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Background Information:
GSK1070916 is a potent, selective and ATP competitive inhibitor of Aurora B and C kinases with Ki values of 0.38 and 1.5 nM, respectively, and is highly selective over Aurora A (Ki = 490 nM). Its inhibition of Aurora B and C is time-dependent, with an enzyme-inhibitor dissociation half-life of >480 min and 270 min respectively, a unique feature compared to other Aurora B Kinase inhibitors under clinical development. It is selective over other kinase targets with an exception of of FLT1, TIE2, SIK, FLT4, and FGFR1 (with IC50 values of 42, 59, 70, 74, and 78 nM, respectively). It is currently in clinical development.
Reference:
1. N. D. Adams, et al., Discovery of GSK1070916, a Potent and Selective Inhibitor of Aurora B/C Kinase, J. Med. Chem., 2010, 53 (10), pp 3973–4001.
2. K. Anderson, et al, Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time, Biochem. J. (2009) 420 (259–265).
APIM050161: GSK-1070916 (NMI-900)
CAS No.: 942918-07-2.
Molecular Formula: C30H33N7O • H2O.
Molecular Weight: 525.6.
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, and Quatitative Elemental Analysis.
Solubility: In DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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