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 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz2[oVtOC53IN88US=> NF\BN4Y4OiCq M4r6d2ROW09? MUHJR|UxRTBwMESg{txO MV[yOlE{PjZ6NB?=
LS174T M3rhVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX2wMlUh|ryP M33LPVczKGh? MYjEUXNQ NHP6RWZKSzVyPUCuNFUh|ryP M3;Me|I3OTN4Nki0
T84 M{f6OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH6SnUxNjVizszN M{TVfVczKGh? MW\EUXNQ NXXPNHJUUUN3ME2wMlA6KM7:TR?= MWeyOlE{PjZ6NB?=
LS180 MmHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nvSVAvPSEQvF2= NYLOR5ZuPzJiaB?= MmLlSG1UVw>? NILnRnBKSzVyPUGg{txO M4LmdFI3OTN4Nki0
SW948 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMlUh|ryP NYHFNWs1PzJiaB?= NHHkcG1FVVOR NWnEXWN2UUN3ME2xJO69VQ>? M{e5c|I3OTN4Nki0
HCT15 NGTGXWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfPNE42KM7:TR?= NEHOfJk4OiCq MUfEUXNQ MnL2TWM2ODxyLkSg{txO M4rBe|I3OTN4Nki0
DLD-1 MlXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWOwMlUh|ryP MVu3NkBp MnzrSG1UVw>? M3;Y[GlEPTB:MD64JO69VQ>? NXvBVnNOOjZzM{[2PFQ>
MIP-101 M4qwOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjsWpAxNjVizszN NFXOcmY4OiCq NHTjd5lFVVOR M2jwXWlEPTB;MTFOwG0> M4nKZ|I3OTN4Nki0
SNU1544 M1P5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXONE42KM7:TR?= M2PxNVczKGh? MVjEUXNQ MlzjTWM2OD1zIN88US=> NIS0e2gzPjF|Nk[4OC=>
OCI-Ly10 MkjWR5l1d3SxeHnjJGF{e2G7 NYL3[YRzPzJiaB?= NF7PTXVFVVOR MYDJR|UxRTBwMEW4JO69VQ>? NEHBd3ozPTh5OEOzNS=>
SU-DHL2 NUnh[4FKS3m2b4TvfIlkKEG|c3H5 NULFcVVbPzJiaB?= NXvuOnliTE2VTx?= NYO0SWt5UUN3ME2wMlAyKM7:TR?= M4f1UFI2QDd6M{Ox
OCI-LY7 MmjRR5l1d3SxeHnjJGF{e2G7 MV63NkBp MlHNSG1UVw>? M2jYOGlEPTB;MD6wPFEh|ryP MnG5NlU5Pzh|M{G=
SU-DHL6 MlfHR5l1d3SxeHnjJGF{e2G7 MU[3NkBp M3z5TmROW09? MWLJR|UxRTBwNEiyJO69VQ>? MknGNlU5Pzh|M{G=
Jeko-1 MXrDfZRwfG:6aXOgRZN{[Xl? MYi3NkBp M3e5VWROW09? Mny5TWM2OD1yLkCyPUDPxE1? NX7HcZl{OjV6N{izN|E>
JVM-2 NFS1NodEgXSxdH;4bYMhSXO|YYm= MYi3NkBp NHLEdJNFVVOR M3vPXWlEPTB;MD6wNUDPxE1? NH3tfWkzPTh5OEOzNS=>
Rec-1 MlTZR5l1d3SxeHnjJGF{e2G7 MX:3NkBp MnG0SG1UVw>? NULnNWd[UUN3ME2wMlA5PyEQvF2= NH;RT2EzPTh5OEOzNS=>
Z-138 NGHSOYtEgXSxdH;4bYMhSXO|YYm= NV\D[HM2PzJiaB?= MkjwSG1UVw>? NUjJd2RxUUN3ME2wMlAyOyEQvF2= MlP1NlU5Pzh|M{G=
H9 MXnDfZRwfG:6aXOgRZN{[Xl? MW[3NkBp NXvXWndvTE2VTx?= M4X3SmlEPTB;MD62JO69VQ>? M3S3OlI2QDd6M{Ox
HH M1:1fWN6fG:2b4jpZ{BCe3OjeR?= M4fQNVczKGh? NU\4RXpOTE2VTx?= NYDCUZo4UUN3ME2wMlch|ryP NIrXeYgzPTh5OEOzNS=>
DND41 NG\zVI1EgXSxdH;4bYMhSXO|YYm= MUe3NkBp MlG4SG1UVw>? MYLJR|UxRTBwMTFOwG0> M3fhcVI2QDd6M{Ox
CCL119 NXG1UlFES3m2b4TvfIlkKEG|c3H5 NEnlcIs4OiCq M2LHZWROW09? NWPVTYc{UUN3ME2wMlA3OiEQvF2= NFTifo8zPTh5OEOzNS=>
J.Cam 1.6 NVrGXFhPS3m2b4TvfIlkKEG|c3H5 NInEfVM4OiCq M{\COmROW09? M3Xid2lEPTB;MD6xNFUh|ryP MofiNlU5Pzh|M{G=
Sup-T1 Mn7RR5l1d3SxeHnjJGF{e2G7 NWLuUIFKPzJiaB?= MofFSG1UVw>? NHflWoxKSzVyPUKuNVQzKM7:TR?= MlKyNlU5Pzh|M{G=
Tib 152 NXLoT3VzS3m2b4TvfIlkKEG|c3H5 M1HD[FczKGh? NVrEb2tbTE2VTx?= MWrJR|UxRTBwODFOwG0> M4DtdFI2QDd6M{Ox
MCF7 MoHKSpVv[3Srb36gRZN{[Xl? MVK1JO69VQ>? NVHEbVlpOjRiaB?= M{LCXmROW09? M2rLNGlv\HWlZYOgS|IwVSCjcoLld5Q> NHHzPWkzPTh|NESwNS=>
MDA-MB-231 NXGzcpVSTnWwY4Tpc44hSXO|YYm= NEPHNZM2KM7:TR?= NHfle2gzPCCq MXnEUXNQ NUTNeZBqUW6mdXPld{BIOy:PIHHydoV{fA>? NHfKfowzPTh|NESwNS=>
MCF7 MWLGeY5kfGmxbjDBd5NigQ>? Mn65OUDPxE1? NGnMVYczPCCq M12yWWROW09? NFPNbIhF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy MUWyOVg{PDRyMR?=
MCF7 M{nvRWZ2dmO2aX;uJGF{e2G7 NILvVHo2KM7:TR?= NUTsR|IyOjRiaB?= MoCySG1UVw>? M1jtSmRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsz MXOyOVg{PDRyMR?=
MCF7 NIn5bI9HfW6ldHnvckBCe3OjeR?= NEi0cJY2KM7:TR?= NE\2fHkzPCCq MlvaSG1UVw>? MomxSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIHP5Z4xqdiCEMR?= NXSxeoI5OjV6M{S0NFE>
MCF7 M4LPbGZ2dmO2aX;uJGF{e2G7 NVHVTlc1PSEQvF2= NWDwb4t1OjRiaB?= NGT0VVBFVVOR M{LqN2lv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlEhX2GoMT;DbZAy MWGyOVg{PDRyMR?=
MCF7 M4jjWmZ2dmO2aX;uJGF{e2G7 M2DUSlUh|ryP MkX3NlQhcA>? NWTrS5BTTE2VTx?= MmPaTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIICyO{BMcXBz MYiyOVg{PDRyMR?=
MDA-MB-231 M{TndmZ2dmO2aX;uJGF{e2G7 NUnQXVlZPSEQvF2= M1HMWVI1KGh? NX;4O2EzTE2VTx?= NFTMenRF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy MVeyOVg{PDRyMR?=
MDA-MB-231 MUHGeY5kfGmxbjDBd5NigQ>? MXexJO69VQ>? MnS5NlQhcA>? MnfMSG1UVw>? Mmm5TY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|I> MYWyOVg{PDRyMR?=
MDA-MB-231 M1zBfWZ2dmO2aX;uJGF{e2G7 MVi1JO69VQ>? MVeyOEBp Ml7XSG1UVw>? MU\E[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz M1\0e|I2QDN2NECx
MDA-MB-231 NV7WV4xMTnWwY4Tpc44hSXO|YYm= M13pbVUh|ryP NWnqRZlYOjRiaB?= M13QOGROW09? MXXJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> MkCxNlU5OzR2MEG=
MDA-MB-231 M2PSRWZ2dmO2aX;uJGF{e2G7 M3uzNVUh|ryP NVjUUHJ4OjRiaB?= NIfldo9FVVOR NF;5bXlKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFI4KEurcEG= NV;6ZpFFOjV6M{S0NFE>
MDA-MB-231 Mly0SpVv[3Srb36gRZN{[Xl? NYP4XmFzPSEQvF2= MmT0NlQhcA>? MVXEUXNQ NUXJXIFDUW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJA2Ow>? MnzHNlU5OzR2MEG=
MCF7 NHT2XlZCeG:ydH;zbZMhSXO|YYm= M4jMVlUh|ryP NGPRXYMzPCCq M2PLW2ROW09? NH;1R3BKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= M3TZVVI2QDN2NECx
MDA-MB-231 MXLBdI9xfG:|aYOgRZN{[Xl? MoL1OUDPxE1? NIHwXm8zPCCq MlLmSG1UVw>? NGHTNndKdmS3Y3XzJIFxd3C2b4TpZ{Bl\WG2aB?= Ml[3NlU5OzR2MEG=
MCF7 NF61TI1HfW6ldHnvckBCe3OjeR?= MXmxJO69VQ>? NVWwbHU5PzJiaB?= NVft[XFuTE2VTx?= M3;ISGlv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= NGq2PWczPTh|NESwNS=>
MDA-MB-231 NYXoSmlLTnWwY4Tpc44hSXO|YYm= M1XGdlEh|ryP M4O3OFczKGh? M2XFT2ROW09? NEPl[llKdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= NYnXb5NqOjV6M{S0NFE>
U-2 OS NVz3RW96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnO5OVAh|ryP NUm1W3RrOjRiaB?= NIDzVWVFVVOR MnzHTWM2OD1zNj62JO69VQ>? MX[yOVc6OjhzMR?=
MG-63 NEHmfZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXu1NEDPxE1? M3LPWFI1KGh? NYnYUXRrTE2VTx?= NF7DOopKSzVyPUmuOUDPxE1? MYCyOVc6OjhzMR?=
U-2 OS MoC4RZBweHSxc3nzJGF{e2G7 MoLqOUDPxE1? NEfkSHAzPCCq NX\6WYp1TE2VTx?= MXzJcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo Mne1NlU4QTJ6MUG=
MG-63 MlvURZBweHSxc3nzJGF{e2G7 MXm1JO69VQ>? MYiyOEBp M4HYVGROW09? NWXC[mN2UW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>? M4r6c|I2Pzl{OEGx
U-2 OS NIrmdFVHfW6ldHnvckBCe3OjeR?= MkLmOUDPxE1? NV;r[ItnOjRiaB?= Mme4SG1UVw>? MUPQdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> M1fzUFI2Pzl{OEGx
MG-63 M3;Oc2Z2dmO2aX;uJGF{e2G7 MYC1JO69VQ>? NIq4cnkzPCCq NETvRpBFVVOR MVLQdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> MoD4NlU4QTJ6MUG=
PANC-1 MofOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWn2UZlSPTBizszN M4\DS|I1KGh? MWTEUXNQ NFLMcnNKSzVyPUeuNUDPxE1? MWmyOVY{OjJ{NR?=
BxPC-3 M17RU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rNZlUxKM7:TR?= Ml\xNlQhcA>? NXO2VJR4TE2VTx?= M2fFc2lEPTB;Nj64JO69VQ>? MlvkNlU3OzJ{MkW=
PANC-1 MXTGeY5kfGmxbjDBd5NigQ>? MX61JO69VQ>? MmeyNlQhcA>? MVTEUXNQ MV\JcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> NYHNZnRyOjV4M{KyNlU>
BxPC-3 Mkf0SpVv[3Srb36gRZN{[Xl? NIXscIk2KM7:TR?= NHu3SZAzPCCq MX3EUXNQ NIjtT2ZKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? NVzrW2xsOjV4M{KyNlU>
PANC-1 NIG3N2pHfW6ldHnvckBCe3OjeR?= NHftN|Y2KM7:TR?= MVGyOEBp NEDpe4dFVVOR MUnJcoR2[2W|IHH1eI9xcGGpaXOgZ4VtdCCmZXH0bC=> M3W0NlI2PjN{MkK1
BxPC-3 NFzPPHpHfW6ldHnvckBCe3OjeR?= NWDJU4xmPSEQvF2= MlK0NlQhcA>? MYTEUXNQ NUjVcI04UW6mdXPld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? NEHRNnkzPTZ|MkKyOS=>
SKOV3 MknwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HMS|ExOCEQvF2= Mny3NlQhcA>? NHzvOGhFVVOR MUHJR|UxRTJyLkS4JO69VQ>? NUPodXM6OjV4MkS3OVA>
OVCAR4 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXrWHkyODBizszN NYTobGg1OjRiaB?= NFLBcWVFVVOR M{j5fGlEPTB;MkKuNVMh|ryP MknrNlU3OjR5NUC=
SKOV3 MXrGeY5kfGmxbjDBd5NigQ>? NWHvUJU1PSEQvF2= M1LvWlczKGh? NGrBbXdFVVOR MnH0TY5lfWOnczDHNk9OKGG{cnXzeC=> NW\t[nVIOjV4MkS3OVA>
OVCAR4 M{nEV2Z2dmO2aX;uJGF{e2G7 M2nVflUh|ryP MWq3NkBp M{fadGROW09? Ml[1TY5lfWOnczDHNk9OKGG{cnXzeC=> NFv5TGczPTZ{NEe1NC=>
SKOV3 M{XQdGFxd3C2b4Ppd{BCe3OjeR?= NFfFTYo2KM7:TR?= Mn;tNlQhcA>? NH3hXW5FVVOR NFHnVJFKdmS3Y3XzJIFxd3C2b4Ppdy=> M3;LRlI2PjJ2N{Ww
OVCAR4 M333TGFxd3C2b4Ppd{BCe3OjeR?= NXLhfWVMPSEQvF2= NVvmfYs{OjRiaB?= MkSySG1UVw>? M1PYVGlv\HWlZYOgZZBweHSxc3nz MXOyOVYzPDd3MB?=
AGS MlHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2r5bVI2KM7:TR?= NVi2[4t2OjRiaB?= NVrBcINLTE2VTx?= MmfuTWM2OD1zOT6wPUDPxE1? NGTITIozPTZyOUmyNy=>
NCI-N78 MlHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37qeVI2KM7:TR?= NWXsVXk6OjRiaB?= MnfpSG1UVw>? NIfMOJBKSzVyPUK2MlM{KM7:TR?= M{HEU|I2PjB7OUKz
AGS M3jrVmFxd3C2b4Ppd{BCe3OjeR?= NYnMNJhwPSEQvF2= NFL2RnczPCCq NXfXU49LTE2VTx?= M3jZbGlv\HWlZYOgZZBweHSxc3nz M2XYflI2PjB7OUKz
NCI-N78 MYHBdI9xfG:|aYOgRZN{[Xl? MlLsOUDPxE1? M4LXUVI1KGh? M1HYNmROW09? MWLJcoR2[2W|IHHwc5B1d3Orcx?= MkjZNlU3ODl7MkO=
AGS MXPGeY5kfGmxbjDBd5NigQ>? MYW1JO69VQ>? M1ruWlI1KGh? MlPOSG1UVw>? M4\X[mlv\HWlZYOgeIhmKGG3dH;wbIFogQ>? NYnscYtQOjV4MEm5NlM>
NCI-N78 NWHqcnZSTnWwY4Tpc44hSXO|YYm= M3PLc|Uh|ryP NWrwcmx[OjRiaB?= M2nadGROW09? NVLWSGhwUW6mdXPld{B1cGViYYX0c5Bp[We7 M1TnZ|I2PjB7OUKz
HSC-3 NVXqN444T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TFelEh|ryP MnjMOFghcA>? Mm\ITWM2OD1yLkW0JO69VQ>? M1\xXlI2OzZ4MUSz
GB30 NYDsR3JrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmxJO69VQ>? MnzqO{Bl NWXtUmtRTE2VTx?= MmnKTWM2OD1yLkCxNUDPxE1? NFiw[3YzPTFyNkSyPC=>
GB9 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;zNUDPxE1? NYDnU4NKPyCm NX;vTY1ITE2VTx?= NXTRZWFtUUN3ME2wMlAzPCEQvF2= NInYO|IzPTFyNkSyPC=>
GB169 NEjVSVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnONUDPxE1? NH;6TlE4KGR? M2HLWmROW09? MX7JR|UxRTBwMEOyJO69VQ>? MoewNlUyODZ2Mki=
T24 NFzOSW9HfW6ldHnvckBCe3OjeR?= M1j2T|Eh|ryP NFHDc4U1QCCq NH7lboNFVVOR NF;IWpNKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NYTiN|VOOjN2MEO2N|M>
RT4 NIPONGZHfW6ldHnvckBCe3OjeR?= M4i3S|Eh|ryP NFH0O2c1QCCq M2f4R2ROW09? MXfJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MmjzNlM1ODN4M{O=
UM-UC-3 NITCW4pHfW6ldHnvckBCe3OjeR?= MUGxJO69VQ>? NWnGPXQzPDhiaB?= NXX0Z3hXTE2VTx?= NFz2ZmpKdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NUDIfFJxOjN2MEO2N|M>
T24 NI\TZ3RCeG:ydH;zbZMhSXO|YYm= MVuzMlE3KM7:TR?= M1G2bFk3KGh? MVfEUXNQ NWjxdZJMUUN3ME2wMlA{ODZizszN Ml;sNlM1ODN4M{O=
RT4 MUXBdI9xfG:|aYOgRZN{[Xl? NXHHXGZnOy5zNjFOwG0> NXLFWI1VQTZiaB?= NVnpcodDTE2VTx?= NU\IXlFSUUN3ME2wMlEyQThizszN MV:yN|QxOzZ|Mx?=
UM-UC-3 MkXuRZBweHSxc3nzJGF{e2G7 MYezMlE3KM7:TR?= MW[5OkBp M2\IO2ROW09? MVPJR|UxRTBwMES0PUDPxE1? Mnv2NlM1ODN4M{O=
OVCAR-5 MnjKSpVv[3Srb36gRZN{[Xl? M4jnV|UxKG6P M{ftXmlvcGmkaYTzJINmdGxibXnndoF1cW:w MlruNlM{OzR|Mke=
SKOV3ip2 NF7FV3NHfW6ldHnvckBCe3OjeR?= NF7jcZU2OCCwTR?= MYPJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NWSzSVVqOjN|M{SzNlc>
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MOLT-4 M4Ww[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHTTHJ1OTBizszN MX:5OkBp M4PKUmlEPTB;MD6wNlYh|ryP M1zld|IxOTB6M{O4
CCRF-CEM MlfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HOVFExKM7:TR?= NH3LR4w6PiCq NWD3T5NWUUN3ME2wMlA6PCEQvF2= NXXX[|dxOjBzMEizN|g>
Kasumi-1 NUn2e5RGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXSxNEDPxE1? MX25OkBp MmfrTWM2OD1yLkGwN{DPxE1? NFjCRYkzODFyOEOzPC=>
Karpas-299 M2rlUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuxNEDPxE1? MYi5OkBp NXHxbnpUUUN3ME2wMlA{QCEQvF2= Mlf6NlAyODh|M{i=
Ramos-RA1 MmLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrkNVAh|ryP MlXNPVYhcA>? M321VGlEPTB;MD6xNlch|ryP Mo\NNlAyODh|M{i=

... 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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