Alisertib (MLN8237) 化学構造
分子量: 518.92

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Quality Control & MSDS

製品説明

  • Compare Aurora Kinase Inhibitors
    Aurora Kinase製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Alisertib (MLN8237)は、1.2nMのIC50による選択的なオーロラA阻害剤です。
ターゲット Aurora A
IC50 1.2 nM [1]
In vitro試験 MLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases. [1] MLN8237 (0.5 μM) treatment inhibits the phosphorylation of Aurora A in MM1.S and OPM1 cells, without affecting the Aurora B mediated histone H3 phosphorylation. MLN8237 significantly inhibits cell proliferation in multiple myeloma (MM) cell lines with IC50 values of 0.003-1.71 μM. MLN8237 displays more potent anti-proliferation activity against primary MM cells and MM cell lines in the presence of BM stroma cells, as well as IL-6 and IGF-1 than against MM cells alone. MLN8237 (0.5 μM) induces 2- to 6-fold increase in G2/M phase in primary MM cells and cell lines, as well as significant apoptosis and senescence, involving the up-regulation of p53, p21 and p27, as well as PARP, caspase 3, and caspase 9 cleavage. In addition, MLN8237 shows strong synergistic anti-MM effect with dexamethasone, as well as additive effect with doxorubicin and bortezomib. [2] MLN8237 (0.5 μM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage of polyploid cells, and subsequently an increase in the percentage of cells in the sub-G1 phase, which can be further enhanced in combination with cisplatin (2.5 μM), involving the higher induction of TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP as compared with a single-agent treatment. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HCT116 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17nUVAvPSEQvF2= NEP5SI44OiCq MU\EUXNQ NVL1bok2UUN3ME2wMlA1KM7:TR?= MWeyOlE{PjZ6NB?=
LS174T NIWxVW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rZT|AvPSEQvF2= NEj6c484OiCq MnztSG1UVw>? NWPjR3k1UUN3ME2wMlA2KM7:TR?= NHK1NWYzPjF|Nk[4OC=>
T84 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrzfYU3OC53IN88US=> NGLJW3o4OiCq MnPGSG1UVw>? NGLJWWdKSzVyPUCuNFkh|ryP M{\5NFI3OTN4Nki0
LS180 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTJNE42KM7:TR?= MlW4O|IhcA>? M2PhPWROW09? MVzJR|UxRTFizszN MoKxNlYyOzZ4OES=
SW948 M{LsS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\WNE42KM7:TR?= NGH2OWQ4OiCq Ml3pSG1UVw>? MV3JR|UxRTFizszN M1HYOlI3OTN4Nki0
HCT15 NELze2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXXNE42KM7:TR?= MX23NkBp MYjEUXNQ M3e3fmlEPTB:MD60JO69VQ>? NX3helF{OjZzM{[2PFQ>
DLD-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3u1VFAvPSEQvF2= M{\UZ|czKGh? MULEUXNQ M1vDRmlEPTB:MD64JO69VQ>? NEXVdXczPjF|Nk[4OC=>
MIP-101 MlyzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoewNE42KM7:TR?= NW\qWIJ7PzJiaB?= MY\EUXNQ NUXrS3ViUUN3ME2xJO69VQ>? MXKyOlE{PjZ6NB?=
SNU1544 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmX4NE42KM7:TR?= M1PLR|czKGh? MkfzSG1UVw>? NH\aW|JKSzVyPUGg{txO NYGwOosyOjZzM{[2PFQ>
OCI-Ly10 M3LUSGN6fG:2b4jpZ{BCe3OjeR?= M1TOVlczKGh? M{TIRmROW09? MVPJR|UxRTBwMEW4JO69VQ>? NGTzSlEzPTh5OEOzNS=>
SU-DHL2 NV7oNYxPS3m2b4TvfIlkKEG|c3H5 MX63NkBp NGHKfXRFVVOR M1jvfmlEPTB;MD6wNUDPxE1? Ml7wNlU5Pzh|M{G=
OCI-LY7 NIn4N2ZEgXSxdH;4bYMhSXO|YYm= MWq3NkBp NHyyUoFFVVOR MonGTWM2OD1yLkC4NUDPxE1? NWDmWo1POjV6N{izN|E>
SU-DHL6 NHXRVlBEgXSxdH;4bYMhSXO|YYm= M1q0XlczKGh? Mo\YSG1UVw>? MYPJR|UxRTBwNEiyJO69VQ>? NUiyfVEyOjV6N{izN|E>
Jeko-1 MXvDfZRwfG:6aXOgRZN{[Xl? NHrWNoU4OiCq MmrVSG1UVw>? MV;JR|UxRTBwMEK5JO69VQ>? Ml72NlU5Pzh|M{G=
JVM-2 NYTUSFQ3S3m2b4TvfIlkKEG|c3H5 NEi5dm44OiCq NFXwXoNFVVOR NVe4WIVmUUN3ME2wMlAyKM7:TR?= MnTMNlU5Pzh|M{G=
Rec-1 NF\6SVZEgXSxdH;4bYMhSXO|YYm= NGm3PVY4OiCq MXLEUXNQ NX;WTnR{UUN3ME2wMlA5PyEQvF2= NX3EV5ZHOjV6N{izN|E>
Z-138 M3fpPGN6fG:2b4jpZ{BCe3OjeR?= MY[3NkBp M2LNcmROW09? MXPJR|UxRTBwMEGzJO69VQ>? NV;uNVE2OjV6N{izN|E>
H9 MnjjR5l1d3SxeHnjJGF{e2G7 MXK3NkBp M4jze2ROW09? NWHsdJFmUUN3ME2wMlYh|ryP MoHtNlU5Pzh|M{G=
HH NGTvVJZEgXSxdH;4bYMhSXO|YYm= Ml\PO|IhcA>? NYfhOWxmTE2VTx?= NIXn[mpKSzVyPUCuO{DPxE1? NHvmNYkzPTh5OEOzNS=>
DND41 NVj5d29zS3m2b4TvfIlkKEG|c3H5 MnHBO|IhcA>? NYHDZ4tiTE2VTx?= NHzpTJdKSzVyPUCuNUDPxE1? NXq3XpQ{OjV6N{izN|E>
CCL119 MmXtR5l1d3SxeHnjJGF{e2G7 MYW3NkBp NHXtbJVFVVOR NVXHcFZ{UUN3ME2wMlA3OiEQvF2= MlfwNlU5Pzh|M{G=
J.Cam 1.6 NW\tVWZES3m2b4TvfIlkKEG|c3H5 M{XiVFczKGh? NWTJSWFSTE2VTx?= MWTJR|UxRTBwMUC1JO69VQ>? M4DWRlI2QDd6M{Ox
Sup-T1 MWnDfZRwfG:6aXOgRZN{[Xl? NF\VZlk4OiCq MmG3SG1UVw>? NYfBfpBHUUN3ME2yMlE1OiEQvF2= MXSyOVg4QDN|MR?=
Tib 152 NE[0Z|JEgXSxdH;4bYMhSXO|YYm= MWW3NkBp NEXlcWRFVVOR MmjUTWM2OD1yLkig{txO Ml65NlU5Pzh|M{G=
MCF7 NGHiXVVHfW6ldHnvckBCe3OjeR?= NHSzeG82KM7:TR?= NICxUG8zPCCq NG\mcG9FVVOR NYTMN5kzUW6mdXPld{BIOi:PIHHydoV{fA>? NHPhdo4zPTh|NESwNS=>
MDA-MB-231 NVnRUm1{TnWwY4Tpc44hSXO|YYm= Mlu3OUDPxE1? NHjNRpAzPCCq MorzSG1UVw>? NIW4dpVKdmS3Y3XzJGc{N01iYYLy[ZN1 M1;WTFI2QDN2NECx
MCF7 NYPtdJNRTnWwY4Tpc44hSXO|YYm= M3zOclUh|ryP MmPhNlQhcA>? MmmzSG1UVw>? MULE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ MYiyOVg{PDRyMR?=
MCF7 NFHFd5RHfW6ldHnvckBCe3OjeR?= NHr2cnM2KM7:TR?= NXG3NlN6OjRiaB?= NXm2NZViTE2VTx?= NILlfHNF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? NY\Rc2c5OjV6M{S0NFE>
MCF7 MX;GeY5kfGmxbjDBd5NigQ>? MlvTOUDPxE1? NHTmcZYzPCCq NHP4S3FFVVOR MV;E[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz NX3aemNjOjV6M{S0NFE>
MCF7 MXLGeY5kfGmxbjDBd5NigQ>? NVnrSmExPSEQvF2= MXiyOEBp M2HmXGROW09? MkXlTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyNUBY[WZzL1PpdFE> MlixNlU5OzR2MEG=
MCF7 Ml64SpVv[3Srb36gRZN{[Xl? MoOzOUDPxE1? MlS4NlQhcA>? NV;DUod5TE2VTx?= MVvJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEK3JGtqeDF? MmnTNlU5OzR2MEG=
MDA-MB-231 NF\WTWpHfW6ldHnvckBCe3OjeR?= Moq2OUDPxE1? NV3ZR2cyOjRiaB?= M{PmdmROW09? MWjE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ NH3oUoUzPTh|NESwNS=>
MDA-MB-231 M3fzcGZ2dmO2aX;uJGF{e2G7 MXyxJO69VQ>? NUXaXWJWOjRiaB?= NEG3XXBFVVOR M37DN2lv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz MXuyOVg{PDRyMR?=
MDA-MB-231 NIL1dYhHfW6ldHnvckBCe3OjeR?= NUG2b|dGPSEQvF2= NULhcFdnOjRiaB?= NWPZV2pKTE2VTx?= Ml7TSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIHP5Z4xqdiCEMR?= MnjYNlU5OzR2MEG=
MDA-MB-231 MlLJSpVv[3Srb36gRZN{[Xl? MkD1OUDPxE1? NG\RPGQzPCCq MVTEUXNQ M2m3Omlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlEhX2GoMT;DbZAy MWOyOVg{PDRyMR?=
MDA-MB-231 M4X5eGZ2dmO2aX;uJGF{e2G7 Mn3yOUDPxE1? NWGwWWJiOjRiaB?= NW\ycXRlTE2VTx?= NITQVoZKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= NGP5c|gzPTh|NESwNS=>
MDA-MB-231 MkDjSpVv[3Srb36gRZN{[Xl? Mo\qOUDPxE1? MnrJNlQhcA>? MnzxSG1UVw>? MYTJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEWz MmDlNlU5OzR2MEG=
MCF7 NYDvSIJlSXCxcITvd4l{KEG|c3H5 NV:0SIxlPSEQvF2= MkXuNlQhcA>? MmT5SG1UVw>? MWDJcoR2[2W|IHHwc5B1d3SrYzDk[YF1cA>? MWGyOVg{PDRyMR?=
MDA-MB-231 MmG3RZBweHSxc3nzJGF{e2G7 M{fwR|Uh|ryP MUWyOEBp NVv6eGpjTE2VTx?= MW\JcoR2[2W|IHHwc5B1d3SrYzDk[YF1cA>? NEfqZ4YzPTh|NESwNS=>
MCF7 M3SyZmZ2dmO2aX;uJGF{e2G7 MXKxJO69VQ>? MnjuO|IhcA>? MXzEUXNQ MonmTY5lfWOnczDheZRweGijZ3njJIRm[XSq NIS0e5MzPTh|NESwNS=>
MDA-MB-231 NVjEWY1LTnWwY4Tpc44hSXO|YYm= MkDBNUDPxE1? MXq3NkBp MWPEUXNQ NUniN4g3UW6mdXPld{BifXSxcHjh[4lkKGSnYYTo NIn3VmwzPTh|NESwNS=>
U-2 OS MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPlXJV4PTBizszN NVTEV2ZsOjRiaB?= MnHFSG1UVw>? NXLESlhmUUN3ME2xOk43KM7:TR?= M1WxfVI2Pzl{OEGx
MG-63 NF7WR3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3X0ZlUxKM7:TR?= M4jJdlI1KGh? M4HNemROW09? M4TvO2lEPTB;OT61JO69VQ>? MoH3NlU4QTJ6MUG=
U-2 OS NWTiN5hbSXCxcITvd4l{KEG|c3H5 NFLF[HE2KM7:TR?= MYOyOEBp NWe3WoRmTE2VTx?= NVLZfI1rUW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>? MlL2NlU4QTJ6MUG=
MG-63 NEX0VIVCeG:ydH;zbZMhSXO|YYm= NYT4c4hmPSEQvF2= MXiyOEBp NIjUOYhFVVOR MU\JcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo MXOyOVc6OjhzMR?=
U-2 OS NUnVUoVtTnWwY4Tpc44hSXO|YYm= MXq1JO69VQ>? MkixNlQhcA>? NV;DO3BYTE2VTx?= NGD3[4dRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? NWfp[3lyOjV5OUK4NVE>
MG-63 NF\rXZlHfW6ldHnvckBCe3OjeR?= NGrMZ|k2KM7:TR?= M2XoXFI1KGh? NEfPcY9FVVOR MV;Qdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> NWjCVY11OjV5OUK4NVE>
PANC-1 M4HFPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLGRYhEPTBizszN MWSyOEBp M37leGROW09? MVnJR|UxRTdwMTFOwG0> M{XlbFI2PjN{MkK1
BxPC-3 NUfRWVNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzhU5g2OCEQvF2= NXrqdIp2OjRiaB?= NHHqVXBFVVOR Ml;qTWM2OD14Lkig{txO NFjnRmEzPTZ|MkKyOS=>
PANC-1 NGW3NlZHfW6ldHnvckBCe3OjeR?= MnTMOUDPxE1? M3npcFI1KGh? MmT2SG1UVw>? MkjvTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDpckBIOi:PIIDoZZNm NV22eXJpOjV4M{KyNlU>
BxPC-3 M{ToOGZ2dmO2aX;uJGF{e2G7 NH;OUZc2KM7:TR?= MkOxNlQhcA>? MlfnSG1UVw>? NYrlbWVFUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBqdiCJMj;NJJBp[XOn NF7zdJgzPTZ|MkKyOS=>
PANC-1 NWS5dVIyTnWwY4Tpc44hSXO|YYm= NGn3Ro02KM7:TR?= NGC5OXAzPCCq NETUfnJFVVOR NE\DeGRKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? Mm\sNlU3OzJ{MkW=
BxPC-3 MnftSpVv[3Srb36gRZN{[Xl? M4jmelUh|ryP Mn6wNlQhcA>? NXzQfJlwTE2VTx?= NILBfVJKdmS3Y3XzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? NUjiXndmOjV4M{KyNlU>
SKOV3 M{my[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHyTmU3OTByIN88US=> NUT1VpljOjRiaB?= NFzvZoNFVVOR MYPJR|UxRTJyLkS4JO69VQ>? NF\WfHozPTZ{NEe1NC=>
OVCAR4 M{f0dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD3UIFzOTByIN88US=> MXiyOEBp NGP5NHJFVVOR NXnaXlVuUUN3ME2yNk4yOyEQvF2= MWOyOVYzPDd3MB?=
SKOV3 NIOwdW1HfW6ldHnvckBCe3OjeR?= MnTIOUDPxE1? MoT4O|IhcA>? NYLWXlB1TE2VTx?= NWrmWGREUW6mdXPld{BIOi:PIHHydoV{fA>? M4TPflI2PjJ2N{Ww
OVCAR4 Mkm4SpVv[3Srb36gRZN{[Xl? NIPlVGE2KM7:TR?= NETOfHg4OiCq MmXESG1UVw>? MoTqTY5lfWOnczDHNk9OKGG{cnXzeC=> MoW0NlU3OjR5NUC=
SKOV3 NIXaRXFCeG:ydH;zbZMhSXO|YYm= MVy1JO69VQ>? NFvMUIYzPCCq NIHtW2RFVVOR MVHJcoR2[2W|IHHwc5B1d3Orcx?= MmjuNlU3OjR5NUC=
OVCAR4 NIKxc4NCeG:ydH;zbZMhSXO|YYm= NYjEfmxvPSEQvF2= NUn4NJRPOjRiaB?= MV\EUXNQ NE\1cY1KdmS3Y3XzJIFxd3C2b4Ppdy=> NVu1NFFHOjV4MkS3OVA>
AGS MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[yOUDPxE1? NF3ZW3YzPCCq NGLUPFhFVVOR MX\JR|UxRTF7LkC5JO69VQ>? MV[yOVYxQTl{Mx?=
NCI-N78 NYD0ZY1XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TiTVI2KM7:TR?= MV6yOEBp MUPEUXNQ NEe0e5JKSzVyPUK2MlM{KM7:TR?= MoXJNlU3ODl7MkO=
AGS MYXBdI9xfG:|aYOgRZN{[Xl? NGnQTHM2KM7:TR?= M3\2XVI1KGh? MVPEUXNQ NGDBfWRKdmS3Y3XzJIFxd3C2b4Ppdy=> M1jjWlI2PjB7OUKz
NCI-N78 M{HrTGFxd3C2b4Ppd{BCe3OjeR?= MUK1JO69VQ>? NVL0OnlWOjRiaB?= MniySG1UVw>? NECwZ3FKdmS3Y3XzJIFxd3C2b4Ppdy=> NV3UO2pYOjV4MEm5NlM>
AGS MYTGeY5kfGmxbjDBd5NigQ>? Ml3SOUDPxE1? MmHQNlQhcA>? MVvEUXNQ MWjJcoR2[2W|IITo[UBifXSxcHjh[5k> NXnSVos3OjV4MEm5NlM>
NCI-N78 MkL4SpVv[3Srb36gRZN{[Xl? NX:zb40yPSEQvF2= M4KxNFI1KGh? MoHQSG1UVw>? M1raUWlv\HWlZYOgeIhmKGG3dH;wbIFogQ>? M13ITFI2PjB7OUKz
HSC-3 MnPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm2OIl{OSEQvF2= NV7VbphoPDhiaB?= M1\IbWlEPTB;MD61OEDPxE1? NGPXfoYzPTN4NkG0Ny=>
GB30 M3nGVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3kNUDPxE1? MU[3JIQ> MojMSG1UVw>? Mnj5TWM2OD1yLkCxNUDPxE1? M3XLdlI2OTB4NEK4
GB9 NXL6N21DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;kVFEh|ryP M4\2ZVch\A>? NFjKZXVFVVOR NUC1bIJRUUN3ME2wMlAzPCEQvF2= NU\ReXVSOjVzME[0Nlg>
GB169 M13NUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTtc2cyKM7:TR?= MUC3JIQ> MVXEUXNQ NVm2WJBFUUN3ME2wMlA{OiEQvF2= M334eFI2OTB4NEK4
T24 MYfGeY5kfGmxbjDBd5NigQ>? MVGxJO69VQ>? MnHFOFghcA>? NHfQWGlFVVOR NWnS[29bUW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MoHtNlM1ODN4M{O=
RT4 MX7GeY5kfGmxbjDBd5NigQ>? MYWxJO69VQ>? NXXiT3VkPDhiaB?= M3PIbWROW09? MoX2TY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M2\EUVI{PDB|NkOz
UM-UC-3 NFHDc|dHfW6ldHnvckBCe3OjeR?= NWLifYdXOSEQvF2= M2j1elQ5KGh? MUPEUXNQ MonaTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M1[wclI{PDB|NkOz
T24 MUnBdI9xfG:|aYOgRZN{[Xl? MnrzN{4yPiEQvF2= M3K0Wlk3KGh? NEKzfoZFVVOR MkTPTWM2OD1yLkCzNFYh|ryP MYeyN|QxOzZ|Mx?=
RT4 MYLBdI9xfG:|aYOgRZN{[Xl? NEDmO3c{NjF4IN88US=> NHrHRW46PiCq M4jZWmROW09? NXPyeXpUUUN3ME2wMlEyQThizszN M3vZ[|I{PDB|NkOz
UM-UC-3 M{jCfWFxd3C2b4Ppd{BCe3OjeR?= MnzSN{4yPiEQvF2= NFu5Z2E6PiCq NHHPR4VFVVOR MUHJR|UxRTBwMES0PUDPxE1? NVzjXWlwOjN2MEO2N|M>
OVCAR-5 MoKwSpVv[3Srb36gRZN{[Xl? MmKyOVAhdk1? Ml;2TY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? MmjBNlM{OzR|Mke=
SKOV3ip2 MnHhSpVv[3Srb36gRZN{[Xl? MnKxOVAhdk1? NHe1eo1KdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MnXLNlM{OzR|Mke=
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MOLT-4 NXXlO|Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLGNVAh|ryP MlP3PVYhcA>? MVTJR|UxRTBwMEK2JO69VQ>? MkjiNlAyODh|M{i=
CCRF-CEM MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGC0bpcyOCEQvF2= MYG5OkBp NIDXUm5KSzVyPUCuNFk1KM7:TR?= MlXJNlAyODh|M{i=
Kasumi-1 M3LPZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O1N|ExKM7:TR?= M3T2blk3KGh? NUDL[mhVUUN3ME2wMlExOyEQvF2= MkfzNlAyODh|M{i=
Karpas-299 NFOzW|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnieHoyOCEQvF2= M3Tne|k3KGh? MYLJR|UxRTBwMEO4JO69VQ>? MlTaNlAyODh|M{i=
Ramos-RA1 M{H1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkOxNVAh|ryP M2jGXVk3KGh? NHrobWtKSzVyPUCuNVI4KM7:TR?= NVTOTJpFOjBzMEizN|g>

... Click to View More Cell Line Experimental Data

In vivo試験 MLN8237 significantly reduces the tumor burden with tumor growth inhibition (TGI) of 42% and 80% at 15 mg/kg and 30 mg/kg, respectively, and prolongs the survival of mice compared with the control. [2]
臨床試験 A Phase II study of MLN8237 for treatment of patients with ovarian, fallopian tube, or peritoneal carcinoma has been completed.
特集 First orally available inhibitor of Aurora A.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Aurora A radioactive Flashplate enzyme assay Aurora A radioactive Flashplate enzyme assay is conducted to determine the nature and degree of MLN8237-mediated inhibition in vitro. Recombinant Aurora A is expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A is conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) is assayed in 50 mM Hepes (pH 7.5), 10 mM MgCl2, 5 mM DTT, 0.05% Tween 20, 2 μM peptide substrate, 3.3 μCi/mL [γ-33P]ATP at 2 μM, and increasing concentrations of MLN8237 by using Image FlashPlates.

細胞アッセイ: [2]

細胞株 MM1.S, MM.1R, LR5, RPMI 8226, DOX40, OPM1, OPM2, INA6, and U266
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 24, 48, and 72 hours
実験の流れ Cells are exposed to various concentrations of MLN8237 for 24, 48, and 72 hours. Cells viability is measured using MTT assay, and cell proliferation is measured using 3[H]-thymidine incorporation. For cell cycle analysis, cells are permeabilized by 70% ethanol at -20 °C, and incubated with 50 μg/mL PI and 20 units/mL RNase-A. DNA content is analyzed by flow cytometry using BDFACS-Canto II and FlowJo software. For the detection of apoptosis and senescence, cells are stained with fluorescein isothiocyanate-annexin V and PI. Apoptotic cells are determined by flow cytometric analysis using BDFACS-Canto II and FlowJo software.

動物実験: [2]

動物モデル Severe combined immune-deficient (SCID) mice inoculated subcutaneously with MM1.S cells
製剤 Formulated in 10% 2-hydroxypropyl-β-cyclodextrin/1% sodium bicarbonate
投薬量 ~30 mg/kg/day
投与方法 Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Alisertib (MLN8237) SDF
分子量 518.92
化学式

C27H20ClFN4O4

CAS No. 1028486-01-2
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 27 mg/mL (52.03 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 15% Captisol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 Benzoic acid, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-

文献中の引用 (46)

Frequently Asked Questions

  • Question 1
    What is the suggested formulation of this compound for mouse injection(i.p.)?

    Answer: It can be dissolved in 6% DMSO/50% PEG 300/5% Tween 80/ddH2O at 10 mg/ml as a clear solution.

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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