Alisertib (MLN8237)

For research use only. Not for use in humans.

目录号:S1133 中文名称:阿利色替

Alisertib (MLN8237) Chemical Structure

CAS No. 1028486-01-2

Alisertib (MLN8237)是一种选择性Aurora A抑制剂,无细胞试验中IC50为1.2 nM,作用于Aurora A比作用于Aurora B选择性强200倍以上。Alisertib 可诱导细胞周期阻滞、细胞凋亡与自噬。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1375.12 现货
RMB 983.87 现货
RMB 1725.78 现货
RMB 5505.84 现货
RMB 14496.3 现货
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客户使用Selleck生产的Alisertib (MLN8237)发表文献254篇:

产品安全说明书

Aurora Kinase抑制剂选择性比较

生物活性

产品描述 Alisertib (MLN8237)是一种选择性Aurora A抑制剂,无细胞试验中IC50为1.2 nM,作用于Aurora A比作用于Aurora B选择性强200倍以上。Alisertib 可诱导细胞周期阻滞、细胞凋亡与自噬。Phase 3。
特性 MLN8237 是第一个口服有效的小分子Aurora A激酶选择性抑制剂。
靶点
Aurora A [1]
(Cell-free assay)
1.2 nM
体外研究

MLN8237作用于Aurora A选择性比作用于结构相关的Aurora B 高200多倍,IC50为396.5 nM, 而对205种其他激酶则没有显著活性。[1] 0.5 μM MLN8237处理MM1.S和 OPM1 细胞,抑制 Aurora A磷酸化,而不影响 Aurora B调节的组蛋白H3磷酸化。MLN8237作用于多发性骨髓瘤(MM) 细胞系,显著抑制细胞增殖,IC50为0.003-1.71 μM。在BM 基质细胞,IL-6和 IGF-1 存在时,MLN8237作用于原代MM 细胞和MM细胞系,抗增殖活性比只有MLN8237单独作用时高很多。0.5 μM MLN8237 作用于原代MM细胞和细胞系,使G2/M 期细胞提高2到6倍,且显著诱导凋亡和衰老,涉及p53, p21 和p27的上调,及 PARP,caspase 3,和 caspase 9的裂解。此外, MLN8237和 Dexamethasone联用具有协同作用,具有强抗MM 功效, 而和Doxorubicin 及Bortezomib联用则具有另外的功能。[2] 0.5 μM MLN8237处理 FLO-1, OE19, 和OE33 食管腺癌细胞系,抑制集落形成,且显著提高多倍体细胞百分数,随后提高G1期细胞百分数,而与 Cisplatin (2.5 μM)联用则效果进一步提高,与单独用药相比,诱导产生更多, TAp73β, PUMA, NOXA, cleaved caspase-3, 和cleaved PARP。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 NXjwbnp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWewMlUh|ryP MX23NkBp NUWwUJdOTE2VTx?= NGPTSJBKSzVyPUCuNFQh|ryP NWXsVVBQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xN|Y3QDRpPkK2NVM3Pjh2PD;hQi=>
LS174T NIL3TnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\2XVAvPSEQvF2= M1u4U|czKGh? MVLEUXNQ NVHCT2NjUUN3ME2wMlA2KM7:TR?= MmTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzM{[2PFQoRjJ4MUO2Olg1RC:jPh?=
T84 M4nPRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXOcFZQOC53IN88US=> MnXtO|IhcA>? MX3EUXNQ MXvJR|UxRTBwMEmg{txO NHLuNZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGzOlY5PCd-Mk[xN|Y3QDR:L3G+
LS180 M1vHTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nPVVAvPSEQvF2= MX63NkBp NEH6XoFFVVOR Ml3UTWM2OD1zIN88US=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF|Nk[4OEc,OjZzM{[2PFQ9N2F-
SW948 MmHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTY[GdCOC53IN88US=> M1;K[VczKGh? NWrldlBkTE2VTx?= NGnJfopKSzVyPUGg{txO MorJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzM{[2PFQoRjJ4MUO2Olg1RC:jPh?=
HCT15 M{DjPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKwMlUh|ryP MVm3NkBp MVHEUXNQ MWHJR|UxRDBwNDFOwG0> M1LkfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUO2Olg1Lz5{NkGzOlY5PDxxYU6=
DLD-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LCV|AvPSEQvF2= M{HYelczKGh? MXjEUXNQ NV\PcpIzUUN3MEywMlgh|ryP M1nQfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUO2Olg1Lz5{NkGzOlY5PDxxYU6=
MIP-101 MmDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmwMlUh|ryP MnfWO|IhcA>? MYfEUXNQ NEPu[4pKSzVyPUGg{txO NEjuVFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGzOlY5PCd-Mk[xN|Y3QDR:L3G+
