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
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客户使用Selleck生产的Alisertib (MLN8237)发表文献224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 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnFbI1IOC53IN88US=> NYS1WVNQPzJiaB?= M1\xR2ROW09? MYTJR|UxRTBwMESg{txO MkXRNlYyOzZ4OES=
LS174T NXrRSJo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\Me|ExNjVizszN NWjEOW1zPzJiaB?= NIHxSGxFVVOR NH:xb4tKSzVyPUCuNFUh|ryP NHPZeVAzPjF|Nk[4OC=>
T84 NH\xdItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqwMlUh|ryP NFjLWnA4OiCq MlLmSG1UVw>? MlrNTWM2OD1yLkC5JO69VQ>? MV6yOlE{PjZ6NB?=
LS180 M1HsTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13U[lAvPSEQvF2= MVi3NkBp NW\0V|JNTE2VTx?= NFPIcpNKSzVyPUGg{txO NXXOXpBKOjZzM{[2PFQ>
SW948 NH30dmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rBTlAvPSEQvF2= MXW3NkBp Mn\rSG1UVw>? NYP1PJpnUUN3ME2xJO69VQ>? NXn5Rno4OjZzM{[2PFQ>
HCT15 NYq5Z|lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHp[I8xNjVizszN NX3FU2c1PzJiaB?= NGXTVnZFVVOR MVXJR|UxRDBwNDFOwG0> MXiyOlE{PjZ6NB?=
DLD-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSwMlUh|ryP MVK3NkBp NI\sRZhFVVOR NV2w[XJ7UUN3MEywMlgh|ryP NVy5[|VuOjZzM{[2PFQ>
MIP-101 M3\0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C5W|AvPSEQvF2= Ml7lO|IhcA>? NEnKRoJFVVOR NYHUeHBoUUN3ME2xJO69VQ>? M1PSelI3OTN4Nki0
SNU1544 NFTuU|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKwMlUh|ryP Mn3rO|IhcA>? M{XrV2ROW09? M1z1ZWlEPTB;MTFOwG0> MVWyOlE{PjZ6NB?=
OCI-Ly10 NYrsTo5bS3m2b4TvfIlkKEG|c3H5 MofWO|IhcA>? M2noOGROW09? MWDJR|UxRTBwMEW4JO69VQ>? MXGyOVg4QDN|MR?=
SU-DHL2 M1\KbGN6fG:2b4jpZ{BCe3OjeR?= NIHSblc4OiCq MW\EUXNQ MmrDTWM2OD1yLkCxJO69VQ>? M3nsd|I2QDd6M{Ox
OCI-LY7 NH7PVIxEgXSxdH;4bYMhSXO|YYm= M{nPUVczKGh? NE\JSXlFVVOR NFLjUGpKSzVyPUCuNFgyKM7:TR?= MX[yOVg4QDN|MR?=
SU-DHL6 MXnDfZRwfG:6aXOgRZN{[Xl? NFqy[Yg4OiCq MVHEUXNQ NXztcpN7UUN3ME2wMlQ5OiEQvF2= M4HMS|I2QDd6M{Ox
Jeko-1 NWXZOFJoS3m2b4TvfIlkKEG|c3H5 NYfVRnlMPzJiaB?= M2XtXmROW09? MkDwTWM2OD1yLkCyPUDPxE1? NUPsT4ozOjV6N{izN|E>
JVM-2 Mn:3R5l1d3SxeHnjJGF{e2G7 NVThTXdZPzJiaB?= M36wfGROW09? M4e5bWlEPTB;MD6wNUDPxE1? MWSyOVg4QDN|MR?=
Rec-1 NVrFPFZES3m2b4TvfIlkKEG|c3H5 NWniSXJsPzJiaB?= NXLqRoU5TE2VTx?= NEfLdZlKSzVyPUCuNFg4KM7:TR?= NF\WeXMzPTh5OEOzNS=>
Z-138 MkjxR5l1d3SxeHnjJGF{e2G7 NHvNOWQ4OiCq NX3Se5ZbTE2VTx?= MkKyTWM2OD1yLkCxN{DPxE1? M4DXXlI2QDd6M{Ox
H9 NVjIW|hRS3m2b4TvfIlkKEG|c3H5 NEfLXXo4OiCq MofYSG1UVw>? NELYW3ZKSzVyPUCuOkDPxE1? MkXqNlU5Pzh|M{G=
