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GSK-1070916

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Chemical Structure| 942918-07-2 同义名 : GSK-1070916A
CAS号 : 942918-07-2
货号 : A600112
分子式 : C30H33N7O
纯度 : 99%
分子量 : 507.629
MDL号 : MFCD22420815
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(31.52 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Aurora B

    Aurora B-INCENP, IC50:3.5 nM

  • Aurora C

    Aurora C-INCENP, IC50:6.5 nM
描述 GSK-1070916 effectively inhibits Aurora B/INCENP and Aurora C/INCENP kinases with dissociation constants (Kis) of 0.38±0.29 nM and 1.45±0.35 nM, respectively, demonstrating lesser potency against Aurora A/TPX2 with a Ki of 492±61 nM. Additionally, this compound shows inhibitory activity against FLT1, TIE2, SIK, FLT4, and FGFR1, with IC50 values of 42, 59, 70, 74, and 78 nM, respectively. In A549 human lung cancer cells, GSK-1070916 exhibits a strong antiproliferative effect, with an EC50 of 7 nM[1]. GSK-1070916 has been tested across a range of tumor cell lines, showing consistent inhibition of the phosphorylation of histone H3 at serine 10 (HH3-S10), with average EC50 values spanning from 8 to 118 nM[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A549 cells Proliferation assay 6-7 d Antiproliferative activity against human A549 cells after 6 to 7 days by celltiter-glo luminescence assay in absence of 70% human serum albumin, EC50=0.007 μM 20420387
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01118611 Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 << Phase 1 Completed - United Kingdom ... 展开 >> Leeds Cancer Centre at St. James's University Hospital Leeds, England, United Kingdom, LS9 7TF Barts and the London School of Medicine London, England, United Kingdom, EC1M 6BQ 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.98mL

19.70mL

3.94mL

1.97mL
参考文献

[1]Adams ND, et al. Discovery of GSK-1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.

[2]Hardwicke MA, et al. GSK-1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol Cancer Ther. 2009 Jul;8(7):1808-17.