE2VTx?= MWfJR|UxRTBwMESg{txO NIrJ[VQzPjF|Nk[4OC=>
LS174T MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1frUlAvPSEQvF2= M16zfVczKGh? NEnIfFlFVVOR M1LIbmlEPTB;MD6wOUDPxE1? MWKyOlE{PjZ6NB?=
T84 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TvdFAvPSEQvF2= NFO5Rm84OiCq NGnPOo9FVVOR Mom0TWM2OD1yLkC5JO69VQ>? M3S0SVI3OTN4Nki0
LS180 Ml3ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz6bYV{OC53IN88US=> M1HIbVczKGh? NUKzU4VpTE2VTx?= M1izbWlEPTB;MTFOwG0> NF:y[4IzPjF|Nk[4OC=>
SW948 M2TvTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXvNE42KM7:TR?= MmrqO|IhcA>? NEnkcpVFVVOR MkjoTWM2OD1zIN88US=> MWCyOlE{PjZ6NB?=
HCT15 NE\GSXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVewMlUh|ryP NXq3TYFEPzJiaB?= MnXmSG1UVw>? NHr2b4VKSzVyPECuOEDPxE1? MlzmNlYyOzZ4OES=
DLD-1 M{m4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoqwNE42KM7:TR?= NEPCSW04OiCq MW\EUXNQ Mmq0TWM2ODxyLkig{txO M4\OS|I3OTN4Nki0
MIP-101 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTYVnExNjVizszN MkW1O|IhcA>? NIPaOIVFVVOR MnTWTWM2OD1zIN88US=> MVOyOlE{PjZ6NB?=
SNU1544 NXWyN|ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6wMlUh|ryP NEH6dlE4OiCq MYLEUXNQ NFXlOWJKSzVyPUGg{txO MkPDNlYyOzZ4OES=
OCI-Ly10 MWTDfZRwfG:6aXOgRZN{[Xl? MVG3NkBp M2K3emROW09? Mnv2TWM2OD1yLkC1PEDPxE1? NGXJWIozPTh5OEOzNS=>
SU-DHL2 M{\CdGN6fG:2b4jpZ{BCe3OjeR?= M3ixO|czKGh? NXP1XlZ2TE2VTx?= MoK0TWM2OD1yLkCxJO69VQ>? MUeyOVg4QDN|MR?=
OCI-LY7 M1npXmN6fG:2b4jpZ{BCe3OjeR?= M4nOW|czKGh? MUnEUXNQ NYqzPXo{UUN3ME2wMlA5OSEQvF2= NVvy[WJIOjV6N{izN|E>
SU-DHL6 MVPDfZRwfG:6aXOgRZN{[Xl? NHn2dZk4OiCq NF3STIFFVVOR NUW4eI01UUN3ME2wMlQ5OiEQvF2= MVKyOVg4QDN|MR?=
Jeko-1 MV;DfZRwfG:6aXOgRZN{[Xl? NEHHelI4OiCq MlLuSG1UVw>? MVLJR|UxRTBwMEK5JO69VQ>? Mmj5NlU5Pzh|M{G=
JVM-2 MX;DfZRwfG:6aXOgRZN{[Xl? M1P2WFczKGh? NYHl[3RSTE2VTx?= Mn3qTWM2OD1yLkCxJO69VQ>? M3XGXVI2QDd6M{Ox
Rec-1 MnruR5l1d3SxeHnjJGF{e2G7 MnzpO|IhcA>? MkHqSG1UVw>? MnrPTWM2OD1yLkC4O{DPxE1? M2PuO|I2QDd6M{Ox
Z-138 Mli3R5l1d3SxeHnjJGF{e2G7 NFHzWmQ4OiCq NGXVUlhFVVOR NH\wSoRKSzVyPUCuNFE{KM7:TR?= NV7yeI9jOjV6N{izN|E>
H9 NH;jXmdEgXSxdH;4bYMhSXO|YYm= NEW5T|c4OiCq NFPUVpBFVVOR MUfJR|UxRTBwNjFOwG0> MmXxNlU5Pzh|M{G=
HH MnvnR5l1d3SxeHnjJGF{e2G7 M1LLcFczKGh? NXHEWXFkTE2VTx?= NFO0VFRKSzVyPUCuO{DPxE1? MVOyOVg4QDN|MR?=
DND41 NUfHVoFpS3m2b4TvfIlkKEG|c3H5 NIL5U5A4OiCq MUfEUXNQ NWDJdG1yUUN3ME2wMlEh|ryP MX6yOVg4QDN|MR?=
CCL119 NUjuPWdYS3m2b4TvfIlkKEG|c3H5 M{\1NFczKGh? MlHnSG1UVw>? MnjJTWM2OD1yLkC2NkDPxE1? NHi5[lIzPTh5OEOzNS=>
J.Cam 1.6 NIjJTItEgXSxdH;4bYMhSXO|YYm= NE[5fY04OiCq NFu0NohFVVOR NVXTbotYUUN3ME2wMlExPSEQvF2= M1fuWlI2QDd6M{Ox
Sup-T1 MYfDfZRwfG:6aXOgRZN{[Xl? M2PxWVczKGh? MoX4SG1UVw>? NIPP[3hKSzVyPUKuNVQzKM7:TR?= NHe0[pkzPTh5OEOzNS=>
Tib 152 M3XvWGN6fG:2b4jpZ{BCe3OjeR?= NGXHeJk4OiCq MWDEUXNQ MkToTWM2OD1yLkig{txO NYDCd|N7OjV6N{izN|E>
MCF7 MkDUSpVv[3Srb36gRZN{[Xl? MXq1JO69VQ>? M{m3[VI1KGh? NIjJc3pFVVOR M2ruSWlv\HWlZYOgS|IwVSCjcoLld5Q> NEH0doYzPTh|NESwNS=>
MDA-MB-231 M3PtSmZ2dmO2aX;uJGF{e2G7 M{PIZVUh|ryP NX;LNml1OjRiaB?= NXTQ[VNLTE2VTx?= MWHJcoR2[2W|IFezM20h[XK{ZYP0 MXWyOVg{PDRyMR?=
MCF7 MmDXSpVv[3Srb36gRZN{[Xl? NYrXbmNSPSEQvF2= MmPoNlQhcA>? NX76Vo9CTE2VTx?= NHr6VmZF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy M4HEZVI2QDN2NECx
MCF7 NXrDcWxtTnWwY4Tpc44hSXO|YYm= MnfROUDPxE1? MkHBNlQhcA>? NVX2e4JnTE2VTx?= NUTWNGNTTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? NFHwZnYzPTh|NESwNS=>
MCF7 MVTGeY5kfGmxbjDBd5NigQ>? NH3LdoE2KM7:TR?= MX:yOEBp NV3v[VdDTE2VTx?= Mny3SIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIHP5Z4xqdiCEMR?= NXTPXFVOOjV6M{S0NFE>
MCF7 MYTGeY5kfGmxbjDBd5NigQ>? MWe1JO69VQ>? M1fiZlI1KGh? M1KxV2ROW09? MXfJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> MYWyOVg{PDRyMR?=
MCF7 MU\GeY5kfGmxbjDBd5NigQ>? MkPQOUDPxE1? MlXpNlQhcA>? MoG5SG1UVw>? M3\2Z2lv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= NUP0SJlwOjV6M{S0NFE>
MDA-MB-231 M2PkVWZ2dmO2aX;uJGF{e2G7 M2jiOVUh|ryP NHW1VnAzPCCq MmKxSG1UVw>? NHz0N2NF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy NGLq[HQzPTh|NESwNS=>
MDA-MB-231 NESwUopHfW6ldHnvckBCe3OjeR?= MlLzNUDPxE1? M4PuUFI1KGh? NI\ZeWtFVVOR MYHJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=> NWD4SYlXOjV6M{S0NFE>
MDA-MB-231 MYrGeY5kfGmxbjDBd5NigQ>? NW\vcm1ZPSEQvF2= NGHTSFgzPCCq MU\EUXNQ MljMSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIHP5Z4xqdiCEMR?= MXGyOVg{PDRyMR?=
MDA-MB-231 Mk\LSpVv[3Srb36gRZN{[Xl? MmKzOUDPxE1? MYqyOEBp Mn7USG1UVw>? NYnrflVCUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? Moe5NlU5OzR2MEG=
MDA-MB-231 NEHuRVRHfW6ldHnvckBCe3OjeR?= M1PCbFUh|ryP M3Hlc|I1KGh? NIXWcFJFVVOR Mlv5TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz M{TWOlI2QDN2NECx
MDA-MB-231 M3vxU2Z2dmO2aX;uJGF{e2G7 Mm\BOUDPxE1? MmLQNlQhcA>? MoriSG1UVw>? NES1eGtKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFU{ MUOyOVg{PDRyMR?=
MCF7 M{fT[mFxd3C2b4Ppd{BCe3OjeR?= NXrBTXM{PSEQvF2= MX6yOEBp M363dWROW09? NYHqOZJ3UW6mdXPld{BieG:ydH;0bYMh\GWjdHi= NVTET2VtOjV6M{S0NFE>
MDA-MB-231 M1XMUWFxd3C2b4Ppd{BCe3OjeR?= NXi4TpBSPSEQvF2= M4GwSlI1KGh? MnrNSG1UVw>? NHX5UJNKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= MlLPNlU5OzR2MEG=
MCF7 NGj1RXhHfW6ldHnvckBCe3OjeR?= NIrnVYoyKM7:TR?= NH\2cmU4OiCq M3e4O2ROW09? M1v3SWlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= MVSyOVg{PDRyMR?=
MDA-MB-231 Moj0SpVv[3Srb36gRZN{[Xl? NHXUSFAyKM7:TR?= M4Dic|czKGh? MV3EUXNQ M3HkTWlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= MXWyOVg{PDRyMR?=
U-2 OS NXuw[G1OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYi1NEDPxE1? NEjqPZczPCCq NEX4N|dFVVOR M1;Hb2lEPTB;MU[uOkDPxE1? MX6yOVc6OjhzMR?=
MG-63 NV;OV29IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O5UlUxKM7:TR?= Ml\5NlQhcA>? Mn3TSG1UVw>? NEPWdVFKSzVyPUmuOUDPxE1? MYGyOVc6OjhzMR?=
U-2 OS MWnBdI9xfG:|aYOgRZN{[Xl? M1PyW|Uh|ryP Moe0NlQhcA>? MlH5SG1UVw>? Mmq4TY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> NHfrc3EzPTd7MkixNS=>
MG-63 NYHDc3Y1SXCxcITvd4l{KEG|c3H5 Moj1OUDPxE1? MXGyOEBp NFHFepRFVVOR NES0WIlKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp M2DycFI2Pzl{OEGx
U-2 OS Mli4SpVv[3Srb36gRZN{[Xl? NGexdHQ2KM7:TR?= MmjYNlQhcA>? MUDEUXNQ NFHwe3VRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? M1fsR|I2Pzl{OEGx
MG-63 M2jETGZ2dmO2aX;uJGF{e2G7 NHHPdZM2KM7:TR?= MXuyOEBp M1LLd2ROW09? MnPrVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MmPxNlU4QTJ6MUG=
PANC-1 NUPnbXdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr4dpc2OCEQvF2= NHTKbXYzPCCq MYHEUXNQ M4jjbGlEPTB;Nz6xJO69VQ>? M1rPS|I2PjN{MkK1
BxPC-3 NGWyPXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWe1NEDPxE1? MV2yOEBp MXHEUXNQ NXXqSXBSUUN3ME22Mlgh|ryP M3PidVI2PjN{MkK1
PANC-1 NVTzUo02TnWwY4Tpc44hSXO|YYm= NH\HXJU2KM7:TR?= M4PUXlI1KGh? M3zBVWROW09? MWjJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> NF\TXnMzPTZ|MkKyOS=>
BxPC-3 M2CxR2Z2dmO2aX;uJGF{e2G7 NYXafFBpPSEQvF2= NGDRTW4zPCCq NXHKXlFTTE2VTx?= M1XQVmlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hTzJxTTDwbIF{\Q>? M{nTRVI2PjN{MkK1
PANC-1 NWmz[YZ3TnWwY4Tpc44hSXO|YYm= NXvUTZdlPSEQvF2= NEDGenYzPCCq NHjoUW9FVVOR M3nH[Glv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MWGyOVY{OjJ{NR?=
BxPC-3 NWTGNGhRTnWwY4Tpc44hSXO|YYm= M{GyNFUh|ryP MVuyOEBp NIrPXmZFVVOR M{XLXGlv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp Moe4NlU3OzJ{MkW=
SKOV3 NGnvPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7uNVAxKM7:TR?= MmrHNlQhcA>? NIrNNHpFVVOR MW\JR|UxRTJyLkS4JO69VQ>? NYS2ZWtROjV4MkS3OVA>
OVCAR4 NUjGcm5xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTxW4hKOTByIN88US=> NUfvbHRWOjRiaB?= NXjFW41XTE2VTx?= M2fXSWlEPTB;MkKuNVMh|ryP NEHqRZYzPTZ{NEe1NC=>
SKOV3 NVjwSIdFTnWwY4Tpc44hSXO|YYm= NYPtcJRxPSEQvF2= NUPLeHY2PzJiaB?= NXPIPWlvTE2VTx?= NUTkS5BwUW6mdXPld{BIOi:PIHHydoV{fA>? NIjJSHIzPTZ{NEe1NC=>
OVCAR4 NVjWb2Y{TnWwY4Tpc44hSXO|YYm= NXvRUogyPSEQvF2= NWTkT21PPzJiaB?= NUnmdIY{TE2VTx?= NGHUdIhKdmS3Y3XzJGczN01iYYLy[ZN1 M4XsSVI2PjJ2N{Ww
SKOV3 MkHLRZBweHSxc3nzJGF{e2G7 NHHDNJU2KM7:TR?= MkHINlQhcA>? M2HGWWROW09? NHPMWVFKdmS3Y3XzJIFxd3C2b4Ppdy=> NIPkNXIzPTZ{NEe1NC=>
OVCAR4 NUWwcWNJSXCxcITvd4l{KEG|c3H5 MoLGOUDPxE1? NGXuN|czPCCq M4ntZ2ROW09? NIPmbZhKdmS3Y3XzJIFxd3C2b4Ppdy=> NEfSNYEzPTZ{NEe1NC=>
AGS MkXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofXNlUh|ryP MX:yOEBp MW\EUXNQ M1;oZWlEPTB;MUmuNFkh|ryP MoPxNlU3ODl7MkO=
NCI-N78 M3nTR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;qOVI2KM7:TR?= NHn3d20zPCCq NVnsW45HTE2VTx?= NXPBcFhiUUN3ME2yOk4{OyEQvF2= NYO1RnAyOjV4MEm5NlM>
AGS NY\DUoVQSXCxcITvd4l{KEG|c3H5 NXTqNHd4PSEQvF2= Mm\nNlQhcA>? MUHEUXNQ MlvsTY5lfWOnczDhdI9xfG:|aYO= NGX3bmwzPTZyOUmyNy=>
NCI-N78 NVLsTZh{SXCxcITvd4l{KEG|c3H5 MVO1JO69VQ>? NEDTW|kzPCCq M2fONGROW09? NV3ESJJ5UW6mdXPld{BieG:ydH;zbZM> MmnNNlU3ODl7MkO=
AGS NU[4eG1vTnWwY4Tpc44hSXO|YYm= MYG1JO69VQ>? M3HjV|I1KGh? NHjodGdFVVOR M1;XSWlv\HWlZYOgeIhmKGG3dH;wbIFogQ>? MVGyOVYxQTl{Mx?=
NCI-N78 M1vyNmZ2dmO2aX;uJGF{e2G7 NULoSW5rPSEQvF2= NY\vdIVWOjRiaB?= Mk\zSG1UVw>? NEDQPWhKdmS3Y3XzJJRp\SCjdYTvdIhi\3l? NVO4UY5COjV4MEm5NlM>
HSC-3 NUXjOVFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvOTFFpOSEQvF2= NHKwOnE1QCCq Mkj2TWM2OD1yLkW0JO69VQ>? MlnaNlU{PjZzNEO=
GB30 NE\zepJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTGbnZGOSEQvF2= M3TvbFch\A>? MVTEUXNQ Mkm0TWM2OD1yLkCxNUDPxE1? NW\NSINtOjVzME[0Nlg>
GB9 NHL2VJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXexJO69VQ>? M2rkOVch\A>? MnflSG1UVw>? M1XSUGlEPTB;MD6wNlQh|ryP MVeyOVExPjR{OB?=
GB169 NEe0cnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7vNUDPxE1? NHK1W4U4KGR? NF\hc5JFVVOR MlPrTWM2OD1yLkCzNkDPxE1? Ml;UNlUyODZ2Mki=
T24 M3zx[GZ2dmO2aX;uJGF{e2G7 NIX6cIEyKM7:TR?= M{DMT|Q5KGh? M{LnW2ROW09? M2Llb2lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MnHrNlM1ODN4M{O=
RT4 MmjFSpVv[3Srb36gRZN{[Xl? NXXSeVJkOSEQvF2= NF;vd|Y1QCCq MnHvSG1UVw>? Mle3TY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M1zxPVI{PDB|NkOz
UM-UC-3 NFPZcWhHfW6ldHnvckBCe3OjeR?= MV:xJO69VQ>? MojYOFghcA>? M2nZT2ROW09? M4PoXWlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NWjGUGF5OjN2MEO2N|M>
T24 MVHBdI9xfG:|aYOgRZN{[Xl? MkDpN{4yPiEQvF2= M3TUflk3KGh? MX\EUXNQ Mlj5TWM2OD1yLkCzNFYh|ryP NYDvVYd[OjN2MEO2N|M>
RT4 NVL2R|VOSXCxcITvd4l{KEG|c3H5 MmPjN{4yPiEQvF2= M4LNPFk3KGh? NGLlO49FVVOR Mmm4TWM2OD1yLkGxPVgh|ryP MlrwNlM1ODN4M{O=
UM-UC-3 NUDFcpJTSXCxcITvd4l{KEG|c3H5 M2jZdVMvOTZizszN MmLQPVYhcA>? NXnOfllkTE2VTx?= M1\UeWlEPTB;MD6wOFQ6KM7:TR?= MYiyN|QxOzZ|Mx?=
OVCAR-5 NGrnPHBHfW6ldHnvckBCe3OjeR?= NWPjcJprPTBibl2= NWj2d5Z1UW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NInNW3EzOzN|NEOyOy=>
SKOV3ip2 NGfCcZhHfW6ldHnvckBCe3OjeR?= MWC1NEBvVQ>? MV\Jcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? MYKyN|M{PDN{Nx?=
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MOLT-4 M{SxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TNXVExKM7:TR?= MVy5OkBp NEX2dFZKSzVyPUCuNFI3KM7:TR?= MUGyNFExQDN|OB?=
CCRF-CEM M4f0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4G4b|ExKM7:TR?= NFnOZmY6PiCq NWqyd2F1UUN3ME2wMlA6PCEQvF2= MV:yNFExQDN|OB?=
Kasumi-1 MnnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j1eFExKM7:TR?= MnHEPVYhcA>? NF;pVHlKSzVyPUCuNVA{KM7:TR?= NYLzUW9lOjBzMEizN|g>
Karpas-299 NEH4UmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fLe|ExKM7:TR?= M3;4VVk3KGh? M{K3OGlEPTB;MD6wN|gh|ryP NYfYOJBIOjBzMEizN|g>
Ramos-RA1 MoPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M130b|ExKM7:TR?= Ml3xPVYhcA>? MUjJR|UxRTBwMUK3JO69VQ>? NESycJIzODFyOEOzPC=>

... 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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