SNU1544 NH7yblVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3zZ3ZzOC53IN88US=> MYK3NkBp NXzq[lFkTE2VTx?= MUjJR|UxRTFizszN NU[5N2ttRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xN|Y3QDRpPkK2NVM3Pjh2PD;hQi=>
OCI-Ly10 M{HBWGN6fG:2b4jpZ{BCe3OjeR?= MWO3NkBp MmS5SG1UVw>? MWTJR|UxRTBwMEW4JO69VQ>? NVf1bZBGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4O|g{OzFpPkK1PFc5OzNzPD;hQi=>
SU-DHL2 MlKxR5l1d3SxeHnjJGF{e2G7 NH:5PW84OiCq NInIbYpFVVOR M{jlUmlEPTB;MD6wNUDPxE1? NWPkdYUzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4O|g{OzFpPkK1PFc5OzNzPD;hQi=>
OCI-LY7 MnPnR5l1d3SxeHnjJGF{e2G7 M2foXlczKGh? MVLEUXNQ MUHJR|UxRTBwMEixJO69VQ>? M1rQfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEe4N|MyLz5{NUi3PFM{OTxxYU6=
SU-DHL6 MlX6R5l1d3SxeHnjJGF{e2G7 Mk\0O|IhcA>? NUjPSWJETE2VTx?= MV;JR|UxRTBwNEiyJO69VQ>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
Jeko-1 NIHuPXBEgXSxdH;4bYMhSXO|YYm= M3;Gb|czKGh? Mkj3SG1UVw>? M2XvRmlEPTB;MD6wNlkh|ryP MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
JVM-2 NVnzPHZpS3m2b4TvfIlkKEG|c3H5 NY\wfZFFPzJiaB?= NX\XUWFRTE2VTx?= Ml;TTWM2OD1yLkCxJO69VQ>? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
Rec-1 MVnDfZRwfG:6aXOgRZN{[Xl? NXrGOYZYPzJiaB?= M{LJcmROW09? NFjrS5BKSzVyPUCuNFg4KM7:TR?= NHvVRY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi3PFM{OSd-MkW4O|g{OzF:L3G+
Z-138 MX;DfZRwfG:6aXOgRZN{[Xl? MX:3NkBp M3;JWmROW09? MYnJR|UxRTBwMEGzJO69VQ>? M2OzfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEe4N|MyLz5{NUi3PFM{OTxxYU6=
H9 Mn3OR5l1d3SxeHnjJGF{e2G7 MVW3NkBp MkPmSG1UVw>? NYX2S4xsUUN3ME2wMlYh|ryP NXGxT4NuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4O|g{OzFpPkK1PFc5OzNzPD;hQi=>
HH NVH4WI5kS3m2b4TvfIlkKEG|c3H5 M3TnNlczKGh? MVvEUXNQ M4nZUWlEPTB;MD63JO69VQ>? MkO0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
DND41 M13zVWN6fG:2b4jpZ{BCe3OjeR?= NV3MZo9mPzJiaB?= NFvGNYtFVVOR NVLMVlFjUUN3ME2wMlEh|ryP NWnOeWtORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4O|g{OzFpPkK1PFc5OzNzPD;hQi=>
CCL119 M2DkSWN6fG:2b4jpZ{BCe3OjeR?= NEPFTYY4OiCq MmXHSG1UVw>? MXnJR|UxRTBwME[yJO69VQ>? M1Gy[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEe4N|MyLz5{NUi3PFM{OTxxYU6=
J.Cam 1.6 NFroTnNEgXSxdH;4bYMhSXO|YYm= NVHPd2doPzJiaB?= MYHEUXNQ NF\FR3RKSzVyPUCuNVA2KM7:TR?= NFzkXZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi3PFM{OSd-MkW4O|g{OzF:L3G+
Sup-T1 MWLDfZRwfG:6aXOgRZN{[Xl? NVrXZWVXPzJiaB?= MUfEUXNQ NF\1cIVKSzVyPUKuNVQzKM7:TR?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
Tib 152 MlHaR5l1d3SxeHnjJGF{e2G7 MXm3NkBp MWPEUXNQ NUeze5NMUUN3ME2wMlgh|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
MCF7 NWG3dmg2TnWwY4Tpc44hSXO|YYm= NUfKWGprPSEQvF2= Mn;pNlQhcA>? MonTSG1UVw>? M{e1Zmlv\HWlZYOgS|IwVSCjcoLld5Q> NV[4N4FNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 M4PlZmZ2dmO2aX;uJGF{e2G7 MWG1JO69VQ>? M3O4cFI1KGh? MmDKSG1UVw>? MWnJcoR2[2W|IFezM20h[XK{ZYP0 NIX5R5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MCF7 NWrzd3MyTnWwY4Tpc44hSXO|YYm= MkTBOUDPxE1? MnW3NlQhcA>? NXPQU|dmTE2VTx?= NVPCfXRnTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzFxQ1TDNi=> NVPTcpp{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MCF7 MWTGeY5kfGmxbjDBd5NigQ>? NEO4N4o2KM7:TR?= NULidY5LOjRiaB?= M2LvU2ROW09? M{jVVWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz MojnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{S0NFEoRjJ3OEO0OFAyRC:jPh?=
MCF7 M4LLOWZ2dmO2aX;uJGF{e2G7 NIXaZ4Y2KM7:TR?= MknONlQhcA>? NIT2VnFFVVOR MVTE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MCF7 MVLGeY5kfGmxbjDBd5NigQ>? NV;LOm9UPSEQvF2= NHzZV2MzPCCq M2LRc2ROW09? NGTRVJJKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFIyKFejZkGvR4lxOQ>? NUK1O2prRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MCF7 NUTPTndOTnWwY4Tpc44hSXO|YYm= M2G1WVUh|ryP M2O5dVI1KGh? MXzEUXNQ NUXMS4F2UW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzPyCNaYCx NViz[W1HRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 M12wXWZ2dmO2aX;uJGF{e2G7 NXLRcWgzPSEQvF2= NGLO[ogzPCCq MkLOSG1UVw>? MlG4SIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|EwS0SFMh?= NV[5NWNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 M2[1cGZ2dmO2aX;uJGF{e2G7 M{P2Z|Eh|ryP MUOyOEBp M2jkOmROW09? M3GyUWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz M3LZZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO0OFAyLz5{NUizOFQxOTxxYU6=
MDA-MB-231 NYX2VnBWTnWwY4Tpc44hSXO|YYm= MXe1JO69VQ>? MYqyOEBp MYTEUXNQ M{\QeWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDjfYNtcW5iQkG= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MDA-MB-231 MlXDSpVv[3Srb36gRZN{[Xl? MmjROUDPxE1? NXTWWlg4OjRiaB?= NUTIPWhuTE2VTx?= Ml\6TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> NWD4OVFPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 NGP2fohHfW6ldHnvckBCe3OjeR?= NYjHbm1jPSEQvF2= MnnmNlQhcA>? M{DPcmROW09? NEHiNZlKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= M3LzUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO0OFAyLz5{NUizOFQxOTxxYU6=
MDA-MB-231 MkXrSpVv[3Srb36gRZN{[Xl? M{HPfFUh|ryP MV[yOEBp NXrYXYF7TE2VTx?= MYrJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEWz MlTJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{S0NFEoRjJ3OEO0OFAyRC:jPh?=
MCF7 Mn;lRZBweHSxc3nzJGF{e2G7 MmDlOUDPxE1? MYeyOEBp MoPvSG1UVw>? MlX2TY5lfWOnczDhdI9xfG:2aXOg[IVifGh? NFKzWos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MDA-MB-231 NHfOcHVCeG:ydH;zbZMhSXO|YYm= M{XvTlUh|ryP NH;2b|IzPCCq MmHLSG1UVw>? MmL0TY5lfWOnczDhdI9xfG:2aXOg[IVifGh? NXnyeWFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
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LAN-5 MX;xTHRUKGG|c3H5 MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NYPtNIFmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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SK-N-MC NGn4W4lyUFSVIHHzd4F6 MnHKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>? M3[2NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32 M1\ZbJFJXFNiYYPzZZk> MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz MkG3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 NEPmcm1yUFSVIHHzd4F6 M3HoUZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNid3NvMjDj[Yxtew>? MkDRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AURKA(T288) / p-EIF4E(S209) / c-Myc; 

PubMed: 28073841     


Inhibition of AURKA with alisertib downregulated p-EIF4E (S209) and c-MYC protein levels as assayed by Western blotting.

phospho-Aurora A / Aurora B; 

PubMed: 22863010     


MLN8237differentially inhibited phosphorylation of Aurora kinases. CMK cells were incubated with 0.1 µM paclitaxel for 18 hr, then DMSO or MLN8237 was added and incubated for 2 hr. The degree of phosphorylation of the Aurora kinases in each sample was determined by Western blot.

H3S10P / H3K27me2 / H3K27me3 / H3K9me2 / H3AcK / H4K16Ac; 

PubMed: 29477140     


THP-1 cells were treated with alisertib or DMSO for 48 h. The levels of histone modifications were detected by western blot analysis with the indicated antibodies. H3 was used as a loading control.

28073841 22863010 29477140
Growth inhibition assay
Cell viability; 

PubMed: 25632225     


PANC-1 and BxPC-3 cells were treated with ALS at concentrations ranging from 0.1 μM to 50 μM for 24 hours. The viability of PANC-1 and BxPC-3 cells determined by MTT assay. ALS, alisertib.

25632225
Immunofluorescence
acetylated α-tubulin / γ-tubulin; 

PubMed: 29401581     


Representative immunofluorescence (IF) image and graph in human PKD1-mutant WT9-7, WT9-12 cells or hTERT-RPE1 (RPE1) cells after 2 hours treatment with vehicle, ganetespib , or alisertib to inhibit AURKA, or combination of alisertib and ganetespib. acetylated α-tubulin (red); γ-tubulin (green); DAPI (blue). Scale bars, 5 μm.

E-cadherin / β-catenin / vimentin / p-SMAD5; 

PubMed: 23334326     


Immunofluorescence analysis of CD24 (-/low) cells treated with1 μM MLN8237 for 48 and 72 h showing reversion of EMT. E-cadherin and p-SMAD5 were labeled in red, β-catenin and vimentin were labeled in green, and DNA was labeled in blue with Hoechst dye.

Centrin-2 / tubulin; 

PubMed: 30899434     


Following inhibition of Aurora A kinase activity with 100 nM alisertib, cells with two or excess centrosomes similarly exhibit disorganized mitotic spindles. Cells with extra centrosomes are efficiently clustered into bipolar spindles prior to anaphase onset while those with supernumerary centrosomes undergo multipolar mitoses. Centrin-2, a marker of centrioles is shown in green, tubulin in red, and chromatin in blue. AurA inhibitor: alisertib.

phospho-Aurora A(T288); 

PubMed: 20382844     


MM1.S cells were treated with DMSO or MLN8237 (0.5μM) for 24 hours and then stained with anti-phospho (Thr288)-Aurora-A kinase antibody (red), αtubulin (green), and DNA (blue). Overlapping localization is shown in the merged images. Arrow indicates Aurora-A autophosphorylation on Thr288 in the centrosome (original magnification ×40). Magnified single mitotic cell image is shown in the right panel. 

