Alisertib (MLN8237)

目录号:S1133 中文名称:阿利色替

仅限科研使用

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。

Alisertib (MLN8237) Chemical Structure

CAS: 1028486-01-2

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 5505.84 现货
RMB 14496.3 现货
大包装 有超大折扣

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客户使用Selleck生产的Alisertib (MLN8237)发表文献305篇:

产品安全说明书

Aurora Kinase抑制剂选择性比较

相关Aurora Kinase产品

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 M1ftS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon0NE42KM7:TR?= MXW3NkBp MUTEUXNQ MVPJR|UxRTBwMESg{txO MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF|Nk[4OEc,OjZzM{[2PFQ9N2F-
LS174T MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HOUlAvPSEQvF2= MmO3O|IhcA>? MUTEUXNQ M{LQR2lEPTB;MD6wOUDPxE1? Mn;LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzM{[2PFQoRjJ4MUO2Olg1RC:jPh?=
T84 M2TvZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2m3dVAvPSEQvF2= M1\YSlczKGh? MmLVSG1UVw>? M1XRdGlEPTB;MD6wPUDPxE1? NXzBdXAzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xN|Y3QDRpPkK2NVM3Pjh2PD;hQi=>
LS180 MlnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXaRpYxNjVizszN Mn3oO|IhcA>? NFXSS|hFVVOR MUnJR|UxRTFizszN M{CwUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUO2Olg1Lz5{NkGzOlY5PDxxYU6=
SW948 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTMfIoxNjVizszN M3XwVFczKGh? MoqwSG1UVw>? MWLJR|UxRTFizszN M4C2d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUO2Olg1Lz5{NkGzOlY5PDxxYU6=
HCT15 NWXBV5RQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSwMlUh|ryP NYXBZ2VXPzJiaB?= Mn24SG1UVw>? NE\nVWtKSzVyPECuOEDPxE1? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF|Nk[4OEc,OjZzM{[2PFQ9N2F-
DLD-1 NUXufW9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjqPGUxNjVizszN MonkO|IhcA>? MVLEUXNQ NXq5R2ZxUUN3MEywMlgh|ryP MnW5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzM{[2PFQoRjJ4MUO2Olg1RC:jPh?=
MIP-101 M1q3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXXdHUxOC53IN88US=> MlrVO|IhcA>? MlHZSG1UVw>? MnPUTWM2OD1zIN88US=> M4G4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUO2Olg1Lz5{NkGzOlY5PDxxYU6=
SNU1544 MnvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTaPJk{OC53IN88US=> MlnpO|IhcA>? MYLEUXNQ M13qXmlEPTB;MTFOwG0> NF3PbVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGzOlY5PCd-Mk[xN|Y3QDR:L3G+
OCI-Ly10 MlXzR5l1d3SxeHnjJGF{e2G7 MUW3NkBp NHjXZWRFVVOR NEC1[4JKSzVyPUCuNFU5KM7:TR?= NFnvZXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi3PFM{OSd-MkW4O|g{OzF:L3G+
SU-DHL2 Ml\VR5l1d3SxeHnjJGF{e2G7 M4TiRVczKGh? NUO0S5NVTE2VTx?= MXjJR|UxRTBwMEGg{txO MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
OCI-LY7 NYTFbpdLS3m2b4TvfIlkKEG|c3H5 M2DsSFczKGh? MlTMSG1UVw>? MUnJR|UxRTBwMEixJO69VQ>? M4Xm[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEe4N|MyLz5{NUi3PFM{OTxxYU6=
SU-DHL6 M1X1dWN6fG:2b4jpZ{BCe3OjeR?= M{fmWFczKGh? NIi5cG9FVVOR MYnJR|UxRTBwNEiyJO69VQ>? MnLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
Jeko-1 NFjU[lBEgXSxdH;4bYMhSXO|YYm= M363eVczKGh? NIXVfolFVVOR M{KzdmlEPTB;MD6wNlkh|ryP M3vNOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEe4N|MyLz5{NUi3PFM{OTxxYU6=
JVM-2 NHSzSHlEgXSxdH;4bYMhSXO|YYm= NFrUfm44OiCq M3jPSWROW09? M1fE[2lEPTB;MD6wNUDPxE1? MoHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
Rec-1 NFnvVZJEgXSxdH;4bYMhSXO|YYm= NVXUcYE4PzJiaB?= Ml;MSG1UVw>? NHHJ[mZKSzVyPUCuNFg4KM7:TR?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
Z-138 NFzBS2tEgXSxdH;4bYMhSXO|YYm= M1L5XVczKGh? NEn2VXBFVVOR MXrJR|UxRTBwMEGzJO69VQ>? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
H9 MYXDfZRwfG:6aXOgRZN{[Xl? MnjlO|IhcA>? MUHEUXNQ NIfKepZKSzVyPUCuOkDPxE1? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
HH M121OmN6fG:2b4jpZ{BCe3OjeR?= MnW4O|IhcA>? M4XGVmROW09? M1nFeWlEPTB;MD63JO69VQ>? M3\XdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEe4N|MyLz5{NUi3PFM{OTxxYU6=
DND41 MVzDfZRwfG:6aXOgRZN{[Xl? NHrqVGc4OiCq NXHiO4t4TE2VTx?= MXHJR|UxRTBwMTFOwG0> Mn3CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
CCL119 MWLDfZRwfG:6aXOgRZN{[Xl? M3Pvc|czKGh? NE[xcVdFVVOR NXL6Z4trUUN3ME2wMlA3OiEQvF2= NEj6OYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi3PFM{OSd-MkW4O|g{OzF:L3G+
J.Cam 1.6 MV7DfZRwfG:6aXOgRZN{[Xl? NET6N3I4OiCq NGfre5BFVVOR M2XOWWlEPTB;MD6xNFUh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OEOzNUc,OjV6N{izN|E9N2F-
Sup-T1 Mkn5R5l1d3SxeHnjJGF{e2G7 MWe3NkBp NYXJU|VUTE2VTx?= M4PmZWlEPTB;Mj6xOFIh|ryP NVjzfphxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4O|g{OzFpPkK1PFc5OzNzPD;hQi=>
Tib 152 M4\zTWN6fG:2b4jpZ{BCe3OjeR?= MVe3NkBp NYrjcWg1TE2VTx?= MkG4TWM2OD1yLkig{txO MojoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6N{izN|EoRjJ3OEe4N|MyRC:jPh?=
MCF7 MVfGeY5kfGmxbjDBd5NigQ>? NWOyOXB4PSEQvF2= NUTDUY5nOjRiaB?= NHi5SnBFVVOR MlX3TY5lfWOnczDHNk9OKGG{cnXzeC=> NGLtOmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MDA-MB-231 NGLP[lZHfW6ldHnvckBCe3OjeR?= MYi1JO69VQ>? MmGwNlQhcA>? M1vsfGROW09? NFi5fJJKdmS3Y3XzJGc{N01iYYLy[ZN1 MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MCF7 NIPlfnpHfW6ldHnvckBCe3OjeR?= MljvOUDPxE1? MUKyOEBp M37zOGROW09? NGC0TY5F\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy NGrtOmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MCF7 NHi0OZNHfW6ldHnvckBCe3OjeR?= M4H0c|Uh|ryP NXmyS3dUOjRiaB?= MWLEUXNQ M{Lk[WRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz M4HVZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO0OFAyLz5{NUizOFQxOTxxYU6=
MCF7 MWDGeY5kfGmxbjDBd5NigQ>? NFLub5Y2KM7:TR?= NULRT3R{OjRiaB?= MX;EUXNQ NUHVU5lZTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=> NIHyPZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MCF7 NU\SNFZpTnWwY4Tpc44hSXO|YYm= NGX5boQ2KM7:TR?= M334dlI1KGh? NFP6bG5FVVOR M1;UXGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlEhX2GoMT;DbZAy NX34UmIxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MCF7 MVPGeY5kfGmxbjDBd5NigQ>? NGnvZ4E2KM7:TR?= NFju[YYzPCCq MWXEUXNQ NHq4OIdKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh|NESwNUc,OjV6M{S0NFE9N2F-
MDA-MB-231 NISzOINHfW6ldHnvckBCe3OjeR?= NH\E[WM2KM7:TR?= M2LOVlI1KGh? MkLQSG1UVw>? NIXUfW5F\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy M1nCclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO0OFAyLz5{NUizOFQxOTxxYU6=
MDA-MB-231 NWD6bGpRTnWwY4Tpc44hSXO|YYm= MUOxJO69VQ>? MnHTNlQhcA>? NHvibpFFVVOR NELSWHZKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NXfnO5diRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 NXLxbG1kTnWwY4Tpc44hSXO|YYm= Ml;zOUDPxE1? NGP2OZMzPCCq NH\UXHpFVVOR MWPE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz MlmxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{S0NFEoRjJ3OEO0OFAyRC:jPh?=
MDA-MB-231 NUPx[5pyTnWwY4Tpc44hSXO|YYm= NXKyVolIPSEQvF2= NG\RdnUzPCCq NXzJVINFTE2VTx?= NVLzbXNrUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? NUjnZ5VrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 NWHyfpk1TnWwY4Tpc44hSXO|YYm= MknnOUDPxE1? NFPoVIIzPCCq NGPxVVZFVVOR M1vHbWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= NYL0R3FyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|Q1ODFpPkK1PFM1PDBzPD;hQi=>
MDA-MB-231 NGHrOW9HfW6ldHnvckBCe3OjeR?= M1WyblUh|ryP MU[yOEBp M1jLUWROW09? M{X1fWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwOVM> NFjwOHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
MCF7 NUjZSI9PSXCxcITvd4l{KEG|c3H5 NWDOdHFEPSEQvF2= MUeyOEBp MWPEUXNQ MkDOTY5lfWOnczDhdI9xfG:2aXOg[IVifGh? M2fHO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO0OFAyLz5{NUizOFQxOTxxYU6=
MDA-MB-231 M325dmFxd3C2b4Ppd{BCe3OjeR?= M16zbVUh|ryP NGPBOnkzPCCq MnntSG1UVw>? NHe2VG5KdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= NIPGbHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizOFQxOSd-MkW4N|Q1ODF:L3G+
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LAN-5 NGfCWGpyUFSVIHHzd4F6 M1HUUJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= M{Xkd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 MXjxTHRUKGG|c3H5 MVrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? NHj5XGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC MnnndWhVWyCjc4PhfS=> NF3ZelhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLV3DJINmdGy| MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 MWLxTHRUKGG|c3H5 NFLtfYFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{ MlWzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 M{jreJFJXFNiYYPzZZk> MoPmdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ NUnRZZNERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-AURKA(T288) / p-EIF4E(S209) / c-Myc phospho-Aurora A / Aurora B H3S10P / H3K27me2 / H3K27me3 / H3K9me2 / H3AcK / H4K16Ac 28073841 22863010 29477140
Growth inhibition assay Cell viability 25632225
Immunofluorescence acetylated α-tubulin / γ-tubulin E-cadherin / β-catenin / vimentin / p-SMAD5 Centrin-2 / tubulin phospho-Aurora A(T288) 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]
  • 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]
  • 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。
动物实验:[2]
  • Animal Models: 皮下接种 MM1.S 细胞的SCID鼠
  • Dosages: ~30 mg/kg/day
  • Administration: 口服处理

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04479306 Active not 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 Completed 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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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.

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