HH NIjLcY5EgXSxdH;4bYMhSXO|YYm= MUW3NkBp M3zvcGROW09? MYTJR|UxRTBwNzFOwG0> NHzn[ZQzPTh5OEOzNS=>
DND41 NVS0RYJvS3m2b4TvfIlkKEG|c3H5 MYe3NkBp MXHEUXNQ NFH0dFNKSzVyPUCuNUDPxE1? MXSyOVg4QDN|MR?=
CCL119 MULDfZRwfG:6aXOgRZN{[Xl? MX:3NkBp MUfEUXNQ M2PlT2lEPTB;MD6wOlIh|ryP M1XSdlI2QDd6M{Ox
J.Cam 1.6 NX65V2w1S3m2b4TvfIlkKEG|c3H5 NXLjbJU3PzJiaB?= NGnkd4ZFVVOR M3HJVWlEPTB;MD6xNFUh|ryP NIPiOlIzPTh5OEOzNS=>
Sup-T1 MmHiR5l1d3SxeHnjJGF{e2G7 NWLzNmV5PzJiaB?= NITzTodFVVOR NWGzWnhZUUN3ME2yMlE1OiEQvF2= NHT0UGkzPTh5OEOzNS=>
Tib 152 MX\DfZRwfG:6aXOgRZN{[Xl? Mo\XO|IhcA>? NXX1eHR2TE2VTx?= MnTPTWM2OD1yLkig{txO M1O0T|I2QDd6M{Ox
MCF7 NUPZZmZFTnWwY4Tpc44hSXO|YYm= NY\GTY1OPSEQvF2= MoPVNlQhcA>? MXfEUXNQ MVvJcoR2[2W|IFeyM20h[XK{ZYP0 MkH2NlU5OzR2MEG=
MDA-MB-231 NXrnOJZSTnWwY4Tpc44hSXO|YYm= M1TTbVUh|ryP NFjH[mEzPCCq MWPEUXNQ NUfU[Y5UUW6mdXPld{BIOy:PIHHydoV{fA>? MVOyOVg{PDRyMR?=
MCF7 M4\k[GZ2dmO2aX;uJGF{e2G7 MmL1OUDPxE1? NIS5OY0zPCCq M3vCRmROW09? NH\kbFZF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy NEjtPGszPTh|NESwNS=>
MCF7 M3q2NWZ2dmO2aX;uJGF{e2G7 NXfY[IpuPSEQvF2= MVKyOEBp NFzQOoFFVVOR MUjE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNi=> M4X3TlI2QDN2NECx
MCF7 NYDVcpNWTnWwY4Tpc44hSXO|YYm= M4m1W|Uh|ryP NUPte5o4OjRiaB?= M3v3SWROW09? NGjwUnFF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx NXvicVVUOjV6M{S0NFE>
MCF7 NGXmTGVHfW6ldHnvckBCe3OjeR?= Ml;WOUDPxE1? M33EeVI1KGh? MW\EUXNQ NEHzXmFKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFIyKFejZkGvR4lxOQ>? MmG5NlU5OzR2MEG=
MCF7 MVPGeY5kfGmxbjDBd5NigQ>? NFWwfoQ2KM7:TR?= MXuyOEBp NUHucnRtTE2VTx?= M2G3NGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= NEi5UG0zPTh|NESwNS=>
MDA-MB-231 NXrCV2FKTnWwY4Tpc44hSXO|YYm= NF7zWVA2KM7:TR?= NIqxUHUzPCCq NVjOboFITE2VTx?= M4\zSWRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsyN0OGQ{K= MX6yOVg{PDRyMR?=
MDA-MB-231 MlfQSpVv[3Srb36gRZN{[Xl? NUfqToRbOSEQvF2= NXPtOGxJOjRiaB?= M2Hr[WROW09? NIXibotKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? MYKyOVg{PDRyMR?=
MDA-MB-231 Mkf2SpVv[3Srb36gRZN{[Xl? NXjoO4NpPSEQvF2= M4fpPVI1KGh? NIL0eHdFVVOR NGLMXIRF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx M2HUTFI2QDN2NECx
MDA-MB-231 Ml3uSpVv[3Srb36gRZN{[Xl? NFnpeWI2KM7:TR?= MXqyOEBp NHn6cnlFVVOR MVrJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> M17nNVI2QDN2NECx
MDA-MB-231 MmjySpVv[3Srb36gRZN{[Xl? M{ToSlUh|ryP MknaNlQhcA>? MULEUXNQ MofWTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz NXzpWlJXOjV6M{S0NFE>
MDA-MB-231 MnXrSpVv[3Srb36gRZN{[Xl? MmXROUDPxE1? MWmyOEBp NE\FZ5ZFVVOR NWL6bHB7UW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJA2Ow>? M4\SWVI2QDN2NECx
MCF7 Mlv3RZBweHSxc3nzJGF{e2G7 Mn;MOUDPxE1? NGPjZmQzPCCq M3zVUmROW09? MlfVTY5lfWOnczDhdI9xfG:2aXOg[IVifGh? MXGyOVg{PDRyMR?=
MDA-MB-231 NYi1fXg5SXCxcITvd4l{KEG|c3H5 MkTCOUDPxE1? MlHmNlQhcA>? NIHVdHZFVVOR NVzF[ZFkUW6mdXPld{BieG:ydH;0bYMh\GWjdHi= NX;pSXppOjV6M{S0NFE>
MCF7 NInqe29HfW6ldHnvckBCe3OjeR?= MnnNNUDPxE1? M2TsUFczKGh? NFPvN4tFVVOR NIPWNIJKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= MoC3NlU5OzR2MEG=
MDA-MB-231 NGnkSnVHfW6ldHnvckBCe3OjeR?= M{H6bVEh|ryP MVy3NkBp MYnEUXNQ NXzsZ3dXUW6mdXPld{BifXSxcHjh[4lkKGSnYYTo MXmyOVg{PDRyMR?=
U-2 OS MoP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\EUZU2OCEQvF2= M2L5clI1KGh? NGHidIVFVVOR MlvjTWM2OD1zNj62JO69VQ>? NELuVWkzPTd7MkixNS=>
MG-63 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnZXm9tPTBizszN Mo\1NlQhcA>? NXOydWozTE2VTx?= MmrvTWM2OD17LkWg{txO MojXNlU4QTJ6MUG=
U-2 OS NEnBOXhCeG:ydH;zbZMhSXO|YYm= NXvsUWo4PSEQvF2= M1PwWVI1KGh? NV32THpETE2VTx?= MYrJcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo Ml76NlU4QTJ6MUG=
MG-63 MnK2RZBweHSxc3nzJGF{e2G7 MVW1JO69VQ>? MkW2NlQhcA>? MWTEUXNQ MWDJcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo M4XhdVI2Pzl{OEGx
U-2 OS MVTGeY5kfGmxbjDBd5NigQ>? MUC1JO69VQ>? MWCyOEBp NIPveYpFVVOR MX7Qdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> MYeyOVc6OjhzMR?=
MG-63 NHPpOGFHfW6ldHnvckBCe3OjeR?= NUnENlZLPSEQvF2= M4fpcVI1KGh? Mn;YSG1UVw>? MkntVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MXyyOVc6OjhzMR?=
PANC-1 MnnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEiySmE2OCEQvF2= NXX3W2xLOjRiaB?= MlvKSG1UVw>? NGLGe2lKSzVyPUeuNUDPxE1? NX3TeG5IOjV4M{KyNlU>
BxPC-3 NHjDT5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\I[5Q2OCEQvF2= NGLCc3AzPCCq NEG5[VhFVVOR Mo\rTWM2OD14Lkig{txO M4nPN|I2PjN{MkK1
PANC-1 MU\GeY5kfGmxbjDBd5NigQ>? NFPHV2I2KM7:TR?= Ml7YNlQhcA>? NHfmPGRFVVOR NEnhUWJKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? M4T0RlI2PjN{MkK1
BxPC-3 MmqwSpVv[3Srb36gRZN{[Xl? Ml23OUDPxE1? MYWyOEBp MULEUXNQ NHHBZnJKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? MVyyOVY{OjJ{NR?=
PANC-1 NWn4UpRCTnWwY4Tpc44hSXO|YYm= MkHBOUDPxE1? NGXCRlAzPCCq MVPEUXNQ M2HS[mlv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp MkDtNlU3OzJ{MkW=
