Alisertib (MLN8237) 化学構造
分子量: 518.92

高品質保証

文献中の引用(46)

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 M4n2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuwMlUh|ryP MmP6O|IhcA>? M4CxT2ROW09? NYC0Xo9EUUN3ME2wMlA1KM7:TR?= M1PnNlI3OTN4Nki0
LS174T MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTNNE42KM7:TR?= NXTjRpBzPzJiaB?= M3nDVmROW09? Ml;wTWM2OD1yLkC1JO69VQ>? M2XjVFI3OTN4Nki0
T84 NVzXW5IzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu0[|gxNjVizszN NXfvbol3PzJiaB?= M3j3fmROW09? NH3F[YxKSzVyPUCuNFkh|ryP MV:yOlE{PjZ6NB?=
LS180 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon6NE42KM7:TR?= M2izPFczKGh? MoPUSG1UVw>? M3jpPWlEPTB;MTFOwG0> Mmm4NlYyOzZ4OES=
SW948 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zKR|AvPSEQvF2= M3TaNFczKGh? MYLEUXNQ NVzR[|NFUUN3ME2xJO69VQ>? NV7pWVRsOjZzM{[2PFQ>
HCT15 M1\mbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XDT|AvPSEQvF2= Ml75O|IhcA>? MlLjSG1UVw>? NUDMR244UUN3MEywMlQh|ryP NFnKUpYzPjF|Nk[4OC=>
DLD-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1GyO|AvPSEQvF2= NVexb|lwPzJiaB?= NW\tdoF1TE2VTx?= MnnZTWM2ODxyLkig{txO NF75UWgzPjF|Nk[4OC=>
MIP-101 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17MUVAvPSEQvF2= Moi5O|IhcA>? NEPFXXRFVVOR NUnrdnk2UUN3ME2xJO69VQ>? NGe1XnkzPjF|Nk[4OC=>
SNU1544 M17wN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCwMlUh|ryP Ml;VO|IhcA>? NHr4N3hFVVOR MX7JR|UxRTFizszN MVWyOlE{PjZ6NB?=
OCI-Ly10 MVHDfZRwfG:6aXOgRZN{[Xl? MmS5O|IhcA>? M2jj[WROW09? NHvtSZVKSzVyPUCuNFU5KM7:TR?= M3LZbVI2QDd6M{Ox
SU-DHL2 M{CwcGN6fG:2b4jpZ{BCe3OjeR?= NH\xb4Y4OiCq NGi2PIxFVVOR NXTHWW9XUUN3ME2wMlAyKM7:TR?= NHLsS|EzPTh5OEOzNS=>
OCI-LY7 MnS1R5l1d3SxeHnjJGF{e2G7 NYrmUZA4PzJiaB?= M1fUTmROW09? M4jhXmlEPTB;MD6wPFEh|ryP MX:yOVg4QDN|MR?=
SU-DHL6 NGTVUZVEgXSxdH;4bYMhSXO|YYm= MXu3NkBp NFjkUpFFVVOR NXTFXGFIUUN3ME2wMlQ5OiEQvF2= MoTENlU5Pzh|M{G=
Jeko-1 MUXDfZRwfG:6aXOgRZN{[Xl? MX:3NkBp NYjjN5JxTE2VTx?= NV64NIpRUUN3ME2wMlAzQSEQvF2= MV:yOVg4QDN|MR?=
JVM-2 MUfDfZRwfG:6aXOgRZN{[Xl? MWK3NkBp MWfEUXNQ NVjrT2Y3UUN3ME2wMlAyKM7:TR?= MUKyOVg4QDN|MR?=
Rec-1 NXW3bIZqS3m2b4TvfIlkKEG|c3H5 MoLGO|IhcA>? MmrPSG1UVw>? NWe1[5BvUUN3ME2wMlA5PyEQvF2= NGnDc2ozPTh5OEOzNS=>
Z-138 MXHDfZRwfG:6aXOgRZN{[Xl? Mmj5O|IhcA>? M{T5SWROW09? MUfJR|UxRTBwMEGzJO69VQ>? MVuyOVg4QDN|MR?=
H9 NVPjNmdVS3m2b4TvfIlkKEG|c3H5 M{HMUlczKGh? NFrZOoxFVVOR M3Phb2lEPTB;MD62JO69VQ>? NUOzZXdjOjV6N{izN|E>
HH M{XWXWN6fG:2b4jpZ{BCe3OjeR?= NXSxb2xZPzJiaB?= MknhSG1UVw>? NEi3W2dKSzVyPUCuO{DPxE1? MnnINlU5Pzh|M{G=
DND41 NX;rbYhSS3m2b4TvfIlkKEG|c3H5 M2H3ZVczKGh? M3\lPWROW09? M{W5cGlEPTB;MD6xJO69VQ>? NFLydG8zPTh5OEOzNS=>
CCL119 MnvRR5l1d3SxeHnjJGF{e2G7 NVPEbWZHPzJiaB?= M1\zTWROW09? M2fadWlEPTB;MD6wOlIh|ryP NEjPPZkzPTh5OEOzNS=>
J.Cam 1.6 Ml3CR5l1d3SxeHnjJGF{e2G7 MkLMO|IhcA>? M2n0NGROW09? MlSyTWM2OD1yLkGwOUDPxE1? Ml\aNlU5Pzh|M{G=
Sup-T1 NFLmbW9EgXSxdH;4bYMhSXO|YYm= M4qwVFczKGh? Mn[zSG1UVw>? MX7JR|UxRTJwMUSyJO69VQ>? NUjtN|lvOjV6N{izN|E>
Tib 152 M{jMfGN6fG:2b4jpZ{BCe3OjeR?= MXm3NkBp M4XqT2ROW09? MkOxTWM2OD1yLkig{txO M2PoNVI2QDd6M{Ox
MCF7 NEjISI5HfW6ldHnvckBCe3OjeR?= M37Te|Uh|ryP M4\LR|I1KGh? M3nQdGROW09? NE\uc3ZKdmS3Y3XzJGczN01iYYLy[ZN1 NF3qVVMzPTh|NESwNS=>
MDA-MB-231 MYfGeY5kfGmxbjDBd5NigQ>? M4PrUlUh|ryP NXjDRpA6OjRiaB?= NX;EdlBXTE2VTx?= Mk\UTY5lfWOnczDHN{9OKGG{cnXzeC=> M3izcVI2QDN2NECx
MCF7 M2LlPWZ2dmO2aX;uJGF{e2G7 NXjGblZLPSEQvF2= NIP2NWkzPCCq NVK2b5BbTE2VTx?= M2XM[2Rm[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDDSGsyN0OGQ{K= NETGbVEzPTh|NESwNS=>
MCF7 MWPGeY5kfGmxbjDBd5NigQ>? MWK1JO69VQ>? MWWyOEBp MYHEUXNQ MnrrSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIFPET|I> MX2yOVg{PDRyMR?=
MCF7 MWXGeY5kfGmxbjDBd5NigQ>? M{f2dlUh|ryP NIXDTY0zPCCq NV7JOYVmTE2VTx?= NGPDe|BF\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gZ5lkdGmwIFKx NIrNbmkzPTh|NESwNS=>
MCF7 NFXrVphHfW6ldHnvckBCe3OjeR?= NEXudFc2KM7:TR?= M4PQbVI1KGh? Mk[2SG1UVw>? MUHJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEKxJHdi\jFxQ3nwNS=> NUTz[5ZTOjV6M{S0NFE>
MCF7 NX3qVINuTnWwY4Tpc44hSXO|YYm= NYPXVJlMPSEQvF2= NGLhbHEzPCCq MWDEUXNQ MULJcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZicEK3JGtqeDF? MVWyOVg{PDRyMR?=
MDA-MB-231 MX7GeY5kfGmxbjDBd5NigQ>? M4jGclUh|ryP MoDnNlQhcA>? NUPuRm8yTE2VTx?= MVPE[YNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2ZiQ1TLNU9ETEN{ M3zjRlI2QDN2NECx
MDA-MB-231 MYLGeY5kfGmxbjDBd5NigQ>? MkDlNUDPxE1? MYWyOEBp MkPpSG1UVw>? NEDZcWxKdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3[gR2RMOg>? M{jkS|I2QDN2NECx
MDA-MB-231 MnL5SpVv[3Srb36gRZN{[Xl? MW[1JO69VQ>? MnfrNlQhcA>? MUXEUXNQ MmDNSIVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIHP5Z4xqdiCEMR?= NVmwepd5OjV6M{S0NFE>
MDA-MB-231 MVHGeY5kfGmxbjDBd5NigQ>? M{HxW|Uh|ryP NULVNIZLOjRiaB?= NF;iUm1FVVOR M3:4Umlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlEhX2GoMT;DbZAy MVGyOVg{PDRyMR?=
MDA-MB-231 MWHGeY5kfGmxbjDBd5NigQ>? MXm1JO69VQ>? MmXONlQhcA>? M3jnTGROW09? M1LI[mlv[3KnYYPld{B1cGViZYjwdoV{e2mxbjDs[ZZmdCCxZjDwNlchU2myMR?= M{TBeVI2QDN2NECx
MDA-MB-231 NV7xfVJwTnWwY4Tpc44hSXO|YYm= MknzOUDPxE1? M3;kUlI1KGh? MmrsSG1UVw>? Mn;RTY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:oIIC1Ny=> MUiyOVg{PDRyMR?=
MCF7 NFu5[ldCeG:ydH;zbZMhSXO|YYm= NXvLd|VoPSEQvF2= NFuydG4zPCCq NEDCboVFVVOR M1\WW2lv\HWlZYOgZZBweHSxdHnjJIRm[XSq NYnyVFhGOjV6M{S0NFE>
MDA-MB-231 MUnBdI9xfG:|aYOgRZN{[Xl? M1PHTFUh|ryP M4j1PVI1KGh? NE\tboZFVVOR M3THc2lv\HWlZYOgZZBweHSxdHnjJIRm[XSq NYfOVIltOjV6M{S0NFE>
MCF7 MoDHSpVv[3Srb36gRZN{[Xl? MkW0NUDPxE1? MVq3NkBp NXzaSFRXTE2VTx?= MnO1TY5lfWOnczDheZRweGijZ3njJIRm[XSq MYGyOVg{PDRyMR?=
MDA-MB-231 MoLDSpVv[3Srb36gRZN{[Xl? MVmxJO69VQ>? MnvZO|IhcA>? M3rxbmROW09? NI\vVo9KdmS3Y3XzJIF2fG:yaHHnbYMh\GWjdHi= NFPz[nEzPTh|NESwNS=>
U-2 OS NHLySIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrPNGc2OCEQvF2= Mle5NlQhcA>? M2PhfWROW09? Mn\PTWM2OD1zNj62JO69VQ>? MkTMNlU4QTJ6MUG=
MG-63 M1HDdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXiXGF{PTBizszN MnToNlQhcA>? NFLPPVBFVVOR MWHJR|UxRTlwNTFOwG0> MX:yOVc6OjhzMR?=
U-2 OS M4nLR2Fxd3C2b4Ppd{BCe3OjeR?= NEP1VJk2KM7:TR?= NWG4cJNEOjRiaB?= MXfEUXNQ NW\S[Fl6UW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cA>? Mk[3NlU4QTJ6MUG=
MG-63 NI[2OJNCeG:ydH;zbZMhSXO|YYm= NV[2dWpkPSEQvF2= M3\lTFI1KGh? NGLPZpVFVVOR NFjwUGxKdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRp NHnoOI4zPTd7MkixNS=>
U-2 OS M2WwXWZ2dmO2aX;uJGF{e2G7 NF7IZ282KM7:TR?= MUWyOEBp MXTEUXNQ NIHGclNRem:vb4Tld{BifXSxcHjh[4lkKGOnbHyg[IVifGh? M3Tud|I2Pzl{OEGx
MG-63 NHLr[4ZHfW6ldHnvckBCe3OjeR?= MYq1JO69VQ>? NXuzO3dYOjRiaB?= MVfEUXNQ MnTzVJJwdW:2ZYOgZZV1d3CqYXfpZ{Bk\WyuIHTlZZRp M3nsRlI2Pzl{OEGx
PANC-1 NH3SUnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fGflUxKM7:TR?= NHnqU3AzPCCq MYrEUXNQ NH75SJNKSzVyPUeuNUDPxE1? MkTuNlU3OzJ{MkW=
BxPC-3 M3n5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37McFUxKM7:TR?= NVPaN4RQOjRiaB?= Ml;OSG1UVw>? MWLJR|UxRTZwODFOwG0> M{PmPFI2PjN{MkK1
PANC-1 Mn;GSpVv[3Srb36gRZN{[Xl? NXv3SXF4PSEQvF2= NHHRbWszPCCq NX3ld3FuTE2VTx?= MlH1TY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDpckBIOi:PIIDoZZNm NYfhWlR{OjV4M{KyNlU>
BxPC-3 NV\FcFVOTnWwY4Tpc44hSXO|YYm= NEO4N4Y2KM7:TR?= MknPNlQhcA>? MVTEUXNQ MVHJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHnuJGczN01icHjhd4U> MoDaNlU3OzJ{MkW=
PANC-1 NUDncoJyTnWwY4Tpc44hSXO|YYm= MUS1JO69VQ>? MXqyOEBp MnjaSG1UVw>? MW\JcoR2[2W|IHH1eI9xcGGpaXOgZ4VtdCCmZXH0bC=> MYiyOVY{OjJ{NR?=
BxPC-3 MoXaSpVv[3Srb36gRZN{[Xl? MUO1JO69VQ>? NFHxVmkzPCCq MoLLSG1UVw>? MkHyTY5lfWOnczDheZRweGijZ3njJINmdGxiZHXheIg> NFPucWUzPTZ|MkKyOS=>
SKOV3 NHLTW3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVqxNFAh|ryP NVezVIl3OjRiaB?= NFPSSGZFVVOR NI\OOnlKSzVyPUKwMlQ5KM7:TR?= MkfKNlU3OjR5NUC=
OVCAR4 NWfocpRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXmxNFAh|ryP M4PxblI1KGh? MoKzSG1UVw>? M{X5WmlEPTB;MkKuNVMh|ryP NGnl[5czPTZ{NEe1NC=>
SKOV3 NYPMUWpQTnWwY4Tpc44hSXO|YYm= NEe3cWc2KM7:TR?= NWmwUIozPzJiaB?= M2r2S2ROW09? NYi0OoM3UW6mdXPld{BIOi:PIHHydoV{fA>? M{\GfFI2PjJ2N{Ww
OVCAR4 M4iwcmZ2dmO2aX;uJGF{e2G7 MXe1JO69VQ>? M3jk[VczKGh? Ml72SG1UVw>? M1TERmlv\HWlZYOgS|IwVSCjcoLld5Q> MoC4NlU3OjR5NUC=
SKOV3 NXvnOItGSXCxcITvd4l{KEG|c3H5 M{PHWVUh|ryP NX71UFJ[OjRiaB?= M2fWU2ROW09? M4e4Nmlv\HWlZYOgZZBweHSxc3nz M4q3bFI2PjJ2N{Ww
OVCAR4 NVvPUW5GSXCxcITvd4l{KEG|c3H5 NX63fpFCPSEQvF2= NWrlOI41OjRiaB?= NEPreVdFVVOR NET3UFJKdmS3Y3XzJIFxd3C2b4Ppdy=> M2TQOVI2PjJ2N{Ww
AGS MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfCVIdyOjVizszN NIm0cpczPCCq M4G4WmROW09? NYfacIdMUUN3ME2xPU4xQSEQvF2= MVKyOVYxQTl{Mx?=
NCI-N78 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHSWJRJOjVizszN MWSyOEBp MlnGSG1UVw>? M2TLbGlEPTB;Mk[uN|Mh|ryP M{exXVI2PjB7OUKz
AGS NH35U4tCeG:ydH;zbZMhSXO|YYm= MkDKOUDPxE1? MVqyOEBp MlqzSG1UVw>? NWW1PWFRUW6mdXPld{BieG:ydH;zbZM> M4PqS|I2PjB7OUKz
NCI-N78 NF;tcXRCeG:ydH;zbZMhSXO|YYm= M3vQd|Uh|ryP NUTJd2Z1OjRiaB?= MWTEUXNQ NFnVSHZKdmS3Y3XzJIFxd3C2b4Ppdy=> NFW1SXEzPTZyOUmyNy=>
AGS Mki2SpVv[3Srb36gRZN{[Xl? NV36R2tWPSEQvF2= NHXvU|MzPCCq NVzuV4JwTE2VTx?= M3f0U2lv\HWlZYOgeIhmKGG3dH;wbIFogQ>? NF7FSoMzPTZyOUmyNy=>
NCI-N78 MV;GeY5kfGmxbjDBd5NigQ>? NVLMZYFFPSEQvF2= MVKyOEBp M3zvS2ROW09? Mmr2TY5lfWOnczD0bIUh[XW2b4DoZYd6 NW[yNGFlOjV4MEm5NlM>
HSC-3 M3jlSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq5NUDPxE1? NXG0b|d4PDhiaB?= NFrGNHFKSzVyPUCuOVQh|ryP MkW2NlU{PjZzNEO=
GB30 M2TqWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[xJO69VQ>? NGLGbVU4KGR? NWribHZPTE2VTx?= NEH4eohKSzVyPUCuNFEyKM7:TR?= M4The|I2OTB4NEK4
GB9 NHH5coVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTKNUDPxE1? M3nC[lch\A>? M3TyNWROW09? NUO4OZVLUUN3ME2wMlAzPCEQvF2= NUn3OHZqOjVzME[0Nlg>
GB169 Mn;sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDVd3JZOSEQvF2= NXjudGUyPyCm Mlu0SG1UVw>? NXGzdmxIUUN3ME2wMlA{OiEQvF2= M2Dm[|I2OTB4NEK4
T24 M4jBSGZ2dmO2aX;uJGF{e2G7 NIHwbW4yKM7:TR?= M3jBR|Q5KGh? MnHJSG1UVw>? Ml;LTY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MUWyN|QxOzZ|Mx?=
RT4 MkC0SpVv[3Srb36gRZN{[Xl? M3;ze|Eh|ryP NXf5RZhEPDhiaB?= MYjEUXNQ MX7JcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 M1ryflI{PDB|NkOz
UM-UC-3 NYDlO3ZMTnWwY4Tpc44hSXO|YYm= M4W3blEh|ryP MVm0PEBp MmmzSG1UVw>? MVTJcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NGS2XGYzOzRyM{[zNy=>
T24 M1HHO2Fxd3C2b4Ppd{BCe3OjeR?= M3;PXFMvOTZizszN Mn3QPVYhcA>? M4Htb2ROW09? M{KwUWlEPTB;MD6wN|A3KM7:TR?= NY\uTVAyOjN2MEO2N|M>
RT4 MmjkRZBweHSxc3nzJGF{e2G7 Mn7vN{4yPiEQvF2= NUe4bldQQTZiaB?= M3PQdGROW09? NH31XVBKSzVyPUCuNVE6QCEQvF2= MoT6NlM1ODN4M{O=
UM-UC-3 M2LET2Fxd3C2b4Ppd{BCe3OjeR?= NYLMUVZ5Oy5zNjFOwG0> NF62TYQ6PiCq M{nWb2ROW09? MV;JR|UxRTBwMES0PUDPxE1? NXjMVnlZOjN2MEO2N|M>
OVCAR-5 NUfveoYxTnWwY4Tpc44hSXO|YYm= MnHsOVAhdk1? Mon6TY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? MmnwNlM{OzR|Mke=
SKOV3ip2 M{DoV2Z2dmO2aX;uJGF{e2G7 NH\Wd2U2OCCwTR?= M1;RRmlvcGmkaYTzJINmdGxibXnndoF1cW:w NVzVXlFXOjN|M{SzNlc>
S462 NUTCeZl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jYWVExOCEQvF2= MmnpO|IhcA>? MnW3SG1UVw>? MVHBeJRmdnWjdHXzJINmdGxiZ4Lve5Rp NF6xU2czOzN{OEGxOC=>
2884 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSxNFAh|ryP NVjFSZFIPzJiaB?= MUXEUXNQ Mn3sRZR1\W63YYTld{Bk\WyuIHfyc5d1cA>? MViyN|MzQDFzNB?=
2885 NIO1W21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jKTlExOCEQvF2= NV;RZ2RlPzJiaB?= NGLET|BFVVOR MYnBeJRmdnWjdHXzJINmdGxiZ4Lve5Rp MYeyN|MzQDFzNB?=
CRL-2396 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjF[HJFOTByIN88US=> MX;3ZZRmeg>? MVLJR|UxRTBwMEmyJO69VQ>? NEi1fZQzOzF3M{WyOC=>
TIB-48 NFX0OHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NECydmMyODBizszN NGXvZ2V4[XSnch?= Mn3hTWM2OD1yLkC4PEDPxE1? MmnHNlMyPTN3MkS=
CRL-2396 M2TldmN6fG:2b4jpZ{BCe3OjeR?= NVTFRYE{OSEQvF2= MkjQOFghcA>? MoHHe4F1\XJ? M4O1XGlv\HWlZYOgZZBweHSxc3nz M1jvbVI{OTV|NUK0
TIB-48 M{DwSmN6fG:2b4jpZ{BCe3OjeR?= NWew[ItCOSEQvF2= NWjCeFdpPDhiaB?= NHPkbXl4[XSnch?= NXX3dZdpUW6mdXPld{BieG:ydH;zbZM> Mkj5NlMyPTN3MkS=
AGS M1fmXGN6fG:2b4jpZ{BCe3OjeR?= MXiwMlUh|ryP NV;zXIFJOjRiaB?= M2PxeGROW09? NEHNWHhF\WO{ZXHz[ZMh[2WubDDzeZJ3cX[jbB?= NVTiZ5N{OjJ7N{K2NVE>
FLO-1 M3;DcGN6fG:2b4jpZ{BCe3OjeR?= MkXNNE42KM7:TR?= NVzTc5kxOjRiaB?= NFnBPJhFVVOR MXTE[YNz\WG|ZYOgZ4VtdCC|dYL2bZZidA>? NVW2[lVwOjJ7N{K2NVE>
OE33 M{jvPGN6fG:2b4jpZ{BCe3OjeR?= NXrWNmRXOC53IN88US=> M4DiWFI1KGh? NFuzSWpFVVOR NYPueIw2TGWlcnXhd4V{KGOnbHygd5Vzfmm4YXy= NGLvZmMzOjl5Mk[xNS=>
SKLMS MoPDR5l1d3SxeHnjJGF{e2G7 NVzENmlkPzVibl2= M{\QfVk3KGh? M1j3Vmlv\HWlZYOgZZBweHSxc3nz NXfnbllEOjJ6MkG5PVc>
Leio285 MYDDfZRwfG:6aXOgRZN{[Xl? NInGOY44PSCwTR?= NHTwclM6PiCq MnzFTY5lfWOnczDhdI9xfG:|aYO= NYPib3FJOjJ6MkG5PVc>
Mes-Sa MnfMR5l1d3SxeHnjJGF{e2G7 NFzBXog4PSCwTR?= MljwPVYhcA>? M3vZfWlv\HWlZYOgZZBweHSxc3nz M3\XPVIzQDJzOUm3
DAOY NIHufZREgXSxdH;4bYMhSXO|YYm= NUXpRpJWOTBizszN MoXnO|IhcA>? MUnEUXNQ MYXJR|UxRTBwMESg{txO MnjhNlI3Pjl|M{W=
IMR32 M1O5cGN6fG:2b4jpZ{BCe3OjeR?= NVWxbFRpOTBizszN MVS3NkBp Mn\HSG1UVw>? MUTJR|UxRTBwMEOg{txO M2mwO|IzPjZ7M{O1
Molt-4 NH;rWm5EgXSxdH;4bYMhSXO|YYm= NVrCUFdJOTBizszN MYi3NkBp NEe3[ItFVVOR NUPtPXZSUUN3ME2wMlAzKM7:TR?= MX6yNlY3QTN|NR?=
MOLM-13 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXVN{DPxE1? NUnPWYRkPzJiaB?= MlPoSIlucW6rc3jld{Bk\WyuII\pZYJqdGm2eR?= MojXNlI1QDh{NEm=
HL-60 MmPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nZXFMh|ryP M4DBXlczKGh? MmruSIlucW6rc3jld{Bk\WyuII\pZYJqdGm2eR?= MmfpNlI1QDh{NEm=
MV4-11 NXLaUJNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjLN{DPxE1? M3\aWlczKGh? M17NNWRqdWmwaYPo[ZMh[2WubDD2bYFjcWyrdIm= M2XpNlIzPDh6MkS5
SKM-1 NUThT4x6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;ETpQ{KM7:TR?= NInlVYI4OiCq NYfsd3liTGmvaX7pd4hmeyClZXzsJJZq[WKrbHn0fS=> NF;3PWkzOjR6OEK0PS=>
SH2 Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlmzN{DPxE1? M{Gzd|czKGh? NILVXG9FcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5 NFrDXHEzOjR6OEK0PS=>
NOMO-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUizJO69VQ>? M3rXVFczKGh? MoXSSIlucW6rc3jld{Bk\WyuII\pZYJqdGm2eR?= NITxZlMzOjR6OEK0PS=>
OCL-AML2 M3v5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfs[YY5OyEQvF2= MmHtO|IhcA>? NWXZUVZlTGmvaX7pd4hmeyClZXzsJJZq[WKrbHn0fS=> NHzGbIUzOjR6OEK0PS=>
PL-21 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF6wUms{KM7:TR?= NXK1fIc5PzJiaB?= NVT1SHNiTGmvaX7pd4hmeyClZXzsJJZq[WKrbHn0fS=> MkL0NlI1QDh{NEm=
KG-1 NEmydmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCzJO69VQ>? NUHnXWV5PzJiaB?= NELqNXhFcW2rbnnzbIV{KGOnbHygeoli[mmuaYT5 Mn7BNlI1QDh{NEm=
A172 NHe5V2xEgXSxdH;4bYMhSXO|YYm= MmHoNVAxKM7:TR?= M1;iNlI1KGh? MlvPSG1UVw>? MWHJR|UxRTBwMUKwJO69VQ>? MWiyNlI4PDN7OR?=
U87 NHjWVJlEgXSxdH;4bYMhSXO|YYm= NXi4dphLOTByIN88US=> NGPJfpQzPCCq NHSxTWtFVVOR MUPJR|UxRTBwMUC1JO69VQ>? MkLWNlIzPzR|OUm=
U251 M3\m[mN6fG:2b4jpZ{BCe3OjeR?= NGW1b2syODBizszN MkjLNlQhcA>? MnXlSG1UVw>? NEPuSFdKSzVyPUCuNVAxKM7:TR?= MmX6NlIzPzR|OUm=
T98 NVXMdlZNS3m2b4TvfIlkKEG|c3H5 MnHSNVAxKM7:TR?= MYGyOEBp MWnEUXNQ NXPT[4llUUN3ME2wMlEzPSEQvF2= NV[0bWRqOjJ{N{SzPVk>
LN18 MknSR5l1d3SxeHnjJGF{e2G7 M4XjSFExOCEQvF2= MoLqNlQhcA>? M4rveGROW09? M1Pye2lEPTB;MD6yNVAh|ryP NXfXVph{OjJ{N{SzPVk>
LN443 M2HQV2N6fG:2b4jpZ{BCe3OjeR?= Mk\qNVAxKM7:TR?= NV\OS5ZNOjRiaB?= M1TqSGROW09? NEO0e|NKSzVyPUCuNlIxKM7:TR?= MXSyNlI4PDN7OR?=
HF66 NW\SeYV7S3m2b4TvfIlkKEG|c3H5 Ml\YNVAxKM7:TR?= M4nBV|I1KGh? NFvydlFFVVOR M1XvV2lEPTB;MD6yNlUh|ryP MVSyNlI4PDN7OR?=
HF2303 NVHVd|h1S3m2b4TvfIlkKEG|c3H5 MXOxNFAh|ryP M2jKNlI1KGh? M2TaUmROW09? MVTJR|UxRTBwME[wJO69VQ>? MVyyNlI4PDN7OR?=
HF2359 NIPZUXVEgXSxdH;4bYMhSXO|YYm= M4niWFExOCEQvF2= NVG1cXM5OjRiaB?= MmPwSG1UVw>? NWCwO4JCUUN3ME2wMlA3OCEQvF2= NVzITohJOjJ{N{SzPVk>
HF2414 NX\C[XFCS3m2b4TvfIlkKEG|c3H5 NX\tU5BCOTByIN88US=> M4jxe|I1KGh? Ml3qSG1UVw>? M4LZZmlEPTB;MD6wPFAh|ryP MnH0NlIzPzR|OUm=
A-673 NFuxVldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml62NVAh|ryP M4fZ[Vk3KGh? MXrEUXNQ MoXGTWM2OD1yLkCzNkDPxE1? M2DLUlIyPDR6NUmx
TC-32 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKxNEDPxE1? M2Hld|k3KGh? M2SxOGROW09? NYPmWXVDUUN3ME2wMlA{QSEQvF2= Mn7RNlE1PDh3OUG=
TC-71 M3roRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTsW5NoOTBizszN M{TvUlk3KGh? NWLBd5hkTE2VTx?= NVzGcId7UUN3ME2wMlExOiEQvF2= NIXFfnAzOTR2OEW5NS=>
SK-N-MC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOxNEDPxE1? MYS5OkBp MVTEUXNQ NE\teG5KSzVyPUCuNFczKM7:TR?= NHPTdZgzOTR2OEW5NS=>
CHLA-9 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XMWlExKM7:TR?= MkPPPVYhcA>? Mn;2SG1UVw>? MV7JR|UxRTBwMEG4JO69VQ>? NV7EVnZqOjF2NEi1PVE>
CHLA-10 NFf2bnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoW4NVAh|ryP M1KxVFk3KGh? MknUSG1UVw>? NX;uU|F[UUN3ME2wMlA3OCEQvF2= MoLuNlE1PDh3OUG=
CHLA-25 MlewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\GSndSOTBizszN MUG5OkBp MnK3SG1UVw>? MlLNTWM2OD1yLkG2PEDPxE1? MYqyNVQ1QDV7MR?=
CHLA-32 M3fYR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxNEDPxE1? MWO5OkBp MVXEUXNQ NHLLSYdKSzVyPUCuNVM3KM7:TR?= NVm3Ro1XOjF2NEi1PVE>
CHLA-56 NInMbGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1G5WFExKM7:TR?= MU[5OkBp NHLMV4dFVVOR NUPW[G9lUUN3ME2xNEDPxE1? MVqyNVQ1QDV7MR?=
CHLA-258 Mlf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XhelExKM7:TR?= NIfBNmQ6PiCq NF;VSW1FVVOR NXvCN4piUUN3ME2wMlE{OiEQvF2= M4Lr[FIyPDR6NUmx
COG-E-352 Mle1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDhbXRyOTBizszN MYe5OkBp NW\oSpVUTE2VTx?= NUnyPXJvUUN3ME2wMlA1OyEQvF2= MVOyNVQ1QDV7MR?=
CHLA-90 M37XV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H0ZVExKM7:TR?= NWOyZpc{QTZiaB?= NFzYOllFVVOR NELWRZdKSzVyPUCuNFYyKM7:TR?= NVW3S3pmOjF2NEi1PVE>
CHLA-119 NVnzeYVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGCxcFcyOCEQvF2= NVrEO|NVQTZiaB?= NVq4eJVXTE2VTx?= M2PDOGlEPTB;MD6wNlIh|ryP MWKyNVQ1QDV7MR?=
CHLA-122 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[2WGI{OTBizszN NX7Jd2JTQTZiaB?= MWnEUXNQ MojXTWM2OD1yLkCxPUDPxE1? M3XMSFIyPDR6NUmx
CHLA-136 NHfpUGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXsfHlbOTBizszN MmSwPVYhcA>? MX\EUXNQ NIfxdVdKSzVyPUCuNFM6KM7:TR?= MkTpNlE1PDh3OUG=
CHLA-140 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4noOlExKM7:TR?= NG\FbIU6PiCq MVrEUXNQ MnTGTWM2OD1yLkCyOkDPxE1? MYmyNVQ1QDV7MR?=
LA-N-6 NFLaTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXuNVAh|ryP NXfrXWFQQTZiaB?= NEXRV3JFVVOR MWnJR|UxRTBwMEW0JO69VQ>? NV\UTpdlOjF2NEi1PVE>
NB-1643 MkHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnniNVAh|ryP M37NNlk3KGh? M{TLOmROW09? M2njU2lEPTB;MD6wN|ch|ryP NEjNUlQzOTR2OEW5NS=>
NB-EBc1 M17Vemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DlbFExKM7:TR?= Mk[0PVYhcA>? MlXVSG1UVw>? MlSwTWM2OD1yLkC1NEDPxE1? NHnob2QzOTR2OEW5NS=>
SK-N-BE-1 NYPZfmpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln0NVAh|ryP Mln2PVYhcA>? Ml\0SG1UVw>? M1;FSmlEPTB;MD6wNlgh|ryP NIewTmozOTR2OEW5NS=>
SK-N-BE-2 M1y0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:xNEDPxE1? NUfZPWNIQTZiaB?= M2W1XmROW09? M1ewR2lEPTB;MD6wN|Yh|ryP NGPGcZEzOTR2OEW5NS=>
SMS-KAN M{\peGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPnNYsyOCEQvF2= M2LHRVk3KGh? MVXEUXNQ M1TsbWlEPTB;MD6wN|Qh|ryP M{nOb|IyPDR6NUmx
SMS-KANR NIXYcmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfaNVAh|ryP M17Pb|k3KGh? M4XG[2ROW09? MonTTWM2OD1yLkCyOkDPxE1? M3rVPFIyPDR6NUmx
SMS-KCN NEPzd|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6xNEDPxE1? MlrOPVYhcA>? MVfEUXNQ NHnsPGZKSzVyPUCuNFE6KM7:TR?= NHThXGMzOTR2OEW5NS=>
SMS-KCNR MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7OTIYyOCEQvF2= M3HsXVk3KGh? NVqyUFJXTE2VTx?= MUHJR|UxRTBwMEGwJO69VQ>? NWO4OGFnOjF2NEi1PVE>
SMS-LHN M33Wbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;ne|JoOTBizszN NUHIPZR{QTZiaB?= NIW0VGZFVVOR NFPoNmJKSzVyPUCuNFMzKM7:TR?= MnHCNlE1PDh3OUG=
SMS-MSN NVjvVGNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTVe5EyOCEQvF2= NWC3e2xrQTZiaB?= NFzTb|JFVVOR NE\2O2RKSzVyPUCuNFIzKM7:TR?= NYTmPXJuOjF2NEi1PVE>
SMS-SAN NFTqV4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:zbVExKM7:TR?= NG\RN4s6PiCq M3\weWROW09? MljlTWM2OD1yLkCyNEDPxE1? NVSwbXJ4OjF2NEi1PVE>
Granta-4 NYX2PZExS3m2b4TvfIlkKEG|c3H5 Mn3KNVAh|ryP NULYWGNpPyCm NVPhVYFZUUN3ME2wMlA1OCEQvF2= MWiyNVI6OTh4Nx?=
DB MWPDfZRwfG:6aXOgRZN{[Xl? MWCxNEDPxE1? MkXzO{Bl NUX5fGo5UUN3ME2wMlA1OiEQvF2= NEjuRY0zOTJ7MUi2Oy=>
RL NXGzW5VNS3m2b4TvfIlkKEG|c3H5 Ml62NVAh|ryP M3jse|ch\A>? MnS3TWM2OD1yLkCxOUDPxE1? Ml2wNlEzQTF6Nke=
K562 NHzVXHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XxcFExKM7:TR?= NIX1[XE6PiCq MWDJR|UxRTBwMEi3JO69VQ>? M3P2NVIyODlzNkOz
LAMA-84 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVyxNEDPxE1? Ml;0PVYhcA>? MYHJR|UxRTBwMEW3JO69VQ>? NV7TT2J[OjFyOUG2N|M>
MM15 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknJOEDPxE1? NFHkUpo4OiCq NXj6UXd4TE2VTx?= NX;ndWNKUUN3ME2wMlE{KM7:TR?= MW[yNFM5Ojh2NB?=
OPM1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV20JO69VQ>? MofzO|IhcA>? NGizOXlFVVOR NFvneFhKSzVyPUCuNFMh|ryP MlOxNlA{QDJ6NES=
RPM1 NULGSXVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvTOEDPxE1? NHvJblU4OiCq M13MV2ROW09? NFfS[IJKSzVyPUGwMlMzKM7:TR?= Mn\xNlA{QDJ6NES=
INA6 NVzxUmlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXW0JO69VQ>? M4DnXVczKGh? MVzEUXNQ M2[5PWlEPTB;MD6wNFIh|ryP NVHWNWU5OjB|OEK4OFQ>
OPM2 NF7u[oNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnZUJY1KM7:TR?= MnftO|IhcA>? Mk[3SG1UVw>? NFrv[FlKSzVyPUSuN|ch|ryP NXnwbHBGOjB|OEK4OFQ>
MM1R NHSwT2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPwTpY1KM7:TR?= M4G4TVczKGh? MknjSG1UVw>? MW\JR|UxRTFwNkig{txO NWX2R2UyOjB|OEK4OFQ>
DOX40 Ml3GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvkOEDPxE1? M1vo[lczKGh? MlnFSG1UVw>? NETvbW5KSzVyPUWuOFgh|ryP M2fuWVIxOzh{OES0
LR5 M4PwWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILpVlM1KM7:TR?= NEjMZW84OiCq MmTmSG1UVw>? MWHJR|UxRTJwNUOg{txO MonCNlA{QDJ6NES=
U266 NWPYdJZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWC1dGVYPCEQvF2= NXrrbm9pPzJiaB?= NEDnR4ZFVVOR MWLJR|UxRTFwNEOg{txO MoK0NlA{QDJ6NES=
RD MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXexNEDPxE1? NF33R3U6PiCq NGPnUXhKSzVyPUCuNlI5KM7:TR?= MlnHNlAyODh|M{i=
Rh41 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTWNIMyOCEQvF2= M3Pwe|k3KGh? Ml3RTWM2OD1yLkC5NEDPxE1? NFPKdZgzODFyOEOzPC=>
Rh30 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDtT2dMOTBizszN M2fPO|k3KGh? NUDC[mNiUUN3ME2wMlI{OCEQvF2= MkXvNlAyODh|M{i=
BT-12 NEHsU2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3S5Z|ExKM7:TR?= MmD5PVYhcA>? MXXJR|UxRTBwME[wJO69VQ>? MVWyNFExQDN|OB?=
CHLA-266 M2Dj[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWSxNEDPxE1? M1\IO|k3KGh? NHW3WW9KSzVyPUCuNFczKM7:TR?= MnTSNlAyODh|M{i=
TC-71 MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXGVWtROTBizszN NFHKZYg6PiCq NV\mZ2plUUN3ME2wMlExOiEQvF2= NXztPJVSOjBzMEizN|g>
SJ-GBM2 NUTlZY1XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoK3NVAh|ryP NET0PVA6PiCq NXy1bVFJUUN3ME2wMlA2OCEQvF2= Ml3ONlAyODh|M{i=
NALM-6 M1vnZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{npflExKM7:TR?= NX3UTWZzQTZiaB?= MoOxTWM2OD1yLkC2NkDPxE1? M1P0TVIxOTB6M{O4
COG-LL-317 M1nWd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH6NVAh|ryP NVf3SVI2QTZiaB?= NXyxPXZDUUN3ME2wMlA1PyEQvF2= NVHFVINrOjBzMEizN|g>
RS4-11 MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1THZlExKM7:TR?= MoDWPVYhcA>? MmXOTWM2OD1yLkCxPEDPxE1? MmS3NlAyODh|M{i=
MOLT-4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;yflExKM7:TR?= M{naelk3KGh? NWXY[|RYUUN3ME2wMlAzPiEQvF2= MXKyNFExQDN|OB?=
CCRF-CEM MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DqdlExKM7:TR?= MYe5OkBp M4S1W2lEPTB;MD6wPVQh|ryP MYCyNFExQDN|OB?=
Kasumi-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnTNVAh|ryP M4TuNFk3KGh? NXjMRlRHUUN3ME2wMlExOyEQvF2= Ml7VNlAyODh|M{i=
Karpas-299 NVfkR|VQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;YN|ExKM7:TR?= NIHk[oI6PiCq MYrJR|UxRTBwMEO4JO69VQ>? M3fvTlIxOTB6M{O4
Ramos-RA1 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fKU|ExKM7:TR?= Mo\3PVYhcA>? M33RS2lEPTB;MD6xNlch|ryP NEDRcmYzODFyOEOzPC=>

... 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 (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)

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