Barasertib (AZD1152-HQPA)

For research use only. Not for use in humans.

目录号：S1147 别名： AZD2811, INH-34 中文名称：巴拉塞替

Barasertib (AZD1152-HQPA) Chemical Structure

CAS No. 722544-51-6

Barasertib (AZD1152-HQPA, AZD2811, INH-34) 是一种高度选择性的Aurora B抑制剂，无细胞试验中IC50为0.37 nM，作用于Aurora B比作用于Aurora A选择性高3700倍左右。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1375.46 现货
RMB 976.12 现货
RMB 3169.53 现货
RMB 5477.43 现货
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客户使用Selleck生产的Barasertib (AZD1152-HQPA)发表文献89篇：

产品安全说明书

Aurora Kinase抑制剂选择性比较

生物活性

产品描述 Barasertib (AZD1152-HQPA, AZD2811, INH-34) 是一种高度选择性的Aurora B抑制剂，无细胞试验中IC50为0.37 nM，作用于Aurora B比作用于Aurora A选择性高3700倍左右。
靶点
Aurora B [1]
(Cell-free assay)
0.37 nM
体外研究

AZD1152作用于Aurora B比作用于Aurora A选择性高3000多倍，IC50为1.368 μM。AZD1152作用于50种其他丝-苏氨酸和酪氨酸激酶，包括FLT3, JAK2, 和 Abl活性更低。AZD1152 抑制造血恶性细胞增殖，如HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, 和K562细胞，IC50为3-40 nM,效果比另一种Aurora激酶抑制剂ZM334739高100多倍，IC50为3-30 μM。AZD1152抑制MOLM13和MV4-11细胞克隆生长，IC50分别为1 nM和2.8 nM,也抑制新分离的抗Imatinib的白血病细胞，IC50 为1-3 nM, 比作用于骨髓单核细胞更有效，IC50>10 nM。AZD1152 诱导携带 4N/8N DNA的细胞累积，随后凋亡，这种作用存在剂量和时间依赖性。 [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LNCaP NFHoU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSwMVUxOCCwTR?= M1TKPFQ5yqCq MnvKTWM2OD1{NTDuUS=> MlfIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{e2OVkoRjJ3Mke3OlU6RC:jPh?=
LNCaP MWnBdI9xfG:|aYOgRZN{[Xl? M1KwUFAuPTByIH7N NV;afpZ7PDkEoHi= NH\PdIlqdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKHSqcn;1[4gh[2G|cHHz[U0{KHWycnXneYxifGmxbh?= M4jp[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mke3OlU6Lz5{NUK3O|Y2QTxxYU6=
LNCaP M3HsdmZ2dmO2aX;uJGF{e2G7 NWnN[HFLPTBibl2= NF\RVIg1QCCq NFvLNIJqdmS3Y3XzJI1q[3KxboXjcIVqKHerdHigZY5mfWenbnnjJI1m[2ijbnnzcS=> M37sNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mke3OlU6Lz5{NUK3O|Y2QTxxYU6=
Ramos NI\ufXpHfW6ldHnvckBCe3OjeR?= NUHGW25jPTByIH7N NG[2bm4xNTd{IHi= NUjqSWhKcW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl M2PEeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
Daudi  M3\zSmZ2dmO2aX;uJGF{e2G7 Moe5OVAxKG6P M2LUO|AuPzJiaB?= Ml\6bY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
L540 MVPGeY5kfGmxbjDBd5NigQ>? M{TUR|UxOCCwTR?= M{P3eVAuPzJiaB?= MY\pcohq[mm2czDBeZJwemFiQjDrbY5ie2V? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
BJAJ NEPPNIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfKNo1GPTByIH7N Mn7tNE04OiCq NVLHWXJ1cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NILLeYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Ramos M{DxZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjZOVAxKG6P NXPGTXJyOC15MjDo MUPpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
Raji NHjPS3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHyOVAxKG6P MVWwMVczKGh? NVXCOGVOcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NEHmNoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Daudi  M3LUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LNPVUxOCCwTR?= M2m5UlAuPzJiaB?= MYLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NFrUSpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
L428 NXHtb5I5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHuOVAxKG6P M3f4[VAuPzJiaB?= NYXVZ2szcW6qaXLpeJMh[2WubDDndo94fGh? NV[1cZYzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
KM-H2 NWXJN|Y5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fGcFUxOCCwTR?= NVrWVoNQOC15MjDo NXrTW3FJcW6qaXLpeJMh[2WubDDndo94fGh? Mn74QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
HDLM-2 M3rHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLHWoI2PTByIH7N NVm3bFdmOC15MjDo M4W1fYlvcGmkaYTzJINmdGxiZ4Lve5Rp NV64bXhxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
L450 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[4[Ic2ODBibl2= MmDBNE04OiCq MXvpcohq[mm2czDj[YxtKGe{b4f0bC=> MoSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
BJAJ MWnBdI9xfG:|aYOgRZN{[Xl? NVXNWm5JPTByIH7N MVSwMVczKGh? M{ezVIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NIe0dIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Ramos M1:0N2Fxd3C2b4Ppd{BCe3OjeR?= M3PNTlUxOCCwTR?= MlTnNE04OiCq NI\oRmtqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> MoXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
Raji MY\BdI9xfG:|aYOgRZN{[Xl? MlTQOVAxKG6P NHv5eYQxNTd{IHi= M1K2Rolv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
Daudi  NF;rSZFCeG:ydH;zbZMhSXO|YYm= MW[1NFAhdk1? MoqwNE04OiCq MYDpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
L428 NF61TpVCeG:ydH;zbZMhSXO|YYm= M{i1NlUxOCCwTR?= MYewMVczKGh? MmnYbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NXTEV3J[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
KM-H2 M2jOTGFxd3C2b4Ppd{BCe3OjeR?= M4LCS|UxOCCwTR?= NXLJbohbOC15MjDo NIS4S4ZqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> MofKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
HDLM-2 NFXxcnRCeG:ydH;zbZMhSXO|YYm= NUjZXVBSPTByIH7N NFLtTo0xNTd{IHi= M2HMfYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M4\sfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
L450 MoHKRZBweHSxc3nzJGF{e2G7 MXi1NFAhdk1? MY[wMVczKGh? M1XtU4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NEm3V3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
SW620 Ml\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT4SWM2OD1zMNMxNk4yKG6P NX;CPGltRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyOFUxQTBpPkKxNlQ2ODlyPD;hQi=>
HCT116 Mki3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTWOWhDTUN3ME2xNeKyOy5|IH7N NEfNfZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK0OVA6OCd-MkGyOFUxQTB:L3G+
MDA-MB-435 M2\aTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPLTG9mOC1zMECwNEBvVQ>? MXSyMVUh\A>? MmHRSG1UVw>? NU\SfXhXUUN3ME2xNlUhdk1? NYTFeFVJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
MDA-MB-468 M1zsbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3OxU|AuOTByMECgcm0> NIDyW4IzNTViZB?= MnHFSG1UVw>? NI\VTndKSzVyPUG0JI5O NE\OVWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG3OVkzPid-MkCxO|U6OjZ:L3G+
MDA-MB-231 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXuNE0yODByMDDuUS=> MlnVNk02KGR? MVTEUXNQ M1T0RWlEPTB;MUC1JI5O M2Gwb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUe1PVI3Lz5{MEG3OVkzPjxxYU6=
BT474 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqwMVExODByIH7N MoWxNk02KGR? M4XmWWROW09? Ml7ZTWM2OD16IH7N MmrHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
MDA-MB-361 MnjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqwMVExODByIH7N NUnrZnU6Oi13IHS= NVXYVVRTTE2VTx?= MYHJR|UxRTdyIH7N MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF5NUmyOkc,OjBzN{W5NlY9N2F-
HER18 M{fsWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX71b3NJOC1zMECwNEBvVQ>? MnXxNk02KGR? M2HQc2ROW09? MXHJR|UxRTJyIH7N NU[2eHdDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
HER18 NIH2blVCeG:ydH;zbZMhSXO|YYm= M33kdVExOCCwTR?= Mn\ZNE8zPC92ODDo M3vuOGROW09? NUe4R|ZscW6mdXPld{BieG:ydH;zbZMh[W6mIILl[JVk\XNiY3zvco9o\W6rYzDwc5RmdnSrYXy= MoqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
MDA-MB-231 NIOzOZdCeG:ydH;zbZMhSXO|YYm= NE\2Tm4yODVibl2= M2fUeFAwOjRxNEigbC=> M{foVmROW09? M{jCOYlv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu NVj6bHQ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
JHH-1 NFLYeWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mli0NE4{6oDVMUCwNOKhdk1? M2K2XlczKGh? M2roXmVEPTB;MUeuOOKyOS5yIH7N NWHaenloRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
JHH-2 M3HLO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfTZ2sxNjQkgKOxNFAxyqCwTR?= MV23NkBp MVvFR|UxRTJzOD6wxtEyOC56IH7N NWLobXl7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
JHH-4 Ml\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIH0TVgxNjQkgKOxNFAxyqCwTR?= M2n3WFczKGh? NEG2[phGSzVyPUG1OU43yrFzNj64JI5O MnXTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HuH-1 NWjSWHR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvNRWZqOC5|4pETNVAxOMLibl2= M1XGTFczKGh? MmHtSWM2OD1{Nz6zxtE2NjBibl2= NUfpPVJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
HuH-6 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnj[GNLOC5|4pETNVAxOMLibl2= NXW4OGV1PzJiaB?= NH3kfXFGSzVyPUOuO:KyOC54IH7N NFLGRYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HuH-7 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVizVmtqOC5|4pETNVAxOMLibl2= NYS1dFlSPzJiaB?= MVLFR|UxRTZwONMxNE4{KG6P MlfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HLE NG\S[IVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPqXncxNjQkgKOxNFAxyqCwTR?= M3f4V|czKGh? NHe2PXpGSzVyPUS1MlnDuTZwNDDuUS=> NXS5RWJvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
HLF NYeyenlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOwMlPjiJNzMECwxsBvVQ>? M3nqb|czKGh? Ml24SWM2OD1zMk[uNeKyOTJwMjDuUS=> NVfITmZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
PLC/PRF/5 NHPFNJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUiwMlPjiJNzMECwxsBvVQ>? M160UlczKGh? M4\DbGVEPTB;N{[uPeKyQS57IH7N NHzOdm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
SK-Hep1 NWTMWId7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\tW5cxNjQkgKOxNFAxyqCwTR?= NFjsN3g4OiCq NVLIZ4hNTUN3ME2yNU46yrFzLkKgcm0> NWOwPXh[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
Hep3B Mn[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jK[|AvO+LCk{GwNFDDqG6P MnzGO|IhcA>? M3viSWVEPTB;Nz62xtEyNjJibl2= NWDY[o5JRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
HepG2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvueVRNOC5|4pETNVAxOMLibl2= MXS3NkBp NHG2UYhGSzVyPUG0MlfDuTFwNzDuUS=> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzM{mzOUc,OTl7MUO5N|U9N2F-
Ramos MlfIRZBweHSxc3nzJGF{e2G7 NHHvSowzPS93MD:xNFAhdk1? MoPpOFghcA>? NX2zfnZxcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ Mm\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6MkOxOlgoRjF7OEKzNVY5RC:jPh?=
Daudi  NUGyXlhySXCxcITvd4l{KEG|c3H5 NIrvNYIzPS93MD:xNFAhdk1? MU[0PEBp MWTpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= MnvCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6MkOxOlgoRjF7OEKzNVY5RC:jPh?=
BALM-14 MXXBdI9xfG:|aYOgRZN{[Xl? MoPJNVIvPS9{NT:1NEBvVQ>? M3WzTFQ5KGh? NWDnZWdocW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ M2XvS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEKzNVY5Lz5zOUiyN|E3QDxxYU6=
BALM-27 NVfXO4l7SXCxcITvd4l{KEG|c3H5 NWrrPJBQOTJwNT:yOU82OCCwTR?= NV3obIRuPDhiaB?= Mkn0bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz M4PT[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEKzNVY5Lz5zOUiyN|E3QDxxYU6=
NB4 MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXaNE4xOS9yLkGvNUDPxE1? M3PwTFQ5KGh? NYXvRW85cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NHW3[Wg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO2O|Q5PCd-MUizOlc1QDR:L3G+
HeLa M{DSN2Z2dmO2aX;uJGF{e2G7 M3TI[FEhfU1? MVmyOEBpenN? M3\1d2lvcGmkaYTpc44hd2ZiYYXyc5JiKEJiYYX0c5Bpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDI[WxiKGOnbHzzJIF1KDFidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmd? M1f2e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNki0OVQ6Lz5{ME[4OFU1QTxxYU6=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
AURKB / pSer10 Histone H3 / TP53 / CDKN1A / MYCN; 

