Alisertib (MLN8237)

For research use only. Not for use in humans.

目录号:S1133

Alisertib (MLN8237) Chemical Structure

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  
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199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。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=>
GB9 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2xJO69VQ>? MlHKO{Bl MXvEUXNQ NHj6fJZKSzVyPUCuNFI1KM7:TR?= MX6yOVExPjR{OB?=
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=>
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TC-71 NYXhTFd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XXSFExKM7:TR?= NW\uWGltQTZiaB?= NFX3dIxKSzVyPUCuNVAzKM7:TR?= MWOyNFExQDN|OB?=
SJ-GBM2 MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\vVIUyOCEQvF2= NVLCS3d[QTZiaB?= M4nrR2lEPTB;MD6wOVAh|ryP NVXybYZTOjBzMEizN|g>
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     


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
  • 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)

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

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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID