Alisertib (MLN8237) 化学構造
分子量: 518.92

高品質保証

文献中の引用(45)

カスタマーフィードバック(10)

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 NXLJdos1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqwMlUh|ryP MmL3O|IhcA>? NGKzOGdFVVOR NWS3fmhnUUN3ME2wMlA1KM7:TR?= MWOyOlE{PjZ6NB?=
LS174T NVz0T5NHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrLNE42KM7:TR?= NHjxepk4OiCq M2jleWROW09? MYPJR|UxRTBwMEWg{txO MnznNlYyOzZ4OES=
T84 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q0NVAvPSEQvF2= NEHMUmw4OiCq NVLXO|lTTE2VTx?= NEjMPZpKSzVyPUCuNFkh|ryP MlGzNlYyOzZ4OES=
LS180 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHu5TWcxNjVizszN NXPvSIpKPzJiaB?= M{WxZWROW09? M2LhZWlEPTB;MTFOwG0> NVzNb|JXOjZzM{[2PFQ>
SW948 NV;Vdpk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGj4OFAxNjVizszN MnfnO|IhcA>? M1PkOWROW09? MYPJR|UxRTFizszN NGrpPVIzPjF|Nk[4OC=>
HCT15 MmT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVywMlUh|ryP NXjhPVRpPzJiaB?= NXfsOYVCTE2VTx?= NYDPS|IxUUN3MEywMlQh|ryP NEjIN3YzPjF|Nk[4OC=>
DLD-1 NUDTZ2pHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGK2OoExNjVizszN NWr1V|NvPzJiaB?= MVnEUXNQ NXSzNGsyUUN3MEywMlgh|ryP MXqyOlE{PjZ6NB?=
MIP-101 MlTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrFNE42KM7:TR?= MkPXO|IhcA>? NHjvUZJFVVOR MXzJR|UxRTFizszN MnXjNlYyOzZ4OES=
SNU1544 NF;5[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWwMlUh|ryP MWm3NkBp MV;EUXNQ NXTD[oNmUUN3ME2xJO69VQ>? NHvJOm4zPjF|Nk[4OC=>
OCI-Ly10 NXe5OG15S3m2b4TvfIlkKEG|c3H5 MoLlO|IhcA>? MlK1SG1UVw>? MXHJR|UxRTBwMEW4JO69VQ>? NGHWb3gzPTh5OEOzNS=>
SU-DHL2 MV7DfZRwfG:6aXOgRZN{[Xl? Mn7kO|IhcA>? NEDvTplFVVOR NHfzWm5KSzVyPUCuNFEh|ryP NYjuSYhHOjV6N{izN|E>
OCI-LY7 M3;v[2N6fG:2b4jpZ{BCe3OjeR?= NWLpU402PzJiaB?= NWTXSmNxTE2VTx?= MofETWM2OD1yLkC4NUDPxE1? NWDLZYJ3OjV6N{izN|E>
SU-DHL6 MoftR5l1d3SxeHnjJGF{e2G7 NXO0WZpnPzJiaB?= MV7EUXNQ Mlv6TWM2OD1yLkS4NkDPxE1? MXWyOVg4QDN|MR?=
Jeko-1 M33p[2N6fG:2b4jpZ{BCe3OjeR?= NH3QUJQ4OiCq MkDHSG1UVw>? NX\3coNFUUN3ME2wMlAzQSEQvF2= NEnSbpMzPTh5OEOzNS=>
JVM-2 MlHHR5l1d3SxeHnjJGF{e2G7 M3LaWVczKGh? MX;EUXNQ MYDJR|UxRTBwMEGg{txO MoO4NlU5Pzh|M{G=
Rec-1 NEPVdo9EgXSxdH;4bYMhSXO|YYm= NWfMZmR[PzJiaB?= MoXuSG1UVw>? NHX6UZFKSzVyPUCuNFg4KM7:TR?= Ml76NlU5Pzh|M{G=
Z-138 NVXjTJZjS3m2b4TvfIlkKEG|c3H5 M{XGdFczKGh? M2DPUGROW09? MU\JR|UxRTBwMEGzJO69VQ>? Mkj5NlU5Pzh|M{G=
H9 M3jafGN6fG:2b4jpZ{BCe3OjeR?= NXfnVpl7PzJiaB?= MmT4SG1UVw>? MXfJR|UxRTBwNjFOwG0> M2fJVVI2QDd6M{Ox
HH M3jYU2N6fG:2b4jpZ{BCe3OjeR?= MXK3NkBp Ml:ySG1UVw>? NUSxPHRFUUN3ME2wMlch|ryP Mnv4NlU5Pzh|M{G=
DND41 MmHTR5l1d3SxeHnjJGF{e2G7 M2XWOFczKGh? MXHEUXNQ NX7YRmprUUN3ME2wMlEh|ryP MWKyOVg4QDN|MR?=
CCL119 MkWzR5l1d3SxeHnjJGF{e2G7 NUH4WpVUPzJiaB?= Mn\FSG1UVw>? MWHJR|UxRTBwME[yJO69VQ>? NHLLO3IzPTh5OEOzNS=>
J.Cam 1.6 MU\DfZRwfG:6aXOgRZN{[Xl? NFfsdnU4OiCq MWnEUXNQ MWTJR|UxRTBwMUC1JO69VQ>? Ml3RNlU5Pzh|M{G=
Sup-T1 MYTDfZRwfG:6aXOgRZN{[Xl? M1;OTVczKGh? MnLkSG1UVw>? Mli5TWM2OD1{LkG0NkDPxE1? MYCyOVg4QDN|MR?=
Tib 152 NGLURZNEgXSxdH;4bYMhSXO|YYm= M4P1R|czKGh? NUK1fFNvTE2VTx?= NF\lc5FKSzVyPUCuPEDPxE1? MVOyOVg4QDN|MR?=
MCF7 NIDvTHNHfW6ldHnvckBCe3OjeR?= Ml\6OUDPxE1? MnPGNlQhcA>? M3nYfWROW09? NVT6dHlwUW6mdXPld{BIOi:PIHHydoV{fA>? NVexcWd6OjV6M{S0NFE>
MDA-MB-231 M{LuTGZ2dmO2aX;uJGF{e2G7 NIrNfVU2KM7:TR?= NETtelAzPCCq MnPJSG1UVw>? M1TiXGlv\HWlZYOgS|MwVSCjcoLld5Q> MoPYNlU5OzR2MEG=
MCF7 MWLGeY5kfGmxbjDBd5NigQ>? MlTWOUDPxE1? M3vwUFI1KGh? M4jhcGROW09? M17xWmRm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsyN0OGQ{K= M3L5eFI2QDN2NECx
MCF7 NY[yVHJGTnWwY4Tpc44hSXO|YYm= NIn5eZU2KM7:TR?= MonmNlQhcA>? NF;yfWtFVVOR NXHBR491TGWlcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? MUKyOVg{PDRyMR?=
MCF7 M{XWU2Z2dmO2aX;uJGF{e2G7 M4H0XlUh|ryP NWTEfmpsOjRiaB?= MXjEUXNQ MXLE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiY4njcIlvKEJz M4\KRlI2QDN2NECx
MCF7 M4TIXWZ2dmO2aX;uJGF{e2G7 NWrYclBkPSEQvF2= MV2yOEBp M4XuVGROW09? NXO4XpU5UW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJJAzOSCZYX[xM2NqeDF? NFHNS2IzPTh|NESwNS=>
MCF7 M4jDS2Z2dmO2aX;uJGF{e2G7 NUnK[YpWPSEQvF2= MnPYNlQhcA>? M{XmTmROW09? M{D0Xmlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= NFiwSHUzPTh|NESwNS=>
MDA-MB-231 NH3CT2dHfW6ldHnvckBCe3OjeR?= NEnYNFg2KM7:TR?= M{D3SFI1KGh? M{\OVWROW09? NF7wd4dF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOS:FRFOy MlLPNlU5OzR2MEG=
MDA-MB-231 NHrue3NHfW6ldHnvckBCe3OjeR?= NXLScnZwOSEQvF2= NXrWemtZOjRiaB?= NGDieWVFVVOR NYLtXmJ5UW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mJGNFUzJ? NIHTTpYzPTh|NESwNS=>
MDA-MB-231 MYfGeY5kfGmxbjDBd5NigQ>? MW[1JO69VQ>? M2PxVVI1KGh? MoWwSG1UVw>? MnHKSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIHP5Z4xqdiCEMR?= MorUNlU5OzR2MEG=
MDA-MB-231 MlvBSpVv[3Srb36gRZN{[Xl? MVu1JO69VQ>? M{jwNVI1KGh? NHLRSJJFVVOR M4fWRWlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlEhX2GoMT;DbZAy MV[yOVg{PDRyMR?=
MDA-MB-231 NGO5TopHfW6ldHnvckBCe3OjeR?= MV61JO69VQ>? MmrrNlQhcA>? NWDufW17TE2VTx?= M2G4Z2lv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= MUmyOVg{PDRyMR?=
MDA-MB-231 NEPKPVJHfW6ldHnvckBCe3OjeR?= M4T3XFUh|ryP Ml;KNlQhcA>? MYfEUXNQ NFrxbGtKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gdFU{ NEPZV20zPTh|NESwNS=>
MCF7 NEjiXlhCeG:ydH;zbZMhSXO|YYm= Mkf6OUDPxE1? NXn1S4hCOjRiaB?= NVzhWVZHTE2VTx?= M3nlbmlv\HWlZYOgZZBweHSxdHnjJIRm[XSq MWCyOVg{PDRyMR?=
MDA-MB-231 NYn4d5VXSXCxcITvd4l{KEG|c3H5 NVLtSWVrPSEQvF2= M2\iNlI1KGh? NG\1NoJFVVOR NXrwbWNSUW6mdXPld{BieG:ydH;0bYMh\GWjdHi= MWSyOVg{PDRyMR?=
MCF7 NE\vOZVHfW6ldHnvckBCe3OjeR?= MU[xJO69VQ>? MY[3NkBp M3npZ2ROW09? M{C1R2lv\HWlZYOgZZV1d3CqYXfpZ{Bl\WG2aB?= M1rOclI2QDN2NECx
MDA-MB-231 MYHGeY5kfGmxbjDBd5NigQ>? Ml34NUDPxE1? MXi3NkBp MlTXSG1UVw>? MXrJcoR2[2W|IHH1eI9xcGGpaXOg[IVifGh? Ml;pNlU5OzR2MEG=
U-2 OS NYH5TpA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVO1NEDPxE1? NFfGeIMzPCCq Mo[ySG1UVw>? MmjZTWM2OD1zNj62JO69VQ>? NXLNVVZIOjV5OUK4NVE>
MG-63 NF3CRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXxeZJUPTBizszN NX;lfZZ[OjRiaB?= NVy4fHVuTE2VTx?= M13OUmlEPTB;OT61JO69VQ>? MnGzNlU4QTJ6MUG=
U-2 OS M4\aU2Fxd3C2b4Ppd{BCe3OjeR?= NVnx[lN7PSEQvF2= NWnSWoRpOjRiaB?= NET2R|RFVVOR MUfJcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo MVeyOVc6OjhzMR?=
MG-63 NUK1NWhRSXCxcITvd4l{KEG|c3H5 NIjHSXc2KM7:TR?= NXPPUpN2OjRiaB?= NE\Dc5BFVVOR M2\2eWlv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> NIf1dVIzPTd7MkixNS=>
U-2 OS NHfDVYZHfW6ldHnvckBCe3OjeR?= MX21JO69VQ>? MnzzNlQhcA>? NXLjPVViTE2VTx?= MU\Qdo9ud3SnczDheZRweGijZ3njJINmdGxiZHXheIg> M1vNZ|I2Pzl{OEGx
MG-63 M1zhdmZ2dmO2aX;uJGF{e2G7 MlrZOUDPxE1? M3LzN|I1KGh? NGDUTmtFVVOR M3n6[HBzd22xdHXzJIF2fG:yaHHnbYMh[2WubDDk[YF1cA>? NWHGenBSOjV5OUK4NVE>
PANC-1 M3fod2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX21NEDPxE1? M{DWflI1KGh? NY\ITmdqTE2VTx?= MVzJR|UxRTdwMTFOwG0> MknmNlU3OzJ{MkW=
BxPC-3 Mon5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLwU4Q2OCEQvF2= NGDuZ3gzPCCq NF36V41FVVOR NVO5Zpc2UUN3ME22Mlgh|ryP M2jVXlI2PjN{MkK1
PANC-1 NGDpc4NHfW6ldHnvckBCe3OjeR?= NVSye2N1PSEQvF2= MnLPNlQhcA>? NFjLc4RFVVOR MlriTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDpckBIOi:PIIDoZZNm MXmyOVY{OjJ{NR?=
BxPC-3 MoCwSpVv[3Srb36gRZN{[Xl? NWXsfGZyPSEQvF2= NFHKSnEzPCCq MoXaSG1UVw>? NEjH[W5KdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIlvKEd{L12gdIhie2V? M37FTVI2PjN{MkK1
PANC-1 Mn7pSpVv[3Srb36gRZN{[Xl? NHnEOGU2KM7:TR?= Mm\BNlQhcA>? M3jOdGROW09? MkPhTY5lfWOnczDheZRweGijZ3njJINmdGxiZHXheIg> MVSyOVY{OjJ{NR?=
BxPC-3 MojQSpVv[3Srb36gRZN{[Xl? MmCxOUDPxE1? NVXkSHZxOjRiaB?= M37sdWROW09? MoTFTY5lfWOnczDheZRweGijZ3njJINmdGxiZHXheIg> M{XMc|I2PjN{MkK1
SKOV3 NFTrToNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[xNFAh|ryP MmroNlQhcA>? NIjRR4tFVVOR NI\K[IRKSzVyPUKwMlQ5KM7:TR?= NFHXPHczPTZ{NEe1NC=>
OVCAR4 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxNFAh|ryP NIH2O3czPCCq MXPEUXNQ NVfjOVNJUUN3ME2yNk4yOyEQvF2= NWrnXlZFOjV4MkS3OVA>
SKOV3 NWHzbWwxTnWwY4Tpc44hSXO|YYm= NG\MSpU2KM7:TR?= NV3xNoRoPzJiaB?= M4P2eGROW09? NFj1V25KdmS3Y3XzJGczN01iYYLy[ZN1 NX7aRVJMOjV4MkS3OVA>
OVCAR4 MYjGeY5kfGmxbjDBd5NigQ>? Mm\OOUDPxE1? NWr5b2o5PzJiaB?= MlTZSG1UVw>? M{LiUGlv\HWlZYOgS|IwVSCjcoLld5Q> MonENlU3OjR5NUC=
SKOV3 NHHreGNCeG:ydH;zbZMhSXO|YYm= M{DKeVUh|ryP M{L0elI1KGh? M{C3dmROW09? NHjwR3NKdmS3Y3XzJIFxd3C2b4Ppdy=> NXTWOYVYOjV4MkS3OVA>
OVCAR4 M1[5PGFxd3C2b4Ppd{BCe3OjeR?= NXjX[5dkPSEQvF2= NGfDXHczPCCq MVfEUXNQ NEPtU2hKdmS3Y3XzJIFxd3C2b4Ppdy=> Mof4NlU3OjR5NUC=
AGS M1vCeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fJXFI2KM7:TR?= NXvYWno2OjRiaB?= MnrlSG1UVw>? M4PmcWlEPTB;MUmuNFkh|ryP NUPIfGpOOjV4MEm5NlM>
NCI-N78 MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrpNlUh|ryP MlzyNlQhcA>? NFvTdZVFVVOR MYnJR|UxRTJ4LkOzJO69VQ>? MojqNlU3ODl7MkO=
AGS MlHBRZBweHSxc3nzJGF{e2G7 NXTBPZhrPSEQvF2= MVKyOEBp NULaSJpoTE2VTx?= M1zRfmlv\HWlZYOgZZBweHSxc3nz MUiyOVYxQTl{Mx?=
NCI-N78 NYLrcZllSXCxcITvd4l{KEG|c3H5 NV:1ZVNFPSEQvF2= MWKyOEBp NIfFcFVFVVOR NVjhSlE{UW6mdXPld{BieG:ydH;zbZM> NIizcIszPTZyOUmyNy=>
AGS MWjGeY5kfGmxbjDBd5NigQ>? MniyOUDPxE1? NV\y[mk6OjRiaB?= NVTiOHl[TE2VTx?= NHXMTGFKdmS3Y3XzJJRp\SCjdYTvdIhi\3l? NGnQV|kzPTZyOUmyNy=>
NCI-N78 M4DqWmZ2dmO2aX;uJGF{e2G7 NFLxZVY2KM7:TR?= MkjwNlQhcA>? NHnwUHNFVVOR NGWyWodKdmS3Y3XzJJRp\SCjdYTvdIhi\3l? NU\Feo1GOjV4MEm5NlM>
HSC-3 NGH2c3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\TNUDPxE1? M160UlQ5KGh? NIT0WJJKSzVyPUCuOVQh|ryP NVnoNZplOjV|Nk[xOFM>
GB30 MoKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TnUFEh|ryP MlHJO{Bl NYq5RZZpTE2VTx?= M3rUUmlEPTB;MD6wNVEh|ryP NFrvO|AzPTFyNkSyPC=>
GB9 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4mxSlEh|ryP MUe3JIQ> NVTJfXJiTE2VTx?= M4j4O2lEPTB;MD6wNlQh|ryP MWCyOVExPjR{OB?=
GB169 NGXNbFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17N[|Eh|ryP MVG3JIQ> NH34cJNFVVOR NXH6XVdbUUN3ME2wMlA{OiEQvF2= NVPHUlVzOjVzME[0Nlg>
T24 NF;IPZhHfW6ldHnvckBCe3OjeR?= M2HlPFEh|ryP NUT1XHM4PDhiaB?= M1HjUWROW09? MkfZTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MXeyN|QxOzZ|Mx?=
RT4 M3H1dWZ2dmO2aX;uJGF{e2G7 NHn2bmwyKM7:TR?= NFf2TYw1QCCq MWTEUXNQ M4HTVmlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NFPze20zOzRyM{[zNy=>
UM-UC-3 MmXtSpVv[3Srb36gRZN{[Xl? NFuwTGgyKM7:TR?= MorzOFghcA>? MYrEUXNQ MVHJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NV3ZeHd5OjN2MEO2N|M>
T24 MnXXRZBweHSxc3nzJGF{e2G7 M{PxNVMvOTZizszN MV25OkBp MVjEUXNQ Ml;WTWM2OD1yLkCzNFYh|ryP MonaNlM1ODN4M{O=
RT4 M3r3WWFxd3C2b4Ppd{BCe3OjeR?= NV\rU2xqOy5zNjFOwG0> MVy5OkBp NGj2[HpFVVOR NV3pcZdwUUN3ME2wMlEyQThizszN NYPwOYNxOjN2MEO2N|M>
UM-UC-3 MXTBdI9xfG:|aYOgRZN{[Xl? NXH4NFZHOy5zNjFOwG0> M3G0bFk3KGh? NHWxO|NFVVOR NWPHfGdCUUN3ME2wMlA1PDlizszN NGfXcW4zOzRyM{[zNy=>
OVCAR-5 NIqyVGRHfW6ldHnvckBCe3OjeR?= MXq1NEBvVQ>? NXjmXWRCUW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NWjsWnkyOjN|M{SzNlc>
SKOV3ip2 NX\OTllkTnWwY4Tpc44hSXO|YYm= MXy1NEBvVQ>? MWnJcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NWf4c4pFOjN|M{SzNlc>
S462 NGPvS2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYixNFAh|ryP NGPzeZo4OiCq M33ZU2ROW09? MVzBeJRmdnWjdHXzJINmdGxiZ4Lve5Rp NI\5d40zOzN{OEGxOC=>
2884 M{jMc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3QNVAxKM7:TR?= NVXH[lJ2PzJiaB?= M4fWOWROW09? MYHBeJRmdnWjdHXzJINmdGxiZ4Lve5Rp NH61[I0zOzN{OEGxOC=>
2885 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmxNFAh|ryP NFjNW|E4OiCq M{DDbWROW09? M{PPfmF1fGWwdXH0[ZMh[2WubDDndo94fGh? M4\HN|I{OzJ6MUG0
CRL-2396 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\Xfo0yODBizszN MWP3ZZRmeg>? Mk\iTWM2OD1yLkC5NkDPxE1? MUKyN|E2OzV{NB?=
TIB-48 NUHQXZZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;mbFl3OTByIN88US=> NX7J[Xc1f2G2ZYK= NVvUemF4UUN3ME2wMlA5QCEQvF2= NVjvV25XOjNzNUO1NlQ>
CRL-2396 NVfjNmY{S3m2b4TvfIlkKEG|c3H5 MmLGNUDPxE1? M{LFSFQ5KGh? NEOxXGt4[XSnch?= MlS1TY5lfWOnczDhdI9xfG:|aYO= NEjkd3czOzF3M{WyOC=>
TIB-48 NHLINnhEgXSxdH;4bYMhSXO|YYm= NEjPPXkyKM7:TR?= MnL6OFghcA>? MXT3ZZRmeg>? MULJcoR2[2W|IHHwc5B1d3Orcx?= MWCyN|E2OzV{NB?=
AGS M3Tk[GN6fG:2b4jpZ{BCe3OjeR?= NF3vOGwxNjVizszN MnrJNlQhcA>? M4DpbmROW09? MonXSIVkemWjc3XzJINmdGxic4Xyeol3[Wx? MYiyNlk4OjZzMR?=
FLO-1 MX3DfZRwfG:6aXOgRZN{[Xl? M{G1V|AvPSEQvF2= M1Tkb|I1KGh? MVfEUXNQ Ml;MSIVkemWjc3XzJINmdGxic4Xyeol3[Wx? MlzDNlI6PzJ4MUG=
OE33 NW[5[XNmS3m2b4TvfIlkKEG|c3H5 MWiwMlUh|ryP MUCyOEBp M{izSGROW09? MlL1SIVkemWjc3XzJINmdGxic4Xyeol3[Wx? MkPXNlI6PzJ4MUG=
SKLMS MoPjR5l1d3SxeHnjJGF{e2G7 MVS3OUBvVQ>? MYe5OkBp M2LYeWlv\HWlZYOgZZBweHSxc3nz NIWxfoszOjh{MUm5Oy=>
Leio285 MUPDfZRwfG:6aXOgRZN{[Xl? MljmO|Uhdk1? M{XkdVk3KGh? NEXvZVJKdmS3Y3XzJIFxd3C2b4Ppdy=> NG\tZpAzOjh{MUm5Oy=>
Mes-Sa NIK1bVBEgXSxdH;4bYMhSXO|YYm= NGXETY84PSCwTR?= NUXrS2FsQTZiaB?= NGDjWG1KdmS3Y3XzJIFxd3C2b4Ppdy=> NFfGS5EzOjh{MUm5Oy=>
DAOY M3LU[2N6fG:2b4jpZ{BCe3OjeR?= MoG4NVAh|ryP M4n5XVczKGh? M33vTmROW09? MXLJR|UxRTBwMESg{txO NHjjc3MzOjZ4OUOzOS=>
IMR32 NVHjZ2t4S3m2b4TvfIlkKEG|c3H5 MUixNEDPxE1? NGP2cXU4OiCq MX3EUXNQ M1nHWWlEPTB;MD6wN{DPxE1? MY[yNlY3QTN|NR?=
Molt-4 Mn\6R5l1d3SxeHnjJGF{e2G7 Ml[3NVAh|ryP Ml21O|IhcA>? M2HPS2ROW09? MmrxTWM2OD1yLkCyJO69VQ>? MYeyNlY3QTN|NR?=
MOLM-13 NWXHUHE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrZd5ZKOyEQvF2= MlrGO|IhcA>? M4rkVWRqdWmwaYPo[ZMh[2WubDD2bYFjcWyrdIm= MkLFNlI1QDh{NEm=
HL-60 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXn5[FRyOyEQvF2= NYDydmRGPzJiaB?= MkjuSIlucW6rc3jld{Bk\WyuII\pZYJqdGm2eR?= Mk\HNlI1QDh{NEm=
MV4-11 NH7NVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4m2bVMh|ryP M3vkNFczKGh? NIjZXXJFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5 MUeyNlQ5QDJ2OR?=
SKM-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HUelMh|ryP MmHwO|IhcA>? NHKxNplFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5 MX:yNlQ5QDJ2OR?=
SH2 M1L1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfqVZh4OyEQvF2= M3nOUVczKGh? MU\EbY1qdmm|aHXzJINmdGxidnnhZoltcXS7 MYKyNlQ5QDJ2OR?=
NOMO-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\zXHY{KM7:TR?= NXXtNGVZPzJiaB?= MYjEbY1qdmm|aHXzJINmdGxidnnhZoltcXS7 M2TzfVIzPDh6MkS5
OCL-AML2 NUSxbpJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHZN{DPxE1? M3nmT|czKGh? MYnEbY1qdmm|aHXzJINmdGxidnnhZoltcXS7 NXTx[|FiOjJ2OEiyOFk>
PL-21 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXezJO69VQ>? MU[3NkBp M{G3[mRqdWmwaYPo[ZMh[2WubDD2bYFjcWyrdIm= M4jRZVIzPDh6MkS5
KG-1 NHrFUGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIn5PI8{KM7:TR?= MlfDO|IhcA>? M4nUWGRqdWmwaYPo[ZMh[2WubDD2bYFjcWyrdIm= MXKyNlQ5QDJ2OR?=
A172 Mmm0R5l1d3SxeHnjJGF{e2G7 NInjVpIyODBizszN MmHPNlQhcA>? NWPHOYVXTE2VTx?= MXTJR|UxRTBwMUKwJO69VQ>? Mn\oNlIzPzR|OUm=
U87 MmTQR5l1d3SxeHnjJGF{e2G7 MXWxNFAh|ryP NGnwTZAzPCCq MYTEUXNQ NUTOOlRLUUN3ME2wMlExPSEQvF2= NX;zcVRlOjJ{N{SzPVk>
U251 M4fBO2N6fG:2b4jpZ{BCe3OjeR?= MX[xNFAh|ryP Ml7mNlQhcA>? MorSSG1UVw>? MXnJR|UxRTBwMUCwJO69VQ>? MWKyNlI4PDN7OR?=
T98 MYfDfZRwfG:6aXOgRZN{[Xl? MXKxNFAh|ryP MXyyOEBp M3Tw[mROW09? Mlz2TWM2OD1yLkGyOUDPxE1? NV;YS4tGOjJ{N{SzPVk>
LN18 M1r5NGN6fG:2b4jpZ{BCe3OjeR?= M2LVWFExOCEQvF2= NHf6N5gzPCCq M3PFSGROW09? MVXJR|UxRTBwMkGwJO69VQ>? NEDxfJMzOjJ5NEO5PS=>
LN443 MoPTR5l1d3SxeHnjJGF{e2G7 NILHd|kyODBizszN NUj1[oRLOjRiaB?= NWD6ZopHTE2VTx?= NWHlO4gyUUN3ME2wMlIzOCEQvF2= M1fDO|IzOjd2M{m5
HF66 NWTwSXFOS3m2b4TvfIlkKEG|c3H5 NHG1XJUyODBizszN MWSyOEBp NI[xZ2xFVVOR NV7S[3NqUUN3ME2wMlIzPSEQvF2= M1LON|IzOjd2M{m5
HF2303 M2LGc2N6fG:2b4jpZ{BCe3OjeR?= NGr5WFIyODBizszN MnvlNlQhcA>? MkjLSG1UVw>? NUHuWlBxUUN3ME2wMlA3OCEQvF2= M2C2UlIzOjd2M{m5
HF2359 M1m1cGN6fG:2b4jpZ{BCe3OjeR?= MU[xNFAh|ryP NYH5TGhqOjRiaB?= NGTwUnhFVVOR NXj2c4o4UUN3ME2wMlA3OCEQvF2= MlXxNlIzPzR|OUm=
HF2414 M2HxbWN6fG:2b4jpZ{BCe3OjeR?= NG\jT5UyODBizszN MlTzNlQhcA>? MVrEUXNQ MYjJR|UxRTBwMEiwJO69VQ>? M16ze|IzOjd2M{m5
A-673 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;KbXZuOTBizszN MoLaPVYhcA>? Mm[3SG1UVw>? MnLtTWM2OD1yLkCzNkDPxE1? M4PpeFIyPDR6NUmx
TC-32 NG\2RWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn1dYhPOTBizszN MXm5OkBp M3PKWWROW09? NVfUdpZKUUN3ME2wMlA{QSEQvF2= MV6yNVQ1QDV7MR?=
TC-71 Mo[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfrNJoyOCEQvF2= M4m1PVk3KGh? NVrW[5l{TE2VTx?= NGrjflBKSzVyPUCuNVAzKM7:TR?= NHz5ZokzOTR2OEW5NS=>
SK-N-MC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3GwS|ExKM7:TR?= MXO5OkBp M3i4ZmROW09? MmTTTWM2OD1yLkC3NkDPxE1? MVqyNVQ1QDV7MR?=
CHLA-9 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\tdlExKM7:TR?= NFzBe4o6PiCq NHruTGJFVVOR NHz4W5pKSzVyPUCuNFE5KM7:TR?= M1\qeFIyPDR6NUmx
CHLA-10 NYL2SnpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLRNVAh|ryP MmXMPVYhcA>? NGn0PItFVVOR NEW0W3dKSzVyPUCuNFYxKM7:TR?= NETsOlgzOTR2OEW5NS=>
CHLA-25 MkS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\5U|ExKM7:TR?= NHn4bo46PiCq NF\UR45FVVOR MUfJR|UxRTBwMU[4JO69VQ>? MXqyNVQ1QDV7MR?=
CHLA-32 NHjw[lFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3CSpJFOTBizszN M2XxOVk3KGh? MYfEUXNQ MmTFTWM2OD1yLkGzOkDPxE1? NX\IeZBQOjF2NEi1PVE>
CHLA-56 M1fBcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13TR|ExKM7:TR?= NHn5PYE6PiCq NGjWdW9FVVOR M3rBR2lEPTB;MUCg{txO NV;2bnhsOjF2NEi1PVE>
CHLA-258 NGW4WYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnXTnQyOCEQvF2= MVy5OkBp M1PzSWROW09? MVLJR|UxRTBwMUOyJO69VQ>? MUiyNVQ1QDV7MR?=
COG-E-352 NFrrSGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWOwO5FKOTBizszN MWO5OkBp MlXuSG1UVw>? M4H0XGlEPTB;MD6wOFMh|ryP NHnt[Y0zOTR2OEW5NS=>
CHLA-90 M4nTVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUSxNEDPxE1? MlPQPVYhcA>? NGX4eoZFVVOR MYfJR|UxRTBwME[xJO69VQ>? NHHh[W0zOTR2OEW5NS=>
CHLA-119 MlXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDGNVAh|ryP MUi5OkBp M3z3WGROW09? NVrrS|RYUUN3ME2wMlAzOiEQvF2= NUDJUo9VOjF2NEi1PVE>
CHLA-122 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\USZMyOCEQvF2= NX;RfYhlQTZiaB?= MmnLSG1UVw>? NV[1cGdEUUN3ME2wMlAyQSEQvF2= MlTyNlE1PDh3OUG=
CHLA-136 NYruOHBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zJRVExKM7:TR?= MVe5OkBp MWTEUXNQ NWfPVo9iUUN3ME2wMlA{QSEQvF2= MVGyNVQ1QDV7MR?=
CHLA-140 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfCNINkOTBizszN M{ixUVk3KGh? NES5bWhFVVOR MljRTWM2OD1yLkCyOkDPxE1? NWrSPG1FOjF2NEi1PVE>
LA-N-6 NXS4O3kzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r1eVExKM7:TR?= NVfUVXFXQTZiaB?= NXLUWFM{TE2VTx?= MnvKTWM2OD1yLkC1OEDPxE1? MV[yNVQ1QDV7MR?=
NB-1643 NUjBOHd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnUfnIyOCEQvF2= MkjvPVYhcA>? NHHySphFVVOR M2jNWWlEPTB;MD6wN|ch|ryP MUGyNVQ1QDV7MR?=
NB-EBc1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TDVVExKM7:TR?= MYO5OkBp NFvEVpJFVVOR M3zVOWlEPTB;MD6wOVAh|ryP MmXPNlE1PDh3OUG=
SK-N-BE-1 NYXhdVRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrSNVAh|ryP MlixPVYhcA>? NEPMTY1FVVOR NYjvS4JEUUN3ME2wMlAzQCEQvF2= M1q1RVIyPDR6NUmx
SK-N-BE-2 NIjuW5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfZO2EyOCEQvF2= MY[5OkBp M3;v[mROW09? MmC3TWM2OD1yLkCzOkDPxE1? Mn\NNlE1PDh3OUG=
SMS-KAN NWOxdHVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInkXWgyOCEQvF2= NHOwUIM6PiCq M1PsZmROW09? NIfI[nNKSzVyPUCuNFM1KM7:TR?= NXfFPIVXOjF2NEi1PVE>
SMS-KANR M2rWdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxNEDPxE1? NGq2VZc6PiCq M1PBSGROW09? MUPJR|UxRTBwMEK2JO69VQ>? MlTuNlE1PDh3OUG=
SMS-KCN NFLabGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVGxNEDPxE1? MWe5OkBp NXXCUZN3TE2VTx?= M2rLd2lEPTB;MD6wNVkh|ryP NVi0VI0{OjF2NEi1PVE>
SMS-KCNR M3\ae2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1[wclExKM7:TR?= M3XBZVk3KGh? NUfTR5FpTE2VTx?= M3HlWGlEPTB;MD6wNVAh|ryP MnPRNlE1PDh3OUG=
SMS-LHN M1TDSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYixNEDPxE1? MX[5OkBp MXLEUXNQ M3zSS2lEPTB;MD6wN|Ih|ryP NV31cldUOjF2NEi1PVE>
SMS-MSN MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HJdlExKM7:TR?= M{Kz[|k3KGh? NX;PVVBvTE2VTx?= MVLJR|UxRTBwMEKyJO69VQ>? M1PrOFIyPDR6NUmx
SMS-SAN NGnXUWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTONVAh|ryP MXS5OkBp MkHOSG1UVw>? NWnnXXp4UUN3ME2wMlAzOCEQvF2= M1TLPFIyPDR6NUmx
Granta-4 NUfiUWNrS3m2b4TvfIlkKEG|c3H5 MYqxNEDPxE1? MmjvO{Bl MVHJR|UxRTBwMESwJO69VQ>? M3\jSVIyOjlzOE[3
DB NIX0SmFEgXSxdH;4bYMhSXO|YYm= MVGxNEDPxE1? M2LDPVch\A>? NGPESYZKSzVyPUCuNFQzKM7:TR?= NXqyXmY{OjF{OUG4Olc>
RL NXLRWIRGS3m2b4TvfIlkKEG|c3H5 MoLBNVAh|ryP NYn2PFF{PyCm MlvFTWM2OD1yLkCxOUDPxE1? MX2yNVI6OTh4Nx?=
K562 NFvkV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWxNEDPxE1? NYLScHJGQTZiaB?= MXzJR|UxRTBwMEi3JO69VQ>? M1;jdlIyODlzNkOz
LAMA-84 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojSNVAh|ryP NV7LcJp4QTZiaB?= NITWNWJKSzVyPUCuNFU4KM7:TR?= MYCyNVA6OTZ|Mx?=
MM15 MnX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:0JO69VQ>? MknkO|IhcA>? MnWySG1UVw>? MYXJR|UxRTBwMUOg{txO MlGxNlA{QDJ6NES=
OPM1 NFnEfm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfUNYU1KM7:TR?= MYG3NkBp MUHEUXNQ Mn3sTWM2OD1yLkCzJO69VQ>? M{PxTlIxOzh{OES0
RPM1 NXXENIVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvtVoc1KM7:TR?= M1[wNVczKGh? MmnZSG1UVw>? MYPJR|UxRTFyLkOyJO69VQ>? MnTyNlA{QDJ6NES=
INA6 MmXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zuXlQh|ryP MVO3NkBp M1r4XmROW09? NFTNVHVKSzVyPUCuNFAzKM7:TR?= MlnaNlA{QDJ6NES=
OPM2 NGnYcYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlq1OEDPxE1? Mm\HO|IhcA>? MnP6SG1UVw>? MWnJR|UxRTRwM{eg{txO M33t[VIxOzh{OES0
MM1R M1LscGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHVcVU1KM7:TR?= MnPwO|IhcA>? NITvTYVFVVOR M37qe2lEPTB;MT62PEDPxE1? NUTyN5JUOjB|OEK4OFQ>
DOX40 NEXRSlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfTOEDPxE1? MYe3NkBp MlPjSG1UVw>? NYG5c3lLUUN3ME21MlQ5KM7:TR?= MUCyNFM5Ojh2NB?=
LR5 MoXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj5TppQPCEQvF2= MUm3NkBp M2HZdWROW09? MWLJR|UxRTJwNUOg{txO MmrTNlA{QDJ6NES=
U266 NXPLcm1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2K5clQh|ryP NELZU4w4OiCq MkDMSG1UVw>? M1e0eGlEPTB;MT60N{DPxE1? MYqyNFM5Ojh2NB?=
RD NF\yfWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXOOGEyOCEQvF2= NWfi[oRWQTZiaB?= M1rhc2lEPTB;MD6yNlgh|ryP M{K0OFIxOTB6M{O4
Rh41 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\SSXoyOCEQvF2= M1\GZ|k3KGh? NGXtdVdKSzVyPUCuNFkxKM7:TR?= MYOyNFExQDN|OB?=
Rh30 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fWVlExKM7:TR?= M{jkNVk3KGh? NWj5XYpQUUN3ME2wMlI{OCEQvF2= MYeyNFExQDN|OB?=
BT-12 NFXzTpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzidmNUOTBizszN NGXEVFg6PiCq NGTDSJVKSzVyPUCuNFYxKM7:TR?= NHvEV5YzODFyOEOzPC=>
CHLA-266 NIH4O4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHXTYwyOCEQvF2= Mm[5PVYhcA>? M{f2TGlEPTB;MD6wO|Ih|ryP NUDpU|VVOjBzMEizN|g>
TC-71 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUixNEDPxE1? MlvuPVYhcA>? M{jtc2lEPTB;MD6xNFIh|ryP NYfSR41lOjBzMEizN|g>
SJ-GBM2 NYDOZlc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LrN|ExKM7:TR?= MUi5OkBp Mo\pTWM2OD1yLkC1NEDPxE1? M32wU|IxOTB6M{O4
NALM-6 NEjGc3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIS3WocyOCEQvF2= NXzFTJY1QTZiaB?= NITpVW1KSzVyPUCuNFYzKM7:TR?= MlrNNlAyODh|M{i=
COG-LL-317 M2S0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOxNEDPxE1? NYLURZFtQTZiaB?= MY\JR|UxRTBwMES3JO69VQ>? NWXnNIRKOjBzMEizN|g>
RS4-11 NUTZXm1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPSNVAh|ryP MVG5OkBp M1P5VGlEPTB;MD6wNVgh|ryP NYDsZYFXOjBzMEizN|g>
MOLT-4 NFTlUXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrJN4QyOCEQvF2= NY\0NnVlQTZiaB?= M3HFTWlEPTB;MD6wNlYh|ryP NV74PWhLOjBzMEizN|g>
CCRF-CEM M{fIVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1WwZ|ExKM7:TR?= NUD0WXc2QTZiaB?= NHLGeotKSzVyPUCuNFk1KM7:TR?= NXK5Rm9EOjBzMEizN|g>
Kasumi-1 NHrNTG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTGNVAh|ryP NUHhephQQTZiaB?= M4DnfGlEPTB;MD6xNFMh|ryP MXWyNFExQDN|OB?=
Karpas-299 Mln4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInhT3MyOCEQvF2= NFTPbGM6PiCq NH7aXJRKSzVyPUCuNFM5KM7:TR?= NGnwNm4zODFyOEOzPC=>
Ramos-RA1 MmnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnR[o9ROTBizszN NEnjZVM6PiCq M4\qWmlEPTB;MD6xNlch|ryP MWiyNFExQDN|OB?=

... 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-

カスタマーフィードバック (10)


Click to enlarge
Rating
Source Cell Stem Cell, 2012, 11, 179-94. Alisertib (MLN8237) purchased from Selleck
Method qPCR
Cell Lines CCE cells
Concentrations 1 uM
Incubation Time 48 h
Results Treatment with the Aurka-specific chemical inhibitor MLN8237 suppressed pluripotency TF expression and decreased fluorescence in the NG4 Nanog-GFP reporter line.

Click to enlarge
Rating
Source EMBO J, 2012, 30, 906-19. Alisertib (MLN8237) purchased from Selleck
Method immunofluorescence
Cell Lines HEK293 cells
Concentrations 0.3 μM
Incubation Time 40 min
Results Incubation of cells with the Aurora-A kinase inhibitor MLN8237 (0.3 μM) induced a change in the localisation of endogenous TACC3 and clathrin from the mitotic spindle to the cytoplasm.

Click to enlarge
Rating
Source J Cell Biol, 2010, 191, 1315-32. Alisertib (MLN8237) purchased from Selleck
Method DAPI staining
Cell Lines HeLa cells
Concentrations 10/20 nM
Incubation Time 15 min/24 h
Results Depletion of PPP6C resulted in a twofold increase in the pT288 form of Aurora A at prometaphase and metaphase spindles compared with control cells, and addition of 10 nM MLN8237 reversed this increase (Fig. A). Importantly, this partial Aurora A inhibition with 10 nM MLN8237 also reduced the micronucleation seen in PPP6C-depleted cells from 40 to 5% (Fig. B).

Click to enlarge
Rating
Source EMBO reports , 2010, 11, 977-984. Alisertib (MLN8237) purchased from Selleck
Method Immunoprecipitation, MS/MS analysis
Cell Lines HeLa cells
Concentrations 0.5 µM
Incubation Time 1 h
Results This phosphopeptide was absent in interphase cells and strongly reduced in mitotic cells treated with the inhibitor.

Click to enlarge
Rating
Source EMBO Mol Med, 2013, 5(1), 149-66. Alisertib (MLN8237) purchased from Selleck
Method Immunofluorescence co-staining
Cell Lines Hs294T xenograft
Concentrations 30 mg/kg
Incubation Time 28 days
Results To extend its findings in vivo, we examined senescence (SA-b-Gal staining), DNA damage (53BP1), NF-kB activity (IkB-a) and the SASP (IL-6) in an Hs294T xenograft tumour after MLN 8237 treatment. Tumour tissues treated with MLN8237 were b-galactosidase-positive (blue), 53BP1 (red) was increased.

Click to enlarge
Rating
Source Oncogene, 2014, 33, 3550-60. Alisertib (MLN8237) purchased from Selleck
Method Western blot, time-lapse microscopy, flow cytometry
Cell Lines HeLa cells
Concentrations 6-1000 nM
Incubation Time 2 h,8 h,24 h,48 h
Results Alisertib inhibits AURKA and AURKB in a concentration-dependent manner.

Click to enlarge
Rating
Source ACS Chem Biol , 2010, 5, 563-576. Alisertib (MLN8237) purchased from Selleck
Method Duplicate radiometric assays
Cell Lines
Concentrations 0.1-1000 nM
Incubation Time
Results These clinical stage compounds MLN8237 and MLN8254, which exhibit subtly different chemistry, display similar potency towards Aurora A in vitro.

Click to enlarge
Rating
Source ACS Chem Biol , 2010, 5, 563-576. Alisertib (MLN8237) purchased from Selleck
Method Colony assays
Cell Lines WT Aurora A-expressing cells
Concentrations 30 nM
Incubation Time 8 d
Results We find that a T217D/W277E double mutant does not induce cellular resistance to MLN8054 or MLN8237 in cells

Click to enlarge
Rating
Source J Biol Chem, 2012, 287, 27670-81. Alisertib (MLN8237) purchased from Selleck
Method Immunofluorescence Microscopy
Cell Lines HeLa cells
Concentrations 100 nM
Incubation Time 2 h
Results The fluorescence intensity of the pT210 signal in the spindle poles was markedly decreasedin Fry-depleted cells. Exposure to MLN8237, a specific inhibitor of Aurora A, also abrogated the pT210 signal in the spindle poles.

Click to enlarge
Rating
Source Mol Cancer, 2011, 10, 131. Alisertib (MLN8237) purchased from Selleck
Method immunofluorescence
Cell Lines U2OS cells
Concentrations 20/50 nM
Incubation Time 4 h
Results MLN8237 treatment lasted 4 hours and yielded the induction of spindle abnormalities. Spindles with multiple poles represented 15-20 % of all PM/Ms in M LN8237-treated cultures, comparable to the occurrence in Aurora-Ai cultures. When MON was added, Eg5 was inhibited, and the generation of spindles with fragmented poles in MLN8237-treated cultures was abolished, with a parallel increase in mono polar figures.

文献中の引用 (45)

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related オーロラ・キナーゼ 阻害剤

  • Ro-3306

    RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases.

  • CCG-1423

    CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.

  • ML141

    ML141 is a potent, selective and reversible non-competitive inhibitor of Rho family GTPase cdc42 with IC50 of 200 nM.

  • Salirasib

    Salirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Phase 2.

  • Barasertib (AZD1152-HQPA)

    Barasertib (AZD1152-HQPA)は、0.37nMのIC50による非常に選択的なオーロラB阻害剤です。

  • VX-680 (Tozasertib, MK-0457)

    VX-680 (Tozasertib, MK-0457)は汎オーロラ・キナーゼ(AK)阻害剤、、オーロラA、オーロラBとオーロラCに作用すると、 Kiapp がそれぞれ 0.6 nM、18 nM 、 4.6 nMになる。

  • Danusertib (PHA-739358)

    Danusertib (PHA-739358)は ポ-ピラゾール分子が小さいauroraキナーゼとBcr-Ablキナーゼ阻害剤、auroraA, B, Cを作用すると、 IC50がそれぞれ 13 nM, 79 nM, 61 nMとなる.

  • ZM 447439

    ZM 447439は、オーロラ選択ATPです-競争的な阻害剤で、オーロラAキナーゼとオーロラBキナーゼに作用すると、IC50が それぞれ 110 nM と 130 nM,になる。

    Features:An Aurora selective ATP-competitive inhibitor.

  • MLN8054

    MLN8054は、4nMのIC50によるオーロラAキナーゼの強力で選択的な阻害剤です。

最近チェックしたアイテム

Tags: Alisertib (MLN8237)を買う | Alisertib (MLN8237)供給者 | Alisertib (MLN8237)を購入する | Alisertib (MLN8237)費用 | Alisertib (MLN8237)生産者 | オーダーAlisertib (MLN8237) | Alisertib (MLN8237)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