PubMed: 26497213     


Downstream effects of barasertib-induced AURKB inhibition on histone H3 phosphorylation and TP53 protein levels in IMR5 and SK-N-BE (2c) as indicated after 24h (left) and 48h (right). TP53 and its downstream effector CDKN1A were up-regulated by barasertib䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

p53 / p21 / p-p38 / p38 ; 

PubMed: 24782314     


U2OS cells were treated with 50 nm or 100 nm AZD1152 for 24 h. p21, p38, p-p38, and p53 levels were determined by immunoblotting β-actin served as a loading control.

26497213 24782314
Immunofluorescence
p21 ; 

PubMed: 24782314     


U2OS cells were treated as in H. Levels of p21 were analyzed by immunostaining. DNA was counterstained with Hoechst 33258.

24782314
Growth inhibition assay
Cell viability ; 

PubMed: 26497213     


Dose response curves to barasertib at 72h of incubation normalized to the DMSO control sample (mean ± SD, n = 5). The inset depicts the normalized AUCs of each response curve. 

26497213
体内研究 AZD1152 按25 mg/kg剂量单独处理MOLM13移植瘤，显著抑制肿瘤生长，平均肿瘤体积从1261 mm3 降低到 71 mm3，且平均肿瘤重量从583 mg降低到78 mg, 观察到坏死组织被吞噬细胞浸润。[1]此外, AZD1152 每天按10-150 mg/kg剂量处理多种人类实体移植瘤，包括 结肠癌，乳腺癌，和肺癌，显著抑制肿瘤生长，这种作用存在剂量依赖性。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验：[1]
- 合并
  • Cell lines: HL-60, NB4, MOLM13, PALL-2, MV4-11, EOL-1,和 K562
  • Concentrations: 溶于 DMSO, 终浓度为~100 nM
  • Incubation Time: 24或48小时
  • Method: 使用不同浓度AZD1152处理细胞 24或 48小时。通过测量 3H-胸甘摄取（在收集前6小时，加入同位素）而测量细胞增殖，根据剂量-反应曲线计算IC50值。通过流式细胞仪分析细胞周期。通过膜联蛋白V–FITC凋亡检测试剂盒测量细胞凋亡。
    (Only for Reference)
动物实验：[1]
- 合并
  • Animal Models: 皮下注射MOLM13细胞的雌性免疫缺陷BALB/c裸鼠
  • Dosages: 5 或25 mg/kg
  • Administration: 腹腔注射，每周4次，或每隔一天一次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 102 mg/mL (200.96 mM)
Water Insoluble
Ethanol '3 mg/mL
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
 7mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 507.56
化学式

C26H30FN7O3
CAS号 722544-51-6
储存条件 粉状
溶于溶剂
别名 AZD2811, INH-34

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03217838 Active not recruiting Drug: AZD2811|Drug: Azacitidine|Drug: Venetoclax Acute Myeloid Leukaemia AstraZeneca July 31 2017 Phase 1|Phase 2
NCT02579226 Completed Drug: AZD2811 Advanced Solid Tumours AstraZeneca October 28 2015 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1：

    Can you let me know what solvent I can use for Barasertib, cat # S1147, for in vivo use? (IP injection in mice)

  • 回答：

    S1147 Barasertib (AZD1152-HQPA) can be dissolved in 30% PEG400/0.5% Tween80/5% Propylene glycol at 30mg/ml as a clear solution. Usually, when prepare the solution, we will add organic solvents first, then add Tween 80, then water. But this compound can not dissolve in 30% PEG400/0.5% Tween80/5% Propylene glycol clearly. After water was added, it became a clear solution.

Selleck产品目录册

Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

  • 泛Aurora Kinase抑制剂

    Danusertib (PHA-739358) : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=13 nM/79 nM/61 nM.

  • 泛Aurora Kinase抑制剂

    SNS-314 Mesylate : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=9 nM/31 nM/3 nM.

  • 活性最高的Aurora Kinase抑制剂

    MK-5108 (VX-689) : Aurora A, IC50=0.064 nM.

  • 用于临床的Aurora Kinase抑制剂

    Alisertib (MLN8237) : Phase III for Relapsed/Refractory Peripheral T-Cell Lymphoma.

  • 经典的Aurora Kinase抑制剂

    Hesperadin : Potently inhibits Aurora B with IC50 of 250 nM.

相关Aurora Kinase产品

  • Ro-3306 New

    RO-3306是一种ATP竞争性的选择性 CDK1 抑制剂，Ki 为20 nM，选择性是其他各种人类激酶的15倍多。RO-3306可增强p53介导的 Bax 激活和线粒体的凋亡。

  • ML141 New

    ML141 (CID-2950007) 是 Rho 家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。 ML141 与 p38 激活增加有关，并可能诱导p38依赖性凋亡/衰老。ML141还可保护神经母细胞瘤细胞免受二甲双胍(metformin)诱导的凋亡。

  • Salirasib New

    Salirasib (Farnesylthiosalicylic acid, FTS)是一种有效的竞争性prenylated protein methyltransferase (PPMTase)抑制剂， Ki为2.6 μM，其抑制Ras甲基化。Salirasib 具有抗肿瘤的活性并可诱导凋亡。Phase 2。

  • Alisertib (MLN8237)

    Alisertib (MLN8237)是一种选择性Aurora A抑制剂，无细胞试验中IC50为1.2 nM，作用于Aurora A比作用于Aurora B选择性强200倍以上。Alisertib 可诱导细胞周期阻滞、细胞凋亡与自噬。Phase 3。

    Features:MLN8237 是第一个口服有效的小分子Aurora A激酶选择性抑制剂。

  • Tozasertib (VX-680, MK-0457)

    Tozasertib (VX-680, MK-0457)是一种pan-Aurora抑制剂，对Aurora A作用最强，无细胞试验中Kiapp为0.6 nM，而对Aurora B/Aurora C的作用较弱，对Aurora A选择性比其他55种激酶高100倍。唯二的例外是 Fms-related tyrosine kinase-3 (FLT-3) 和 BCR-ABL tyrosine kinase，也可被 Tozasertib 抑制，对应的Ki值均为30 nM和30 nM。Tozasertib 可诱导凋亡和自噬。Phase 2。

  • Danusertib (PHA-739358)

    Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C，无细胞试验中IC50为13 nM/79 nM/61 nM，适度有效作用于Abl，TrkA，c-RET和FGFR1，对Lck，VEGFR2/3，c-Kit，CDK2等作用效果稍弱。Danusertib 可诱导凋亡、细胞周期阻滞和自噬。Phase 2。

  • ZM 447439

    ZM 447439是一种选择性的，ATP竞争性Aurora A和Aurora B抑制剂，IC50分别为110 nM和130 nM，作用于Aurora A/B比作用于MEK1， Src， Lck选择性高8倍，对CDK1/2/4， Plk1， Chk1等几乎没有作用效果。

    Features:ZM-447439是Aurora选择性ATP竞争性抑制剂

  • MLN8054

    MLN8054是一种有效的，选择性Aurora A抑制剂，在Sf9昆虫细胞中IC50为4 nM，作用于Aurora A比作用于Aurora B选择性高40倍。Phase 1。

    Features:MLN8054是有效的 Aurora A激酶选择性抑制剂。

  • MK-5108 (VX-689)

    MK-5108 (VX-689)是一种高选择性的Aurora A抑制剂，无细胞试验中IC50为0.064 nM，作用于Aurora A比作用于Aurora B/C选择性高220和190倍，作用于TrkA的选择性低100倍。MK-5108 (VX-689) 可诱导自噬。Phase 1。

  • Aurora A Inhibitor I (TC-S 7010)

    Aurora A Inhibitor I (TC-S 7010) 是一种新型有效的，选择性Aurora A抑制剂，无细胞试验中IC50为3.4 nM，作用于Aurora A比作用于Aurora B选择性高1000倍。Aurora A Inhibitor I (TC-S 7010) 可通过ROS介导的UPR信号通路来触发凋亡。

    Features:Aurora A Inhibitor I 是2,4-二苯胺嘧啶抑制剂。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID