Alisertib (MLN8237)

For research use only. Not for use in humans.

目录号：S1133

Molecular Weight(MW): 518.92

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。Phase 3。

规格

价格

库存

购买数量

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199篇：

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Sci Rep, 2018, 8(1):14017

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Sci Transl Med, 2017, 9(372)

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FASEB J, 2017, 32(2):625-638

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Sci Rep, 2017, 7:45514

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Sci Rep, 2017, 7(1):17978

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Sci Rep, 2017, 7:45514

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Oncotarget, 2017, 8(68):112313-112329

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Pharmaceuticals (Basel), 2017, 10(3)

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Oncotarget, 2017, 8(31):50376-50392

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Oncotarget, 2017, 8(34):57047-57057

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Nat Commun, 2016, 7:10180

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ACS Chem Biol, 2016, 11(12):3400-3411

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Sci Rep, 2016, 6:19567

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Cancer Biol Ther, 2016, 17(5):566-76

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Cell Cycle, 2016, 15(3):413-24

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Biol Bull, 2016, 231(1):61-72

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Nat Cell Biol, 2015, 17(2):113-22

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Nat Cell Biol, 2015, 17(2):113-22

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Nat Commun, 2015, 6:8388

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Mol Cancer, 2015, 14(1):83

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J Cell Sci, 2015, 128(3):527-40

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Int J Mol Sci, 2015, 17(1)

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Breast Cancer Res Tr, 2015, 149(3):715-26

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Cell Cycle, 2015, 14(24):3908-19

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Drug Des Devel Ther, 2015, 9:575-601

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BMC Res Notes, 2015, 8:484

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Genes Cancer, 2015, 6(5-6):184-213

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Oncotarget, 2015, 6(34):35247-62

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Clin Cancer Res, 2014, 34(5):2269-74

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Oncogene, 2014, 33(42):4985-96

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Oncogene, 2014, 33(27):3550-60

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Cell Death Dis, 2014, 5:e1253

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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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Mol Oncol, 2014, 8(8):1419-28

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Mol Cancer Res, 2014, 12(3):433-9

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J Transl Med, 2014, 12(1):200

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

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FEBS Lett, 2014, 588(14):2198-205

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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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Biochem Biophys Res Commun, 2014, 452(3):845-51

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Neurosci Lett, 2014, 583:199-204

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J Pediatr Surg, 2014, 49(1):159-65

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Oncotarget, 2014, 5(12):4071-86

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Nat Commun, 2013, 4:2656

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Cancer Res, 2013, 73(20):6310-22

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EMBO Rep, 2013, 14(9):829-36

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Oral Oncol, 2013, 49(6):551-9

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ACS Chem Biol, 2013, 8(7):1451-9

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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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PLoS One, 2012, 7(2):e30734

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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

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。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	NWCxXnVVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXWwMlUh\|ryP	M1nC[lczKGh?	MoDmSG1UVw>?	M4S0VmlEPTB;MD6wOEDPxE1?	NIHVcJczPjF\|Nk[4OC=>
LS174T	NEH6fWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NX3IblBqOC53IN88US=>	M4TEblczKGh?	NH62S5ZFVVOR	Ml\STWM2OD1yLkC1JO69VQ>?	NVzqd4hCOjZzM{[2PFQ>
T84	NWDicHVlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml35NE42KM7:TR?=	NWD4cXl5PzJiaB?=	NGnFU21FVVOR	MnHuTWM2OD1yLkC5JO69VQ>?	M1PR[lI3OTN4Nki0
LS180	MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NV3UZnZCOC53IN88US=>	MlH4O\|IhcA>?	MkPGSG1UVw>?	Ml;WTWM2OD1zIN88US=>	MnXvNlYyOzZ4OES=
SW948	M1LhPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF;ofIMxNjVizszN	NX3rSXJtPzJiaB?=	NYfaUFlXTE2VTx?=	M2rlSWlEPTB;MTFOwG0>	MXmyOlE{PjZ6NB?=
HCT15	NXHEcYpET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NH64Z4IxNjVizszN	MVO3NkBp	NULJZo5GTE2VTx?=	MXTJR\|UxRDBwNDFOwG0>	NW\HdVY1OjZzM{[2PFQ>
DLD-1	NVTKdWhpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mk[1NE42KM7:TR?=	NXj3NZJsPzJiaB?=	NInnUWdFVVOR	M1PkRWlEPTB:MD64JO69VQ>?	MkTHNlYyOzZ4OES=
MIP-101	M3PXRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1Kwd\|AvPSEQvF2=	MYW3NkBp	M4[0dGROW09?	NHjofoVKSzVyPUGg{txO	MljXNlYyOzZ4OES=
SNU1544	NF76dVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml\PNE42KM7:TR?=	M4jTdFczKGh?	M{fCPWROW09?	NInPe25KSzVyPUGg{txO	NF7TcXQzPjF\|Nk[4OC=>
OCI-Ly10	MXvDfZRwfG:6aXOgRZN{[Xl?		NULi[JNxPzJiaB?=	NYniNXhGTE2VTx?=	M2fDfmlEPTB;MD6wOVgh\|ryP	MUmyOVg4QDN\|MR?=
SU-DHL2	MUXDfZRwfG:6aXOgRZN{[Xl?		NGP4ZVE4OiCq	NVPqPJZGTE2VTx?=	MV;JR\|UxRTBwMEGg{txO	MUOyOVg4QDN\|MR?=
OCI-LY7	MnXxR5l1d3SxeHnjJGF{e2G7		MYW3NkBp	NFTnbndFVVOR	MVfJR\|UxRTBwMEixJO69VQ>?	MnXPNlU5Pzh\|M{G=
SU-DHL6	M1TV[GN6fG:2b4jpZ{BCe3OjeR?=		NYH4[nViPzJiaB?=	MlS3SG1UVw>?	M4jKS2lEPTB;MD60PFIh\|ryP	NYnlTHRZOjV6N{izN\|E>
Jeko-1	MXnDfZRwfG:6aXOgRZN{[Xl?		MmLuO\|IhcA>?	MVzEUXNQ	MV3JR\|UxRTBwMEK5JO69VQ>?	NILONYszPTh5OEOzNS=>
JVM-2	NFTzU2dEgXSxdH;4bYMhSXO\|YYm=		NYXqdow{PzJiaB?=	M120fGROW09?	MWHJR\|UxRTBwMEGg{txO	MonkNlU5Pzh\|M{G=
Rec-1	MlzrR5l1d3SxeHnjJGF{e2G7		M4TuOlczKGh?	MVnEUXNQ	NYXqbXhkUUN3ME2wMlA5PyEQvF2=	MVyyOVg4QDN\|MR?=
Z-138	MXzDfZRwfG:6aXOgRZN{[Xl?		MVe3NkBp	MkTySG1UVw>?	NVnCRnBTUUN3ME2wMlAyOyEQvF2=	MoixNlU5Pzh\|M{G=
H9	MXLDfZRwfG:6aXOgRZN{[Xl?		MoLPO\|IhcA>?	M1TuXGROW09?	MVzJR\|UxRTBwNjFOwG0>	NED4S2IzPTh5OEOzNS=>
HH	NF\mUVlEgXSxdH;4bYMhSXO\|YYm=		NUPBPZFQPzJiaB?=	NWPZSGVKTE2VTx?=	M3izU2lEPTB;MD63JO69VQ>?	M1LjSlI2QDd6M{Ox
DND41	NV7hNnVDS3m2b4TvfIlkKEG\|c3H5		M2\HUFczKGh?	NEjsRY1FVVOR	NF:1c2hKSzVyPUCuNUDPxE1?	MXyyOVg4QDN\|MR?=
CCL119	NHPjZ\|JEgXSxdH;4bYMhSXO\|YYm=		NFrBeXA4OiCq	NXvhWW9QTE2VTx?=	NXW4NIVlUUN3ME2wMlA3OiEQvF2=	NWPKWmtROjV6N{izN\|E>
J.Cam 1.6	Mn;ER5l1d3SxeHnjJGF{e2G7		M3P2flczKGh?	NWTJXJZWTE2VTx?=	MX7JR\|UxRTBwMUC1JO69VQ>?	Mlj0NlU5Pzh\|M{G=
Sup-T1	MVnDfZRwfG:6aXOgRZN{[Xl?		M1Tob\|czKGh?	M3u3cGROW09?	MXnJR\|UxRTJwMUSyJO69VQ>?	MX2yOVg4QDN\|MR?=
Tib 152	MkX6R5l1d3SxeHnjJGF{e2G7		NHfUT5A4OiCq	MW\EUXNQ	NWLiPIt6UUN3ME2wMlgh\|ryP	M2fCd\|I2QDd6M{Ox
MCF7	MnfNSpVv[3Srb36gRZN{[Xl?	M4GybVUh\|ryP	M4LaV\|I1KGh?	MVPEUXNQ	MljRTY5lfWOnczDHNk9OKGG{cnXzeC=>	MkPqNlU5OzR2MEG=
MDA-MB-231	MlO2SpVv[3Srb36gRZN{[Xl?	MV[1JO69VQ>?	NGnheYszPCCq	M3nKTWROW09?	NX:2R5BLUW6mdXPld{BIOy:PIHHydoV{fA>?	M{\CVlI2QDN2NECx
MCF7	NXXmcox7TnWwY4Tpc44hSXO\|YYm=	M{jZd\|Uh\|ryP	NHnQOogzPCCq	M3fmSmROW09?	MXLE[YNz\WG\|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{	NIrkZo0zPTh\|NESwNS=>
MCF7	NHjDbY5HfW6ldHnvckBCe3OjeR?=	M3jtPVUh\|ryP	NXTsS3JoOjRiaB?=	MlXiSG1UVw>?	NVjkeGlZTGWlcnXhd4V{KHSqZTDlfJBz\XO\|aX;uJIxmfmWuIH;mJGNFUzJ?	NVrVZWtDOjV6M{S0NFE>
MCF7	MlX0SpVv[3Srb36gRZN{[Xl?	MUK1JO69VQ>?	MWqyOEBp	NG\5eVFFVVOR	NI\3WnNF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx	M1K3eVI2QDN2NECx
MCF7	M17TSGZ2dmO2aX;uJGF{e2G7	M2W4SlUh\|ryP	MoTlNlQhcA>?	NY[yRVNKTE2VTx?=	M33S[Wlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlEhX2GoMT;DbZAy	NWHuc24xOjV6M{S0NFE>
MCF7	NY\pXoNDTnWwY4Tpc44hSXO\|YYm=	NYLtS\|lGPSEQvF2=	MXOyOEBp	MXXEUXNQ	NEjGblhKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG=	NGP2NW0zPTh\|NESwNS=>
MDA-MB-231	MW\GeY5kfGmxbjDBd5NigQ>?	MWK1JO69VQ>?	NXPDWWRWOjRiaB?=	NVe4[o5qTE2VTx?=	MnzUSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET\|EwS0SFMh?=	NHj0bpozPTh\|NESwNS=>
MDA-MB-231	NFf2XYlHfW6ldHnvckBCe3OjeR?=	NV\oOmt[OSEQvF2=	MX:yOEBp	NE\iRXlFVVOR	M2nFOGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz	NXzYUZpmOjV6M{S0NFE>
MDA-MB-231	NXPEdlJITnWwY4Tpc44hSXO\|YYm=	NVzKOXhHPSEQvF2=	M37KblI1KGh?	M2m3bGROW09?	NV3PO4lPTGWlcnXhd4V{KHSqZTDlfJBz\XO\|aX;uJIxmfmWuIH;mJIN6[2yrbjDCNS=>	Mn3nNlU5OzR2MEG=
MDA-MB-231	NX7DRolQTnWwY4Tpc44hSXO\|YYm=	MmrKOUDPxE1?	MYqyOEBp	MlXWSG1UVw>?	MWTJcoNz\WG\|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=>	M17SUlI2QDN2NECx
MDA-MB-231	M3jne2Z2dmO2aX;uJGF{e2G7	MVW1JO69VQ>?	NHj3UW4zPCCq	M{D6UmROW09?	M4DVeWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?=	M{\RflI2QDN2NECx
MDA-MB-231	NITrSFVHfW6ldHnvckBCe3OjeR?=	Ml3COUDPxE1?	NV65cZhUOjRiaB?=	NWHOUJBiTE2VTx?=	MWjJcoNz\WG\|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEWz	MnrjNlU5OzR2MEG=
