GSK1070916   Click here for help

GtoPdb Ligand ID: 8358

Synonyms: compound 17k [PMID 20420387] | GSK-1070916
Compound class: Synthetic organic
Comment: GSK1070916 is reported to be an ATP-competitive, potent and selective inhibitor of Aurora kinases B and C [1].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 6
Hydrogen bond donors 2
Rotatable bonds 9
Topological polar surface area 82.08
Molecular weight 507.27
XLogP 5.11
No. Lipinski's rules broken 1
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Canonical SMILES CCn1nc(c(c1)c1ccnc2c1cc([nH]2)c1cccc(c1)CN(C)C)c1ccc(cc1)NC(=O)N(C)C
Isomeric SMILES CCn1nc(c(c1)c1ccnc2c1cc([nH]2)c1cccc(c1)CN(C)C)c1ccc(cc1)NC(=O)N(C)C
InChI InChI=1S/C30H33N7O/c1-6-37-19-26(28(34-37)21-10-12-23(13-11-21)32-30(38)36(4)5)24-14-15-31-29-25(24)17-27(33-29)22-9-7-8-20(16-22)18-35(2)3/h7-17,19H,6,18H2,1-5H3,(H,31,33)(H,32,38)
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Summary of Clinical Use Click here for help
One Phase 1 clinical trial assessing GSK1070916 in patients with advanced solid tumors has been completed (see NCT01118611).
Mechanism Of Action and Pharmacodynamic Effects Click here for help
The Aurora kinases are essential components involved in the regulation of mitosis [2]. These enzymes are frequently overexpressed or amplified in human tumours. Small molecule Aurora kinase inhibitors are therefore being sought as cancer chemotherapeutics [3-4].
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01118611 Aurora B/C Kinase Inhibitor GSK1070916A in Treating Patients With Advanced Solid Tumors Phase 1 Interventional Cancer Research UK