化学性质:
规格 | 10mM (in 1mL DMSO)5mg 10mg 50mg 200mg |
CAS | 94 |
别名 |
|
化学名 | 3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea |
分子式 | C30H33N7O |
分子量 | 507.63 |
溶解度 | >25.4mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
GSK1070916 is a potent and selective inhibitor of Aurora B/C Kinase with Ki values of 0.38nM and 1.5nM, respectively [1].
GSK1070916 is a reversible ATP-competitive inhibitor of Aurora B and Aurora C with Ki values of 0.38nM and 1.5nM, respectively. The SPA assay shows GSK1070916 has a good selectivity over Aurora A. It inhibits Aurora B with IC50 value of 5nM but 1259nM for Aurora A. It is also reported that treatment of GSK1070916 suppresses cell proliferation in A549 human lung cancer cells with EC50 value of 7nM. Moreover, both in vitro and in vivo assays demonstrate GSK1070916 can inhibit the phosphorylation of histone H3, which is a substrate of Aurora B. GSK1070916 can also suppress tumor growth in mice with HL-60 tumor xenografts [1].
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标签:GSK1070916
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