29401581 23334326 30899434 20382844
体内研究 MLN8237口服处理,显著降低肿瘤负担,按15 mg/kg 和30 mg/kg剂量处理肿瘤生长抑制率(TGI) 分别为42%和80%,且与对照组相比,延迟小鼠寿命。[2] MLN8237 (30 mg/kg) 与Cisplatin (2 mg/kg) 联用作用于FLO-1移植瘤,与单独用药相比,抗癌活性增强,伴随着Ki-67表达受抑制,细胞核p73蛋白和cleaved caspase 3表达增强。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

Aurora A放射性闪光板酶实验:

进行Aurora A放射性闪光板酶实验,测定体外MLN8237抑制程度。在Sf9细胞中表达重组Aurora A,然后使用GST亲和层析进行纯化。Aurora A 肽底物与生物素联合形成生物素-GLRRASLG。在50 mM Hepes (pH 7.5), 10 mM MgCl2, 5 mM DTT, 0.05% Tween-20, 2 μM 肽底物, 3.3 μCi/mL [γ-33 P]ATP 2 μM, 和浓度不断增高的MLN8237 的混合物中进行Aurora A激酶 (5 nM)实验。
细胞实验:[2]
- 合并
  • Cell lines: MM1.S, MM.1R, LR5, RPMI 8226, DOX40, OPM1, OPM2, INA6, 和U266
  • Concentrations: 溶于DMSO,终浓度为~10 μM
  • Incubation Time: 24, 48, 和72小时
  • Method: 使用不同浓度MLN8237处理细胞24, 48,和72小时。通过MTT实验测定细胞活力,通过测定 3[3H]-胸甘渗透而测定细胞增殖。为了分析细胞周期,使用70%乙醇在-20oC下使细胞通透,然后与50 μg/mL PI 和20 单位/mL RNase-A温育。 通过流式细胞仪使用 BDFACS-Canto II和FlowJo软件分析DNA含量。 为了测定凋亡和衰老,使用异硫氰酸荧光素-annexin V和PI对细胞进行染色。通过流式细胞仪使用 BDFACS-Canto II和FlowJo软件测定凋亡细胞。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 皮下接种 MM1.S 细胞的SCID鼠
  • Dosages: ~30 mg/kg/day
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 27 mg/mL (52.03 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5%DMSO+30% PEG300+5%Tween-80+ddH2O
6mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 518.92
化学式

C27H20ClFN4O4

CAS号 1028486-01-2
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04479306 Recruiting Drug: Alisertib|Drug: Osimertinib|Drug: Sapanisertib Recurrent Lung Non-Small Cell Carcinoma|Stage IIIB Lung Cancer AJCC v8|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 M.D. Anderson Cancer Center June 18 2020 Phase 1
NCT02812056 Withdrawn Drug: Alisertib|Drug: TAK-228 Malignant Neoplasms of Digestive Organs|Malignant Neoplasms of Female Genital Organs|Malignant Neoplasms of Lip Oral Cavity and Pharynx|Malignant Neoplasms of Male Genital Organs M.D. Anderson Cancer Center|Millennium Pharmaceuticals Inc. September 2016 Phase 1
NCT02719691 Active not recruiting Drug: Alisertib|Drug: MLN0128 Metastatic Breast Cancer|Solid Tumors University of Colorado Denver May 13 2016 Phase 1
NCT02367352 Terminated Drug: Alisertib|Drug: Paclitaxel Advanced Solid Tumors|Ovarian Cancer|Small Cell Lung Cancer Millennium Pharmaceuticals Inc.|Takeda March 19 2015 Phase 1

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    What is the suggested formulation of this compound for mouse injection(i.p.)?

  • 回答:

    It can be dissolved in 6% DMSO/50% PEG 300/5% Tween 80/ddH2O at 10 mg/ml as a clear solution.

Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

相关Aurora Kinase产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID