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
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客户使用Selleck生产的Barasertib (AZD1152-HQPA)发表文献95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 MoDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[xNE02ODBibl2= MoP5OFjDqGh? NHOzW|JKSzVyPUK1JI5O MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ5N{[1PUc,OjV{N{e2OVk9N2F-
LNCaP NV3Ud|Q4SXCxcITvd4l{KEG|c3H5 NFHmWYExNTVyMDDuUS=> MUC0POKhcA>? MkTMbY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bEB1cHKxdXfoJINie3Cjc3WtN{B2eHKnZ4XsZZRqd25? NIe1Vo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3O|Y2QSd-MkWyO|c3PTl:L3G+
LNCaP NXzzWG1OTnWwY4Tpc44hSXO|YYm= NWrkfXdtPTBibl2= MX60PEBp M4LQdIlv\HWlZYOgcYlkem:wdXPs[Ykhf2m2aDDhcoV2\2WwaXOgcYVkcGGwaYPt NIXQU5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3O|Y2QSd-MkWyO|c3PTl:L3G+
Ramos MXvGeY5kfGmxbjDBd5NigQ>? M2Ljd|UxOCCwTR?= MUWwMVczKGh? M4DCPYlvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= M1G5VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
Daudi  NHvSNJhHfW6ldHnvckBCe3OjeR?= MVK1NFAhdk1? M1vrTVAuPzJiaB?= NX\4eZp[cW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl M4jaSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
L540 MoLBSpVv[3Srb36gRZN{[Xl? MnyyOVAxKG6P MofpNE04OiCq MXLpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? M4[0VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
BJAJ NIrHb4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDjNIM2ODBibl2= M1yyZlAuPzJiaB?= NXrmS|U6cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NIrwUoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Ramos M3\yfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYL3PFJ4PTByIH7N Ml7rNE04OiCq MnnmbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MnXkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
Raji NWrXZo5VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDCRY9jPTByIH7N NIW5T20xNTd{IHi= M{LkPYlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NF:zSYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Daudi  M3XsR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\iPGhsPTByIH7N NWPpe4R5OC15MjDo NEPXV2VqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MkLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
L428 M3y2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnj5OVAxKG6P Mnv6NE04OiCq NFu3VFhqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MkT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
KM-H2 M1\OR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3ZXHI2ODBibl2= NWLKPXNROC15MjDo MXrpcohq[mm2czDj[YxtKGe{b4f0bC=> NH3PSHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
HDLM-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHYOVAxKG6P MlLaNE04OiCq M4fnTolvcGmkaYTzJINmdGxiZ4Lve5Rp M4HPblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
L450 MlfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[yXlJkPTByIH7N Ml;GNE04OiCq NHn2OoRqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmPJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
BJAJ NWexfm9mSXCxcITvd4l{KEG|c3H5 MVy1NFAhdk1? M{TOVFAuPzJiaB?= MUXpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NF7qcnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Ramos Mn\kRZBweHSxc3nzJGF{e2G7 NXnMUnB[PTByIH7N NXvIUFJOOC15MjDo MnvQbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NYXZc|IzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
Raji NUToXYJmSXCxcITvd4l{KEG|c3H5 MoexOVAxKG6P MWKwMVczKGh? NHLGUJBqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NXLRTYhLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
Daudi  NF3DV5NCeG:ydH;zbZMhSXO|YYm= NEnvVZo2ODBibl2= NIXQV2UxNTd{IHi= M3:yXIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M2TTclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
L428 NHXuXmxCeG:ydH;zbZMhSXO|YYm= M4fLe|UxOCCwTR?= MVqwMVczKGh? MoHpbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NUnZUmlURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
KM-H2 NXvJWoZzSXCxcITvd4l{KEG|c3H5 M1TpWVUxOCCwTR?= MUWwMVczKGh? MmDHbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
HDLM-2 NHu3R4FCeG:ydH;zbZMhSXO|YYm= MUC1NFAhdk1? MmnyNE04OiCq MkDibY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NVjXRY9ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
L450 NIDwU3FCeG:ydH;zbZMhSXO|YYm= M{PHRlUxOCCwTR?= M4nmfVAuPzJiaB?= M4TP[Ilv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M1K5PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
SW620 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTrWJhWTUN3ME2xNOKyOi5zIH7N M3Hn[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkS1NFkxLz5{MUK0OVA6ODxxYU6=
HCT116 M3\IXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3GxXGVEPTB;MUJCtVMvOyCwTR?= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ2NUC5NEc,OjF{NEWwPVA9N2F-
MDA-MB-435 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S5b|AuOTByMECgcm0> MkK1Nk02KGR? NWX1VIt7TE2VTx?= NHztPIdKSzVyPUGyOUBvVQ>? NUPucZczRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
MDA-MB-468 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPRNE0yODByMDDuUS=> MV[yMVUh\A>? M3rFb2ROW09? NF;OfmtKSzVyPUG0JI5O MmS5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
MDA-MB-231 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PkT|AuOTByMECgcm0> MU[yMVUh\A>? MU\EUXNQ NFXzNWdKSzVyPUGwOUBvVQ>? NX3rO|lpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
BT474 MnLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXywMVExODByIH7N NXe4elFMOi13IHS= MWXEUXNQ M3L3[2lEPTB;ODDuUS=> NXnwdnlvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
MDA-MB-361 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVSwMVExODByIH7N M4mzXlIuPSCm NWi3OWJSTE2VTx?= NGXRdXpKSzVyPUewJI5O MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF5NUmyOkc,OjBzN{W5NlY9N2F-
HER18 NWXpU49wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPnNE0yODByMDDuUS=> M3HTPVIuPSCm M4DjNWROW09? NILXdZJKSzVyPUKwJI5O NXrCe4FFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
HER18 Mo\mRZBweHSxc3nzJGF{e2G7 MofVNVAxKG6P NF\mS|IxNzJ2L{S4JIg> MnPSSG1UVw>? MUnpcoR2[2W|IHHwc5B1d3OrczDhcoQhemWmdXPld{BkdG:wb3flcolkKHCxdHXueIlidA>? Mo\3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
MDA-MB-231 NHzyRoVCeG:ydH;zbZMhSXO|YYm= NIfkXWgyODVibl2= MVWwM|I1NzR6IHi= NFT1U2FFVVOR M2\xWIlv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF5NUmyOkc,OjBzN{W5NlY9N2F-
JHH-1 NX6wclFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSwMlPjiJNzMECwxsBvVQ>? NY\xOVlqPzJiaB?= NYXSeXZnTUN3ME2xO{41yrFzLkCgcm0> MnjWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
JHH-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnv5NE4{6oDVMUCwNOKhdk1? M4WxTVczKGh? M1ewUWVEPTB;MkG4MlDDuTFyLkigcm0> MnTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
JHH-4 MmDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\jNmp2OC5|4pETNVAxOMLibl2= M3TqbVczKGh? NHnwZlBGSzVyPUG1OU43yrFzNj64JI5O NH7XbVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HuH-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHINmJ[OC5|4pETNVAxOMLibl2= NUjhe4RCPzJiaB?= M4XWfmVEPTB;MkeuN:KyPS5yIH7N NYfqOndrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
HuH-6 NWTFXlNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;DNE4{6oDVMUCwNOKhdk1? MUO3NkBp MlPwSWM2OD1|LkhCtVAvPiCwTR?= M2i5VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUGzPVM2Lz5zOUmxN|k{PTxxYU6=
HuH-7 MlnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDpNE4{6oDVMUCwNOKhdk1? MYq3NkBp NXz5c4hiTUN3ME22MljDuTBwMzDuUS=> NGfab5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HLE NVPOXlA1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXwT3M6OC5|4pETNVAxOMLibl2= M{LmWFczKGh? NYWxW|BzTUN3ME20OU46yrF4LkSgcm0> NWHsOYRQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
HLF NW[yWVRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MormNE4{6oDVMUCwNOKhdk1? MmGwO|IhcA>? Mn;hSWM2OD1zMk[uNeKyOTJwMjDuUS=> NUjVW3BoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
PLC/PRF/5 M2TKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofaNE4{6oDVMUCwNOKhdk1? MU[3NkBp MYDFR|UxRTd4LkpCtVkvQSCwTR?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzM{mzOUc,OTl7MUO5N|U9N2F-
SK-Hep1 MknDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIL0OIsxNjQkgKOxNFAxyqCwTR?= MkfGO|IhcA>? M4\VS2VEPTB;MkGuPeKyOS5{IH7N NY[1bZVuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
Hep3B M{DVWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHqbXUxNjQkgKOxNFAxyqCwTR?= NH\VZ2I4OiCq MX3FR|UxRTdwNtMxNU4zKG6P NGL2UXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HepG2 MkjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4qzPVAvO+LCk{GwNFDDqG6P NFfxOYM4OiCq NIPrR5hGSzVyPUG0MlfDuTFwNzDuUS=> NFTlfVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
Ramos MXfBdI9xfG:|aYOgRZN{[Xl? MlHQNlUwPTBxMUCwJI5O M{LxbFQ5KGh? M3uzc4lv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> NWm0ZnJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4NlMyPjhpPkG5PFI{OTZ6PD;hQi=>
Daudi  NIGxT2tCeG:ydH;zbZMhSXO|YYm= NUDtbWJWOjVxNUCvNVAxKG6P NGn3Wno1QCCq NHrG[FhqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> M4KyclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEKzNVY5Lz5zOUiyN|E3QDxxYU6=
BALM-14 NIj2SYZCeG:ydH;zbZMhSXO|YYm= MkPYNVIvPS9{NT:1NEBvVQ>? M4HvdFQ5KGh? Moj1bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz NUnRV3U6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4NlMyPjhpPkG5PFI{OTZ6PD;hQi=>
BALM-27 NYDhV3N[SXCxcITvd4l{KEG|c3H5 NFr5cpUyOi53L{K1M|UxKG6P MV20PEBp M3;jT4lv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> MlvTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6MkOxOlgoRjF7OEKzNVY5RC:jPh?=
NB4 MkHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofONE4xOS9yLkGvNUDPxE1? NFmwSJI1QCCq MkLkbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NUTkVYZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOlc1QDRpPkG4N|Y4PDh2PD;hQi=>
HeLa MWPGeY5kfGmxbjDBd5NigQ>? MnKxNUB2VQ>? NF[4cWwzPCCqcoO= MmfxTY5pcWKrdHnvckBw\iCjdYLvdoEhSiCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFjlUIEh[2WubIOgZZQhOSC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0eIlv\w>? M1PqRVxiKHSjcnfleF0oZ2KuYX7rK{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 Terminated Drug: AZD2811|Drug: Azacitidine|Drug: Venetoclax Acute Myeloid Leukaemia AstraZeneca November 27 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