BxPC-3 M1LKTWZ2dmO2aX;uJGF{e2G7 NEXqWYE2KM7:TR?= NH;PdYczPCCq NIrpW5hFVVOR NY\QV2hnUW6mdXPld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? M4jwbVI2PjN{MkK1
SKOV3 MmTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITEeZgyODBizszN NE\T[YUzPCCq NGrJeIxFVVOR MVzJR|UxRTJyLkS4JO69VQ>? NEPCW5AzPTZ{NEe1NC=>
OVCAR4 NGC5W2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:4NVAxKM7:TR?= MnzXNlQhcA>? MVLEUXNQ M13pR2lEPTB;MkKuNVMh|ryP MX2yOVYzPDd3MB?=
SKOV3 M4GwfmZ2dmO2aX;uJGF{e2G7 MlviOUDPxE1? NUDXWmpmPzJiaB?= M4\vTmROW09? M1Ky[2lv\HWlZYOgS|IwVSCjcoLld5Q> NGPRXoozPTZ{NEe1NC=>
OVCAR4 NUW1cXduTnWwY4Tpc44hSXO|YYm= NHHKOlU2KM7:TR?= MlLwO|IhcA>? MXfEUXNQ M2DXc2lv\HWlZYOgS|IwVSCjcoLld5Q> Mkf0NlU3OjR5NUC=
SKOV3 NV\MRmhsSXCxcITvd4l{KEG|c3H5 NWHjVpJzPSEQvF2= M2PydlI1KGh? M4jTeWROW09? MlHjTY5lfWOnczDhdI9xfG:|aYO= NHvx[WgzPTZ{NEe1NC=>
OVCAR4 M4XFdWFxd3C2b4Ppd{BCe3OjeR?= M2TVUVUh|ryP MUOyOEBp NYL3cnJkTE2VTx?= NEKzVYxKdmS3Y3XzJIFxd3C2b4Ppdy=> MkD2NlU3OjR5NUC=
AGS NXu5SohMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LqT|I2KM7:TR?= MXqyOEBp Mn7MSG1UVw>? NYj0TI9iUUN3ME2xPU4xQSEQvF2= MVSyOVYxQTl{Mx?=
NCI-N78 MlTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;HNlUh|ryP MXuyOEBp MWXEUXNQ MWHJR|UxRTJ4LkOzJO69VQ>? MlzVNlU3ODl7MkO=
AGS NVLyWnFRSXCxcITvd4l{KEG|c3H5 MoXlOUDPxE1? M{LUXVI1KGh? Ml\JSG1UVw>? MYjJcoR2[2W|IHHwc5B1d3Orcx?= M2jYelI2PjB7OUKz
NCI-N78 NY\SbJBPSXCxcITvd4l{KEG|c3H5 NFHrW4g2KM7:TR?= NGPxNGczPCCq MmewSG1UVw>? NFq3eFVKdmS3Y3XzJIFxd3C2b4Ppdy=> M{\V[FI2PjB7OUKz
AGS MmfTSpVv[3Srb36gRZN{[Xl? M4H1dFUh|ryP MUOyOEBp NEfkbm5FVVOR M3LpVmlv\HWlZYOgeIhmKGG3dH;wbIFogQ>? MUSyOVYxQTl{Mx?=
NCI-N78 MX7GeY5kfGmxbjDBd5NigQ>? MYC1JO69VQ>? MoX4NlQhcA>? MXzEUXNQ MmjGTY5lfWOnczD0bIUh[XW2b4DoZYd6 MWWyOVYxQTl{Mx?=
HSC-3 MoHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWH4cJhCOSEQvF2= NI\mbpk1QCCq NF[2NHVKSzVyPUCuOVQh|ryP NVy1VWNxOjV|Nk[xOFM>
GB30 MnXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf4OYgyKM7:TR?= M{HOZlch\A>? Mme3SG1UVw>? NYTTcmpWUUN3ME2wMlAyOSEQvF2= NVvzeYNQOjVzME[0Nlg>
GB9 NVK1[Xd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXSxJO69VQ>? NGKyUGY4KGR? M1jGbGROW09? MmnETWM2OD1yLkCyOEDPxE1? MUWyOVExPjR{OB?=
GB169 M17sPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHZPZcyKM7:TR?= MofGO{Bl NYXVe4tjTE2VTx?= NFu0U2JKSzVyPUCuNFMzKM7:TR?= NGnEOZczPTFyNkSyPC=>
T24 NFTJNWxHfW6ldHnvckBCe3OjeR?= MlO0NUDPxE1? MUK0PEBp M2jLNGROW09? M3Hz[mlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M4fyeVI{PDB|NkOz
RT4 MkD1SpVv[3Srb36gRZN{[Xl? MoLTNUDPxE1? MXS0PEBp NF;udlNFVVOR NEnTPG9KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NHnqV5MzOzRyM{[zNy=>
UM-UC-3 NWnwVXFlTnWwY4Tpc44hSXO|YYm= NFLie3YyKM7:TR?= NV;yPIZxPDhiaB?= NVjidWc2TE2VTx?= NVjJ[29nUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NGf3bpkzOzRyM{[zNy=>
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CHLA-266 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTveZBlOTBizszN NYrzc41RQTZiaB?= MVvJR|UxRTBwMEeyJO69VQ>? M4nzXFIxOTB6M{O4
TC-71 NXHHfY9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HTRlExKM7:TR?= MoT0PVYhcA>? M1TPZWlEPTB;MD6xNFIh|ryP MVeyNFExQDN|OB?=
SJ-GBM2 NV6zV4lRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHKzSocyOCEQvF2= M2\vSlk3KGh? NVHZcHVbUUN3ME2wMlA2OCEQvF2= NFrycZgzODFyOEOzPC=>
NALM-6 M1TXbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGOzRoEyOCEQvF2= NInQeJk6PiCq NH74b|dKSzVyPUCuNFYzKM7:TR?= M{jENlIxOTB6M{O4
COG-LL-317 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDZR3dzOTBizszN NFviSYw6PiCq M4Kxe2lEPTB;MD6wOFch|ryP Mom1NlAyODh|M{i=
RS4-11 M3HPXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHmNVAh|ryP M2P5Tlk3KGh? MknITWM2OD1yLkCxPEDPxE1? NXnjcIZHOjBzMEizN|g>
MOLT-4 MkLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vRO|ExKM7:TR?= MVK5OkBp NFm5V|lKSzVyPUCuNFI3KM7:TR?= NVvMOHp4OjBzMEizN|g>
CCRF-CEM MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTMNVAh|ryP NV;oWlZ4QTZiaB?= M3jkXmlEPTB;MD6wPVQh|ryP M3XCTFIxOTB6M{O4
Kasumi-1 M1zuNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\IdHVzOTBizszN M33YVFk3KGh? NXLJboJ7UUN3ME2wMlExOyEQvF2= M4C3[VIxOTB6M{O4
Karpas-299 M1G2TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TSW|ExKM7:TR?= Mn;5PVYhcA>? NU\UZmxQUUN3ME2wMlA{QCEQvF2= NGLYe3ozODFyOEOzPC=>
Ramos-RA1 NUHETWtCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnJWo8yOCEQvF2= MYG5OkBp MYrJR|UxRTBwMUK3JO69VQ>? NY\vS2JEOjBzMEizN|g>

... 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
8mg/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、MSDS / 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、MSDS / 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 EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma|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|National Cancer Institute (NCI) 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 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