基本属性 生物活性体外研究体内研究 用途与合成方法 供应商 相关产品
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GSK1070916

基本属性 生物活性体外研究体内研究 用途与合成方法 供应商 相关产品
GSK1070916
GSK1070916 性质
  • 密度 1.21
GSK1070916 用途与合成方法
  • 生物活性GSK1070916是一种可逆的,ATP竞争性的Aurora B/C抑制剂,IC50为3.5 nM/6.5 nM,比作用于紧密相关的Aurora A-TPX2复合体选择性高100倍以上。 Phase 1。
  • 体外研究GSK1070916 selectively inhibits Aurora B and Aurora C with Ki of 0.38 nM and 1.5 nM over Aurora A with Ki of 490 nM. Inhibition of Aurora B and Aurora C is time-dependent, with an enzyme-inhibitor dissociation half-life of >480 min and 270 min respectively. In addition, GSK1070916 is also a competitive inhibitor with respect to ATP. Human tumor cells treated with GSK1070916 shows dose-dependent inhibition of phosphorylation on serine 10 of Histone H3, a substrate specific for Aurora B. Moreover, GSK1070916 inhibits the proliferation of tumor cells with EC50 values of <10 nM in over 100 cell lines spanning a broad range of tumor types, with a median EC50 of 8 nM. Although GSK1070916 has potent activity against proliferating cells, a dramatic shift in potency is observed in primary, nondividing, normal human vein endothelial cells. Furthermore, GSK1070916-treated cells do not arrest in mitosis but instead fails to divide and become polyploid, ultimately leading to apoptosis. In another study, it is also reported high chromosome number associated with resistance to the inhibition of Aurora B and C suggests cells with a mechanism to bypass the high ploidy checkpoint are resistant to GSK1070916.
  • 体内研究GSK1070916 (25, 50, or 100 mg/kg) shows dose-dependent inhibition of phosphorylation of an Aurora B–specific substrate in mice and consistent with its broad cellular activity, has antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models.
GSK1070916供应商更多
  • 公司名称:上海波以尔化工有限公司
  • 联系电话:86-15221043597
  • 产品介绍: 中文名称:N'-[4-[4-[2-[3-[(二甲基氨基)甲基]苯基]-1H-吡咯并[2,3-B]吡啶-4-基]-1-乙基-1H-吡唑-3-基]苯基]-N,N-二甲基脲
    英文名称:N'-4-4-2-3-(Dimethylamino)methylphenyl-1H-pyrrolo2,3-bpyridin-4-yl-1-ethyl-1H-pyrazol-3-ylphenyl-N,N-dimethylurea
    CAS:942918-07-2
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  • 公司名称:上海佰世凯化学科技有限公司
  • 联系电话:+86(0)21-20908456
  • 产品介绍: 英文名称:GSK 1070916
    CAS:942918-07-2
    备注:C14668
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  • 公司名称:上海景颜化工科技有限公司
  • 联系电话:13817811078,021-50426030
  • 产品介绍: 英文名称:GSK1070916
    纯度:98%
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  • 公司名称:凯方医药科技(上海)有限公司
  • 联系电话:021-67220633 & 021-37212706
  • 产品介绍: 英文名称:3-(4-(4-(2-(3-((DiMethylaMino)Methyl)phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-ethyl-1H-pyrazol-3-yl)phenyl)-1,1-diMethylurea
    CAS:942918-07-2
    纯度:99% 包装信息:5KG;1KG
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  • 公司名称:武汉永璨生物科技有限公司
  • 联系电话:0086-27-5925 3327; QQ:40199614
  • 产品介绍: 英文名称:GSK1070916
    CAS:942918-07-2
    纯度:98% 包装信息:1g,5g,10g,50g 备注:only used for research
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"GSK1070916"相关产品信息