Alisertib (MLN8237)

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。

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RMB 983.87 现货
RMB 1725.78 现货
RMB 5505.84 现货
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客户使用Selleck该产品发表文献49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 Ml;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlUh|ryP NHTvWJQ4OiCq Mm\TSG1UVw>? NHrwVWZKSzVyPUCuNFQh|ryP Ml:3NlYyOzZ4OES=
LS174T MonWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP3NE42KM7:TR?= NIW3T4Y4OiCq MWPEUXNQ MVfJR|UxRTBwMEWg{txO MXyyOlE{PjZ6NB?=
T84 NF21dHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[wMlUh|ryP NG\JSoQ4OiCq MWDEUXNQ MmDpTWM2OD1yLkC5JO69VQ>? NXjQWpFLOjZzM{[2PFQ>
LS180 M4rweGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmwMlUh|ryP Mn\VO|IhcA>? MnzYSG1UVw>? M4HBT2lEPTB;MTFOwG0> MX[yOlE{PjZ6NB?=
SW948 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXLNE42KM7:TR?= NWGxO3RQPzJiaB?= MVzEUXNQ MWXJR|UxRTFizszN MVmyOlE{PjZ6NB?=
HCT15 NFHZO41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTjSoVwOC53IN88US=> MXq3NkBp MUfEUXNQ MnnSTWM2ODxyLkSg{txO NFXvVoUzPjF|Nk[4OC=>
DLD-1 NXvoRXRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzrfIQxNjVizszN NUjoXVMxPzJiaB?= MUTEUXNQ M{fHXmlEPTB:MD64JO69VQ>? Mo\JNlYyOzZ4OES=
MIP-101 MnSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHq1RYoxNjVizszN M1rIUVczKGh? MU\EUXNQ NHfFcXFKSzVyPUGg{txO M2HCOVI3OTN4Nki0
SNU1544 NFjkb4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PFbFAvPSEQvF2= M4HUTlczKGh? NHvsU2lFVVOR NHvKTG5KSzVyPUGg{txO NHP4fYIzPjF|Nk[4OC=>
OCI-Ly10 M1HnPWN6fG:2b4jpZ{BCe3OjeR?= M{PuWFczKGh? Mn\wSG1UVw>? NVf5WYtzUUN3ME2wMlA2QCEQvF2= M2HZV|I2QDd6M{Ox
SU-DHL2 M3jWfWN6fG:2b4jpZ{BCe3OjeR?= NVrNbGRIPzJiaB?= MYXEUXNQ NU\Vb|JZUUN3ME2wMlAyKM7:TR?= Mn7LNlU5Pzh|M{G=
OCI-LY7 NGjFT2VEgXSxdH;4bYMhSXO|YYm= M1fNVlczKGh? M4HtfGROW09? NH\yT|VKSzVyPUCuNFgyKM7:TR?= MXyyOVg4QDN|MR?=
SU-DHL6 NEHEe5REgXSxdH;4bYMhSXO|YYm= NXy2e5k1PzJiaB?= MmPaSG1UVw>? MlLyTWM2OD1yLkS4NkDPxE1? Mm\pNlU5Pzh|M{G=
Jeko-1 M4T5e2N6fG:2b4jpZ{BCe3OjeR?= M3T2NFczKGh? NFPYU3BFVVOR NV7rc4NLUUN3ME2wMlAzQSEQvF2= NUfUd21WOjV6N{izN|E>
JVM-2 MUXDfZRwfG:6aXOgRZN{[Xl? M3LuXlczKGh? M2jHcGROW09? MkXuTWM2OD1yLkCxJO69VQ>? M3HNR|I2QDd6M{Ox
Rec-1 M{jTXGN6fG:2b4jpZ{BCe3OjeR?= M1;jR|czKGh? MYDEUXNQ M1n5e2lEPTB;MD6wPFch|ryP NV72V4hHOjV6N{izN|E>
Z-138 M1f0eGN6fG:2b4jpZ{BCe3OjeR?= MWe3NkBp M4KwfmROW09? NWSxeVl{UUN3ME2wMlAyOyEQvF2= MYKyOVg4QDN|MR?=
H9 MUDDfZRwfG:6aXOgRZN{[Xl? MoP0O|IhcA>? MWDEUXNQ NXzHVmk5UUN3ME2wMlYh|ryP NYnLSmFQOjV6N{izN|E>
HH M1T0fWN6fG:2b4jpZ{BCe3OjeR?= MXK3NkBp NHHxbmRFVVOR M{jPUGlEPTB;MD63JO69VQ>? MmTDNlU5Pzh|M{G=
DND41 NIGySo1EgXSxdH;4bYMhSXO|YYm= NIHIZZY4OiCq NUjTSmZETE2VTx?= Mn\OTWM2OD1yLkGg{txO NHXzfFEzPTh5OEOzNS=>
CCL119 MnrOR5l1d3SxeHnjJGF{e2G7 NFTWN2I4OiCq MmL4SG1UVw>? MmDDTWM2OD1yLkC2NkDPxE1? MUGyOVg4QDN|MR?=
J.Cam 1.6 NIj1WWZEgXSxdH;4bYMhSXO|YYm= NYLa[5UyPzJiaB?= NUi3PJBITE2VTx?= MnLiTWM2OD1yLkGwOUDPxE1? NE\XUGozPTh5OEOzNS=>
Sup-T1 NYDQUWE2S3m2b4TvfIlkKEG|c3H5 Mn;wO|IhcA>? M3PrR2ROW09? MXnJR|UxRTJwMUSyJO69VQ>? M3;FWFI2QDd6M{Ox
Tib 152 NH\mN3VEgXSxdH;4bYMhSXO|YYm= NFr6VHI4OiCq MlrDSG1UVw>? MoDQTWM2OD1yLkig{txO NFXkeW8zPTh5OEOzNS=>
MCF7 NHfUe|ZHfW6ldHnvckBCe3OjeR?= NIC1N482KM7:TR?= M37BblI1KGh? M{DYTWROW09? MWDJcoR2[2W|IFeyM20h[XK{ZYP0 NEnhcnYzPTh|NESwNS=>
MDA-MB-231 NUTRfHlZTnWwY4Tpc44hSXO|YYm= M1\BN|Uh|ryP M1rCVlI1KGh? NI\aOoVFVVOR M1rkNGlv\HWlZYOgS|MwVSCjcoLld5Q> NGfmXlYzPTh|NESwNS=>
MCF7 Mn\tSpVv[3Srb36gRZN{[Xl? MofWOUDPxE1? NIDIbHkzPCCq NYPBbJdjTE2VTx?= MmDNSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|EwS0SFMh?= MUSyOVg{PDRyMR?=
MCF7 MlzNSpVv[3Srb36gRZN{[Xl? NVXWNHZ{PSEQvF2= NFfnc4MzPCCq NUnhO2NUTE2VTx?= NYHJe4t3TGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? M4jNfVI2QDN2NECx
MCF7 MlXwSpVv[3Srb36gRZN{[Xl? MXi1JO69VQ>? M2jyVlI1KGh? MXnEUXNQ MYLE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz NEK4OGUzPTh|NESwNS=>
MCF7 NHTFO|NHfW6ldHnvckBCe3OjeR?= M2PDflUh|ryP M2m3flI1KGh? MYHEUXNQ Mlq0TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> MnW4NlU5OzR2MEG=
MCF7 NVjVdZdzTnWwY4Tpc44hSXO|YYm= NUPVfZlTPSEQvF2= NHP4UY4zPCCq NFrITIJFVVOR NXnVb3ZtUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzPyCNaYCx NF3YNFEzPTh|NESwNS=>
MDA-MB-231 MlPBSpVv[3Srb36gRZN{[Xl? NXHz[ppJPSEQvF2= NHHacWUzPCCq Mn;DSG1UVw>? NYSxdm9WTGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzFxQ1TDNi=> M4nC[FI2QDN2NECx
MDA-MB-231 NGj0[3FHfW6ldHnvckBCe3OjeR?= M4TETVEh|ryP MnmwNlQhcA>? MYXEUXNQ M4XQdGlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz MkHWNlU5OzR2MEG=
MDA-MB-231 NInGS2ZHfW6ldHnvckBCe3OjeR?= MV:1JO69VQ>? NGjmOVAzPCCq MorBSG1UVw>? MWrE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz MYeyOVg{PDRyMR?=
MDA-MB-231 Mn;VSpVv[3Srb36gRZN{[Xl? MUW1JO69VQ>? MVOyOEBp M2\kTGROW09? NYDiNHZtUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? NXKxfId4OjV6M{S0NFE>
MDA-MB-231 MojLSpVv[3Srb36gRZN{[Xl? NXrpcGYzPSEQvF2= NXm2UYh1OjRiaB?= NYfxPIl4TE2VTx?= NGfhXpFKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= NEOxVJEzPTh|NESwNS=>
MDA-MB-231 MofpSpVv[3Srb36gRZN{[Xl? MVW1JO69VQ>? M2nhfFI1KGh? MoC5SG1UVw>? NIDUPZZKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFU{ M2DGU|I2QDN2NECx
MCF7 M3K3OGFxd3C2b4Ppd{BCe3OjeR?= M3vGeFUh|ryP NY\vR5RnOjRiaB?= M2DLN2ROW09? NHf1XodKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= M4P2OVI2QDN2NECx
MDA-MB-231 M3XXU2Fxd3C2b4Ppd{BCe3OjeR?= M{fjS|Uh|ryP NUCxUVJVOjRiaB?= NXPwWnV4TE2VTx?= NWnG[VVGUW6mdXPld{BieG:ydH;0bYMh\GWjdHi= MlX4NlU5OzR2MEG=
MCF7 MkjoSpVv[3Srb36gRZN{[Xl? NVTzfmRiOSEQvF2= MUi3NkBp NYDCb4JCTE2VTx?= Mn;aTY5lfWOnczDheZRweGijZ3njJIRm[XSq MnTMNlU5OzR2MEG=
MDA-MB-231 M3m3WGZ2dmO2aX;uJGF{e2G7 NV\MVXBtOSEQvF2= MXS3NkBp NVLT[mdSTE2VTx?= NFv3O3hKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= MX[yOVg{PDRyMR?=
U-2 OS MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\UOVAh|ryP MlztNlQhcA>? MWPEUXNQ MojxTWM2OD1zNj62JO69VQ>? MkH1NlU4QTJ6MUG=
MG-63 MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILmd3c2OCEQvF2= MVGyOEBp NXS5PZdkTE2VTx?= NU\rTIlEUUN3ME25MlUh|ryP MXGyOVc6OjhzMR?=
U-2 OS NHPnWIhCeG:ydH;zbZMhSXO|YYm= MmPBOUDPxE1? NIHPcm0zPCCq MWTEUXNQ M17m[Glv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> Mo[yNlU4QTJ6MUG=
MG-63 MUDBdI9xfG:|aYOgRZN{[Xl? MXG1JO69VQ>? MlzXNlQhcA>? NEfZd4dFVVOR M2PsVGlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> NFrJXnozPTd7MkixNS=>
U-2 OS MoK3SpVv[3Srb36gRZN{[Xl? MWm1JO69VQ>? NVrlVpM2OjRiaB?= NFz1fppFVVOR NVT1TXlnWHKxbX;0[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq NE\aV5QzPTd7MkixNS=>
MG-63 NVzrbWtYTnWwY4Tpc44hSXO|YYm= NFLlUGk2KM7:TR?= NHzFbnozPCCq NEfXflJFVVOR MYfQdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> NXPKU2lrOjV5OUK4NVE>
PANC-1 NYDaWJBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDHcpJ1PTBizszN NX7adnBlOjRiaB?= NF\LV2xFVVOR NX\QdYh1UUN3ME23MlEh|ryP M{jXNlI2PjN{MkK1
BxPC-3 M4DkVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\4[Yx2PTBizszN M{PS[|I1KGh? NWnRdXFWTE2VTx?= NIrzdZVKSzVyPU[uPEDPxE1? MV[yOVY{OjJ{NR?=
PANC-1 MV7GeY5kfGmxbjDBd5NigQ>? NF30eVM2KM7:TR?= MUCyOEBp NX3CSXF6TE2VTx?= MWrJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> NHj6[|czPTZ|MkKyOS=>
BxPC-3 NX7XS|V4TnWwY4Tpc44hSXO|YYm= M2jnZVUh|ryP MV2yOEBp MXTEUXNQ NXHMb3NqUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBqdiCJMj;NJJBp[XOn MUGyOVY{OjJ{NR?=
PANC-1 MlTWSpVv[3Srb36gRZN{[Xl? MlHEOUDPxE1? M1fEUlI1KGh? MlPISG1UVw>? MUPJcoR2[2W|IHH1eI9xcGGpaXOgZ4VtdCCmZXH0bC=> MmjMNlU3OzJ{MkW=
BxPC-3 M4KzR2Z2dmO2aX;uJGF{e2G7 M4q0VVUh|ryP MXqyOEBp MlXFSG1UVw>? M33hSWlv\HWlZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp M{jwUlI2PjN{MkK1
SKOV3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHaNYcyODBizszN MljDNlQhcA>? MnnzSG1UVw>? MYHJR|UxRTJyLkS4JO69VQ>? MoPENlU3OjR5NUC=
OVCAR4 NELHe4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVixU2tLOTByIN88US=> MUGyOEBp NVj6WlRsTE2VTx?= NI\IZ|dKSzVyPUKyMlE{KM7:TR?= NU[0N25VOjV4MkS3OVA>
SKOV3 M1;EVWZ2dmO2aX;uJGF{e2G7 MmfqOUDPxE1? M3fzNFczKGh? NVj2bXBDTE2VTx?= NFf5No1KdmS3Y3XzJGczN01iYYLy[ZN1 MVyyOVYzPDd3MB?=
OVCAR4 M1i0O2Z2dmO2aX;uJGF{e2G7 Mke3OUDPxE1? Mk[5O|IhcA>? MlLQSG1UVw>? MoLLTY5lfWOnczDHNk9OKGG{cnXzeC=> MW[yOVYzPDd3MB?=
SKOV3 NHTzT2dCeG:ydH;zbZMhSXO|YYm= MoHxOUDPxE1? NX7PT2hxOjRiaB?= NXHSdZF6TE2VTx?= NEXUZ21KdmS3Y3XzJIFxd3C2b4Ppdy=> NUfwRWNEOjV4MkS3OVA>
OVCAR4 MUXBdI9xfG:|aYOgRZN{[Xl? M4fpNFUh|ryP NEPtdWMzPCCq NF7tbZhFVVOR MmTlTY5lfWOnczDhdI9xfG:|aYO= M{\wV|I2PjJ2N{Ww
AGS NX;lTlk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIj0TXMzPSEQvF2= NXS2W2R1OjRiaB?= NW\HeYpOTE2VTx?= NITxVlhKSzVyPUG5MlA6KM7:TR?= MlHpNlU3ODl7MkO=
NCI-N78 NGDYfmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\jNlUh|ryP NUXmXWQ6OjRiaB?= M1yzNmROW09? MX\JR|UxRTJ4LkOzJO69VQ>? MXyyOVYxQTl{Mx?=
AGS NVrSOZR5SXCxcITvd4l{KEG|c3H5 NX\rZ|MyPSEQvF2= M320c|I1KGh? MoLySG1UVw>? NYHJfmtXUW6mdXPld{BieG:ydH;zbZM> M3X3OVI2PjB7OUKz
NCI-N78 MlyxRZBweHSxc3nzJGF{e2G7 MY[1JO69VQ>? NVnqRWNvOjRiaB?= NHW0S3JFVVOR NXnmfGZVUW6mdXPld{BieG:ydH;zbZM> NGnER2gzPTZyOUmyNy=>
AGS NYDyRVRKTnWwY4Tpc44hSXO|YYm= NUHUUVAzPSEQvF2= MYOyOEBp MWjEUXNQ MkTFTY5lfWOnczD0bIUh[XW2b4DoZYd6 NHjSV|AzPTZyOUmyNy=>
NCI-N78 MX;GeY5kfGmxbjDBd5NigQ>? NUXwRW5DPSEQvF2= MVqyOEBp MVXEUXNQ MYnJcoR2[2W|IITo[UBifXSxcHjh[5k> NXHoXYRMOjV4MEm5NlM>
HSC-3 Mln3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHoOG9pOSEQvF2= NEP3TVQ1QCCq MkDlTWM2OD1yLkW0JO69VQ>? NVzrWWFCOjV|Nk[xOFM>
GB30 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTFNUDPxE1? M2nnSlch\A>? M{PWcmROW09? NHnuOJlKSzVyPUCuNFEyKM7:TR?= MUmyOVExPjR{OB?=
GB9 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWeybJhwOSEQvF2= NU\RUVdLPyCm M37YWGROW09? M2DrVGlEPTB;MD6wNlQh|ryP MYiyOVExPjR{OB?=
GB169 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D0U|Eh|ryP NY\sepF1PyCm NUPJOGpRTE2VTx?= M2XafmlEPTB;MD6wN|Ih|ryP NV3oXphUOjVzME[0Nlg>
T24 NEXaXYdHfW6ldHnvckBCe3OjeR?= MWSxJO69VQ>? NFvIc5A1QCCq NFvRXmZFVVOR M{PGNmlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NX65OoFrOjN2MEO2N|M>
RT4 M3nOOWZ2dmO2aX;uJGF{e2G7 MnjsNUDPxE1? NUjWSo9yPDhiaB?= NGDKVVJFVVOR MorETY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NGWwemUzOzRyM{[zNy=>
UM-UC-3 NFzVZZRHfW6ldHnvckBCe3OjeR?= MUmxJO69VQ>? NYTxc5ZYPDhiaB?= NF7LVWhFVVOR M13QN2lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MlvENlM1ODN4M{O=
T24 MXTBdI9xfG:|aYOgRZN{[Xl? M{foZlMvOTZizszN NETQTJk6PiCq NWe2dHRITE2VTx?= NEXFOnhKSzVyPUCuNFMxPiEQvF2= NIXUUY4zOzRyM{[zNy=>
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SJ-GBM2 NWC4UmVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHxcIcyOCEQvF2= MoTTPVYhcA>? NFjWcHlKSzVyPUCuNFUxKM7:TR?= NGLRcVEzODFyOEOzPC=>
NALM-6 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TTdlExKM7:TR?= M3[y[|k3KGh? NGO2R2RKSzVyPUCuNFYzKM7:TR?= NInzVHMzODFyOEOzPC=>
COG-LL-317 MoXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPRNJFJOTBizszN M4K4blk3KGh? NVHySGprUUN3ME2wMlA1PyEQvF2= NV[z[nZUOjBzMEizN|g>
RS4-11 NVq1UmpzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKxNEDPxE1? NFrM[lY6PiCq NVf5fFJsUUN3ME2wMlAyQCEQvF2= MkflNlAyODh|M{i=
MOLT-4 MlHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfVVHExOTBizszN M1G2V|k3KGh? M17we2lEPTB;MD6wNlYh|ryP NXi0N3JjOjBzMEizN|g>
CCRF-CEM NHHrdVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoOwNVAh|ryP M1npUFk3KGh? NV\hbWQ4UUN3ME2wMlA6PCEQvF2= M2XXTlIxOTB6M{O4
Kasumi-1 MoqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13jWlExKM7:TR?= MV65OkBp MXrJR|UxRTBwMUCzJO69VQ>? NVXRd|YyOjBzMEizN|g>
Karpas-299 M{P3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7j[ngyOCEQvF2= MlvIPVYhcA>? MX;JR|UxRTBwMEO4JO69VQ>? MWOyNFExQDN|OB?=
Ramos-RA1 NGHwWWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLnNVAh|ryP MoDhPVYhcA>? M4S4RmlEPTB;MD6xNlch|ryP MVqyNFExQDN|OB?=

... 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]
+ 展开

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]
+ 展开
  • 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]
+ 展开
  • 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
稳定性 powder
in solvent
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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02860000 Recruiting Estrogen Receptor Status|HER2/Neu Negative|Invasive Breast Carcinoma|Postmenopausal|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Mayo Clinic|National Cancer Institute (NCI) July 6 2017 Phase 2
NCT02860000 Recruiting Estrogen Receptor Status|HER2/Neu Negative|Invasive Breast Carcinoma|Postmenopausal|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Mayo Clinic|National Cancer Institute (NCI) July 6 2017 Phase 2
NCT02700022 Terminated Diffuse Large B-cell Lymphoma|Follicular Lymphoma|Burkitt Lymphoma UNC Lineberger Comprehensive Cancer Center|Millennium Pharmaceuticals Inc. October 2016 Phase 1
NCT02700022 Terminated Diffuse Large B-cell Lymphoma|Follicular Lymphoma|Burkitt Lymphoma UNC Lineberger Comprehensive Cancer Center|Millennium Pharmaceuticals Inc. October 2016 Phase 1
NCT02812056 Withdrawn 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
NCT02812056 Withdrawn 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

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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