Alisertib (MLN8237)

For research use only. Not for use in humans.

目录号：S1133 中文名称：阿利色替

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
5mg	RMB 983.87	现货
10mg	RMB 1725.78	现货
50mg	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：

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BMC Res Notes, 2015, 8:484

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Cell Death Dis, 2014, 5:e1177

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Cell Death Dis, 2014, 6:e1595

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Endocr Relat Cancer, 2014, 21(5):797-811

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Cell Cycle, 2014, 13(14):2248-61

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Chembiochem, 2014, 15(3):443-50

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PLoS One, 2014, 9(12):e113989

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PLoS One, 2014,

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Nat Commun, 2013, 4:2656

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Leukemia, 2013, 27(3):560-8

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J Cell Sci, 2013, 126(Pt 9):2102-13

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Epigenetics Chromatin, 2013, 6(1):21

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Cancer Biol Ther, 2013, 14(5):436-49

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Oncotarget, 2013,

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Breast Cancer Res Tr, 2012, 135(2):433-44

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Cell Cycle, 2012, 11(2):296-309

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Cell Cycle, 2012, 11(13):2567-77

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Oncotarget, 2011,

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J Cell Biol, 2010, 191(7):1315-32

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EMBO Rep, 2010, 11(12):977-84

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ACS Chem Biol, 2010, 5(6):563-76

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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

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=>
T24	NG\PfHFCeG:ydH;zbZMhSXO\|YYm=	NWPvWZBjOy5zNjFOwG0>	MWO5OkBp	NVnkeJhSTE2VTx?=	MlToTWM2OD1yLkCzNFYh\|ryP	M3Pm[VI{PDB\|NkOz
RT4	NGO4S3FCeG:ydH;zbZMhSXO\|YYm=	NYfGWGc2Oy5zNjFOwG0>	MWC5OkBp	MUDEUXNQ	MlnyTWM2OD1yLkGxPVgh\|ryP	MoPCNlM1ODN4M{O=
UM-UC-3	NHLzbXBCeG:ydH;zbZMhSXO\|YYm=	NW\PRmFtOy5zNjFOwG0>	MUG5OkBp	M2SwfGROW09?	NUHOXYY6UUN3ME2wMlA1PDlizszN	NHLTdWwzOzRyM{[zNy=>
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RD	NVfYeWw{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4nNRlExKM7:TR?=	Mn;DPVYhcA>?		NIPOUYZKSzVyPUCuNlI5KM7:TR?=	MYOyNFExQDN\|OB?=
Rh41	MmDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYexNEDPxE1?	NIryXXE6PiCq		NU\ofW9NUUN3ME2wMlA6OCEQvF2=	M4DEd\|IxOTB6M{O4
Rh30	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFnNOnkyOCEQvF2=	M3vkblk3KGh?		NGT5eGdKSzVyPUCuNlMxKM7:TR?=	NIXxUpYzODFyOEOzPC=>
BT-12	M{\sSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NW\iU2lKOTBizszN	NGTxRpU6PiCq		MXfJR\|UxRTBwME[wJO69VQ>?	NIj4VWszODFyOEOzPC=>
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 Clin Cancer Res 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 Cell 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 Mol Cells 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 Drug Des Devel Ther 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 FASEB J 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 Oncogene 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 Oncotarget 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 Blood 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]

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-20^oC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)

参考文献

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 Download Alisertib (MLN8237) SDF

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
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

每只动物给药体积

动物数量

只

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，注：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：取 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。

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。

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2020-09-01)

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

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

泛Aurora Kinase抑制剂

Danusertib (PHA-739358) : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=13 nM/79 nM/61 nM.
泛Aurora Kinase抑制剂

SNS-314 Mesylate : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=9 nM/31 nM/3 nM.
活性最高的Aurora Kinase抑制剂

MK-5108 (VX-689) : Aurora A, IC50=0.064 nM.
用于临床的Aurora Kinase抑制剂

VX-680 (Tozasertib, MK-0457) : Phase II for Advanced Non-Small Cell Lung Cancer (NSCLC).
经典的Aurora Kinase抑制剂

Hesperadin : Potently inhibits Aurora B with IC50 of 250 nM.

研究领域

产品类型

定制您的化合物库

Alisertib (MLN8237)

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

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)

参考文献

溶解度 (25°C)

化学数据 Download Alisertib (MLN8237) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2020-09-01)

技术支持

常见问题及建议解决方法

Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

相关Aurora Kinase产品