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GSK1070916

Cat No.
CEI-1354
Description
GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B and C with IC50 value of 3.5 nM and 6.5 nM, respectively.
Product Overview
GSK1070916 is a potent and selective inhibitor of Aurora B/C Kinase with Ki values of 0.38nM and 1.5nM, respectively. 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.
CAS No.
942918-07-2
Molecular Weight
507.63
Purity
0.98
Storage
Store at -20°C
Targets
Aurora B; Aurora C
IC50
3.5 nM; 6.5 nM
Molecular Formula
C30H33N7O
Chemical Name
3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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