MCF7	MYPBdI9xfG:\|aYOgRZN{[Xl?	NYPkNpoxPSEQvF2=	M2fUcVI1KGh?	MWXEUXNQ	MoPhTY5lfWOnczDhdI9xfG:2aXOg[IVifGh?	MYqyOVg{PDRyMR?=
MDA-MB-231	M2LFe2Fxd3C2b4Ppd{BCe3OjeR?=	MYS1JO69VQ>?	MmfQNlQhcA>?	M1P0UGROW09?	NGjVbnlKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?=	NGPqW2szPTh\|NESwNS=>
MCF7	NUXtcpNCTnWwY4Tpc44hSXO\|YYm=	NYTvNoRzOSEQvF2=	MoHYO\|IhcA>?	NVP4dZZ7TE2VTx?=	Mn;ETY5lfWOnczDheZRweGijZ3njJIRm[XSq	M3vpTFI2QDN2NECx
MDA-MB-231	MoLISpVv[3Srb36gRZN{[Xl?	MXSxJO69VQ>?	NVrmUXVKPzJiaB?=	MlLwSG1UVw>?	MnPNTY5lfWOnczDheZRweGijZ3njJIRm[XSq	Mn7kNlU5OzR2MEG=
U-2 OS	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmryOVAh\|ryP	NYDmcph3OjRiaB?=	NX3CXo45TE2VTx?=	M1TidmlEPTB;MU[uOkDPxE1?	M4jXcVI2Pzl{OEGx
MG-63	NVvHNFlYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWm1NEDPxE1?	NY\lOpF5OjRiaB?=	MnXySG1UVw>?	NHr0bJpKSzVyPUmuOUDPxE1?	MVSyOVc6OjhzMR?=
U-2 OS	M{DHfGFxd3C2b4Ppd{BCe3OjeR?=	MVi1JO69VQ>?	M3\sdVI1KGh?	NUXvSot7TE2VTx?=	NV;rdVcxUW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>?	MmnKNlU4QTJ6MUG=
MG-63	MW\BdI9xfG:\|aYOgRZN{[Xl?	MmD3OUDPxE1?	NHvjTpYzPCCq	MVHEUXNQ	MlzxTY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=>	Ml;1NlU4QTJ6MUG=
U-2 OS	MlXTSpVv[3Srb36gRZN{[Xl?	MmnmOUDPxE1?	NHfTNVEzPCCq	MX7EUXNQ	M3rOc3Bzd22xdHXzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>?	M1XEUFI2Pzl{OEGx
MG-63	NXTmS3g1TnWwY4Tpc44hSXO\|YYm=	NW[0N5VsPSEQvF2=	M2T1fVI1KGh?	NFyxcFFFVVOR	MWLQdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg>	NGO5NmgzPTd7MkixNS=>
PANC-1	Mn;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3vxSFUxKM7:TR?=	NGflfXEzPCCq	NXjHeHdrTE2VTx?=	MYjJR\|UxRTdwMTFOwG0>	M1G3U\|I2PjN{MkK1
BxPC-3	NH\teWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4OyRVUxKM7:TR?=	MUKyOEBp	NVTrTnRFTE2VTx?=	NXPXUGFjUUN3ME22Mlgh\|ryP	MkDtNlU3OzJ{MkW=
PANC-1	M3rq[GZ2dmO2aX;uJGF{e2G7	NFr0Z4U2KM7:TR?=	NFzGTFkzPCCq	Mon4SG1UVw>?	Ml\MTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW\|dDDpckBIOi:PIIDoZZNm	NEL4W2EzPTZ\|MkKyOS=>
BxPC-3	NHPuNnVHfW6ldHnvckBCe3OjeR?=	NXq2VXk{PSEQvF2=	MVSyOEBp	MXvEUXNQ	M{XIRmlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgbY4hTzJxTTDwbIF{\Q>?	M{nz[FI2PjN{MkK1
PANC-1	M33iUmZ2dmO2aX;uJGF{e2G7	M1G3clUh\|ryP	MWKyOEBp	Mn6ySG1UVw>?	NIjJTZlKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>?	M{G5[VI2PjN{MkK1
BxPC-3	NHH1V\|FHfW6ldHnvckBCe3OjeR?=	M{HKOlUh\|ryP	MWqyOEBp	M{LpTmROW09?	Ml34TY5lfWOnczDheZRweGijZ3njJINmdGxiZHXheIg>	MkPzNlU3OzJ{MkW=
SKOV3	NEHDXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVG5[XRtOTByIN88US=>	NVLBVnhFOjRiaB?=	MnflSG1UVw>?	NYrQUXlRUUN3ME2yNE41QCEQvF2=	M{nK[VI2PjJ2N{Ww
OVCAR4	M13rbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXnK[IlnOTByIN88US=>	MVqyOEBp	MWfEUXNQ	MmW2TWM2OD1{Mj6xN{DPxE1?	NVnGUGVDOjV4MkS3OVA>
SKOV3	NIXGb41HfW6ldHnvckBCe3OjeR?=	NXrkdnl{PSEQvF2=	M4P2dFczKGh?	MXjEUXNQ	MmS4TY5lfWOnczDHNk9OKGG{cnXzeC=>	MnfoNlU3OjR5NUC=
OVCAR4	NELLXVZHfW6ldHnvckBCe3OjeR?=	MWS1JO69VQ>?	MlHqO\|IhcA>?	NEWx[5VFVVOR	M4X1WGlv\HWlZYOgS\|IwVSCjcoLld5Q>	MWWyOVYzPDd3MB?=
SKOV3	NWq5enZISXCxcITvd4l{KEG\|c3H5	MWS1JO69VQ>?	Mni5NlQhcA>?	NFq0Zo1FVVOR	M1[2Z2lv\HWlZYOgZZBweHSxc3nz	M1nn[VI2PjJ2N{Ww
OVCAR4	Mk[1RZBweHSxc3nzJGF{e2G7	NVP5dol3PSEQvF2=	M2LjXlI1KGh?	NGCyS2dFVVOR	M{DCN2lv\HWlZYOgZZBweHSxc3nz	NVjaRXNmOjV4MkS3OVA>
AGS	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4nEO\|I2KM7:TR?=	M3rDRlI1KGh?	M4HEeGROW09?	MojRTWM2OD1zOT6wPUDPxE1?	NY\mXpJqOjV4MEm5NlM>
NCI-N78	NEHqUJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MX2yOUDPxE1?	NX\0emQ3OjRiaB?=	MWrEUXNQ	M4HtbmlEPTB;Mk[uN\|Mh\|ryP	MlTKNlU3ODl7MkO=
AGS	NIrxZ29CeG:ydH;zbZMhSXO\|YYm=	MmH0OUDPxE1?	NUjHWlhFOjRiaB?=	M132W2ROW09?	M2Owdmlv\HWlZYOgZZBweHSxc3nz	MYKyOVYxQTl{Mx?=
NCI-N78	MUPBdI9xfG:\|aYOgRZN{[Xl?	NYrXbmYxPSEQvF2=	NHvSSVgzPCCq	NGrJdGVFVVOR	M3OzVmlv\HWlZYOgZZBweHSxc3nz	MoPDNlU3ODl7MkO=
AGS	MX;GeY5kfGmxbjDBd5NigQ>?	MUK1JO69VQ>?	NW\iSm8yOjRiaB?=	NFPRVVRFVVOR	M3zyb2lv\HWlZYOgeIhmKGG3dH;wbIFogQ>?	NUjHNYFoOjV4MEm5NlM>
NCI-N78	MVXGeY5kfGmxbjDBd5NigQ>?	M{fiO\|Uh\|ryP	NGLMSWkzPCCq	Ml7OSG1UVw>?	MXLJcoR2[2W\|IITo[UBifXSxcHjh[5k>	MnPRNlU3ODl7MkO=
HSC-3	NXy5OllGT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MofCNUDPxE1?	M1X2fFQ5KGh?		MV\JR\|UxRTBwNUSg{txO	NUD6cGJzOjV\|Nk[xOFM>
GB30	NGPHU4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYS1fWJ[OSEQvF2=	MVS3JIQ>	MkewSG1UVw>?	NV\ldZU2UUN3ME2wMlAyOSEQvF2=	NHLTWJkzPTFyNkSyPC=>
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GB169	MkPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnnyNUDPxE1?	MonsO{Bl	MVrEUXNQ	M3Hn[WlEPTB;MD6wN\|Ih\|ryP	NXzENodTOjVzME[0Nlg>
T24	NF7GOZNHfW6ldHnvckBCe3OjeR?=	NFWzZmwyKM7:TR?=	NE\4bXc1QCCq	MVrEUXNQ	MVzJcoR2[2W\|IHPlcIwh[3mlbHWgZZJz\XO2	MkDZNlM1ODN4M{O=
RT4	M4L1V2Z2dmO2aX;uJGF{e2G7	Ml;BNUDPxE1?	M1yyUFQ5KGh?	NWjtfZI3TE2VTx?=	MVLJcoR2[2W\|IHPlcIwh[3mlbHWgZZJz\XO2	NFvWcZAzOzRyM{[zNy=>
UM-UC-3	MnvOSpVv[3Srb36gRZN{[Xl?	MVmxJO69VQ>?	NX:2WpJUPDhiaB?=	NWPz[ol6TE2VTx?=	NH3ab5ZKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0	NHqyOWQzOzRyM{[zNy=>
T24	NVX4ZY9XSXCxcITvd4l{KEG\|c3H5	NYPi[nNkOy5zNjFOwG0>	MWW5OkBp	NVS2WGJGTE2VTx?=	M3jWdWlEPTB;MD6wN\|A3KM7:TR?=	M2PORVI{PDB\|NkOz
RT4	NIPEfIVCeG:ydH;zbZMhSXO\|YYm=	NXrxOIg5Oy5zNjFOwG0>	NEKx[Fg6PiCq	M3j6ZmROW09?	NFK2SFBKSzVyPUCuNVE6QCEQvF2=	M4rFV\|I{PDB\|NkOz
UM-UC-3	NYDJU\|VOSXCxcITvd4l{KEG\|c3H5	MWizMlE3KM7:TR?=	NIXaSlk6PiCq	NIK4WXRFVVOR	MYTJR\|UxRTBwMES0PUDPxE1?	MnTQNlM1ODN4M{O=
OVCAR-5	NV7HWHNqTnWwY4Tpc44hSXO\|YYm=	M1voNFUxKG6P			MlXSTY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25?	Mm\zNlM{OzR\|Mke=
SKOV3ip2	NI\6eGRHfW6ldHnvckBCe3OjeR?=	NV64cG5mPTBibl2=			MXjJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>?	M3HkVVI{OzN2M{K3
S462	NGLyd3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXrldGhPOTByIN88US=>	MkTGO\|IhcA>?	NGm4Oo1FVVOR	Ml3ERZR1\W63YYTld{Bk\WyuIHfyc5d1cA>?	M1z2flI{OzJ6MUG0
2884	MnfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2jNWlExOCEQvF2=	NGD5e2M4OiCq	M164eWROW09?	NIPwTm5CfHSnboXheIV{KGOnbHyg[5Jwf3Sq	Mo\NNlM{OjhzMUS=
2885	M33vRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NIrjZ\|QyODBizszN	M2jkNlczKGh?	NFLYPIdFVVOR	NYW5dnNsSXS2ZX71ZZRmeyClZXzsJIdzd3e2aB?=	NGjxVm0zOzN{OEGxOC=>
CRL-2396	NWPXbZBPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{XUOFExOCEQvF2=		M{XDOZdifGW{	MVPJR\|UxRTBwMEmyJO69VQ>?	NYWwZYpJOjNzNUO1NlQ>
TIB-48	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWCxNFAh\|ryP		MV\3ZZRmeg>?	M{n5XWlEPTB;MD6wPFgh\|ryP	M2joPFI{OTV\|NUK0
CRL-2396	NIe0dYxEgXSxdH;4bYMhSXO\|YYm=	NHTvZmMyKM7:TR?=	NHzFWZo1QCCq	MWT3ZZRmeg>?	MnHBTY5lfWOnczDhdI9xfG:\|aYO=	M1;pd\|I{OTV\|NUK0
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OCL-AML2	NWPLSZRJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWqzJO69VQ>?	M{W2OFczKGh?		MnzSSIlucW6rc3jld{Bk\WyuII\pZYJqdGm2eR?=	MV6yNlQ5QDJ2OR?=
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A-673	NXH1UlJJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MlrDNVAh\|ryP	NFrvW2k6PiCq	NVHLUldNTE2VTx?=	MY\JR\|UxRTBwMEOyJO69VQ>?	NGXCZ4ozOTR2OEW5NS=>
TC-32	M1foZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MV2xNEDPxE1?	NYX3SXFuQTZiaB?=	MWrEUXNQ	M4HObmlEPTB;MD6wN\|kh\|ryP	NHW4co4zOTR2OEW5NS=>
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SK-N-MC	NVLVNYk6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGnxeJIyOCEQvF2=	NYHKfXVkQTZiaB?=	M3jjbWROW09?	NHKwTW5KSzVyPUCuNFczKM7:TR?=	NGS3fZUzOTR2OEW5NS=>
CHLA-9	NHT2NXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2\OVlExKM7:TR?=	Mo\xPVYhcA>?	NVuxd\|hpTE2VTx?=	M{HmdWlEPTB;MD6wNVgh\|ryP	MV:yNVQ1QDV7MR?=
CHLA-10	NWfBZW5QT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUi2VmJjOTBizszN	Mn7jPVYhcA>?	M3;FU2ROW09?	M163W2lEPTB;MD6wOlAh\|ryP	NXfMWWhTOjF2NEi1PVE>
CHLA-25	NV;QXJdvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVK1W2tNOTBizszN	Mlm5PVYhcA>?	MV3EUXNQ	MW\JR\|UxRTBwMU[4JO69VQ>?	NF7vdlAzOTR2OEW5NS=>
CHLA-32	MnfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVGxNEDPxE1?	M1m2R\|k3KGh?	Mn32SG1UVw>?	MoLrTWM2OD1yLkGzOkDPxE1?	MX6yNVQ1QDV7MR?=
CHLA-56	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUCxUnhMOTBizszN	M1exb\|k3KGh?	NVf0XmQ4TE2VTx?=	MYXJR\|UxRTFyIN88US=>	MXuyNVQ1QDV7MR?=
CHLA-258	NVfSVnZiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYPlNmQ3OTBizszN	NY\1bnVGQTZiaB?=	MmLGSG1UVw>?	MoLCTWM2OD1yLkGzNkDPxE1?	MVWyNVQ1QDV7MR?=
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CHLA-119	NFjTd\|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVuxNEDPxE1?	M1q1S\|k3KGh?	MnuySG1UVw>?	MkfOTWM2OD1yLkCyNkDPxE1?	NF7mTlEzOTR2OEW5NS=>
CHLA-122	MnG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWO4e2tDOTBizszN	NWe0OJBSQTZiaB?=	MlP0SG1UVw>?	MlTPTWM2OD1yLkCxPUDPxE1?	NYXtZWhWOjF2NEi1PVE>
CHLA-136	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX2xNEDPxE1?	Ml7kPVYhcA>?	MYrEUXNQ	M1:2WmlEPTB;MD6wN\|kh\|ryP	M2HqOlIyPDR6NUmx
CHLA-140	Mn3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUSxNEDPxE1?	NEj3UnY6PiCq	NETodZdFVVOR	NV3adFluUUN3ME2wMlAzPiEQvF2=	M1nJ[\|IyPDR6NUmx
LA-N-6	NFz6fpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHvVfJkyOCEQvF2=	M2H4RVk3KGh?	NF7WbZFFVVOR	NUjiWJpYUUN3ME2wMlA2PCEQvF2=	M{PRVlIyPDR6NUmx
NB-1643	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NI\CV\|cyOCEQvF2=	NVTC[IgzQTZiaB?=	NIC3SoVFVVOR	M4rBcGlEPTB;MD6wN\|ch\|ryP	NHjWWWIzOTR2OEW5NS=>
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SK-N-BE-1	Mkf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3LNSlExKM7:TR?=	MWW5OkBp	MnrnSG1UVw>?	NETJSFVKSzVyPUCuNFI5KM7:TR?=	MknJNlE1PDh3OUG=
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SMS-KAN	M33YT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHTPUJAyOCEQvF2=	M130Ulk3KGh?	M3zLXWROW09?	NUDldWNFUUN3ME2wMlA{PCEQvF2=	NEHrbHAzOTR2OEW5NS=>
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SMS-KCNR	NHzUWmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXvCfnVCOTBizszN	M4LYbFk3KGh?	NV:xNmhCTE2VTx?=	NVT2TJBHUUN3ME2wMlAyOCEQvF2=	MX:yNVQ1QDV7MR?=
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DB	MX\DfZRwfG:6aXOgRZN{[Xl?	NWnkW3p4OTBizszN	NX3FRpIxPyCm		MWHJR\|UxRTBwMESyJO69VQ>?	NUL2cHZDOjF{OUG4Olc>
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LAMA-84	NIjMTYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3fhdFExKM7:TR?=	M3LmNlk3KGh?		MlvJTWM2OD1yLkC1O{DPxE1?	NFrldmszOTB7MU[zNy=>
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RD	NGGzcHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYnue4c4OTBizszN	NGfJWoo6PiCq		M{H3WWlEPTB;MD6yNlgh\|ryP	MkX5NlAyODh\|M{i=
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BT-12	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MW[xNEDPxE1?	NFzkN4g6PiCq		NIi1XY9KSzVyPUCuNFYxKM7:TR?=	MXqyNFExQDN\|OB?=
CHLA-266	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXm4fXhtOTBizszN	MmewPVYhcA>?		MVfJR\|UxRTBwMEeyJO69VQ>?	MWmyNFExQDN\|OB?=
TC-71	NYXhTFd{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3XXSFExKM7:TR?=	NW\uWGltQTZiaB?=		NFX3dIxKSzVyPUCuNVAzKM7:TR?=	MWOyNFExQDN\|OB?=
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NALM-6	NFHPe5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M121[\|ExKM7:TR?=	M3;NcFk3KGh?		M3vnSGlEPTB;MD6wOlIh\|ryP	NVnNO2luOjBzMEizN\|g>
COG-LL-317	NGG1O45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3jLelExKM7:TR?=	NXnL[YhMQTZiaB?=		MmroTWM2OD1yLkC0O{DPxE1?	NVGzZmp4OjBzMEizN\|g>
RS4-11	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4m3N\|ExKM7:TR?=	MoHOPVYhcA>?		MVvJR\|UxRTBwMEG4JO69VQ>?	MX[yNFExQDN\|OB?=
MOLT-4	NHPNd3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M13CfVExKM7:TR?=	NV\kT5JZQTZiaB?=		MkPyTWM2OD1yLkCyOkDPxE1?	M4nwV\|IxOTB6M{O4
CCRF-CEM	NXzjPZZoT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MlvDNVAh\|ryP	NWfFV3BPQTZiaB?=		NF7hdYFKSzVyPUCuNFk1KM7:TR?=	M3ewWVIxOTB6M{O4
Kasumi-1	NV7PUGFyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYXWTZNxOTBizszN	NITmWoY6PiCq		NITJXmlKSzVyPUCuNVA{KM7:TR?=	Mnz4NlAyODh\|M{i=
Karpas-299	Ml\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M37uXVExKM7:TR?=	NYHyRW9uQTZiaB?=		MV7JR\|UxRTBwMEO4JO69VQ>?	MkTkNlAyODh\|M{i=
Ramos-RA1	MoXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2rkfVExKM7:TR?=	MoP6PVYhcA>?		MV;JR\|UxRTBwMUK3JO69VQ>?	NVfEeGt7OjBzMEizN\|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 Formulation: 在10% 2-羟丙基-β-环糊精/1％碳酸氢钠中配制 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
储存条件	2年 -80°C 溶于溶剂
别名	N/A

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 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
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

Alisertib (MLN8237)

客户使用Selleck生产的Alisertib (MLN8237)发表文献199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

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 2019-10-14)

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