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GSK-1070916 is an inhibitor of aurora kinases B and C (AurB/C) that exhibits anticancer chemotherapeutic activity. GSK-1070916 prevents AurB from phosphorylating serine 10 of histone H3. In cellular and animal models of lung cancer, GSK-1070916 inhibits cellular proliferation and induces tumor regression. In models of colon cancer, breast cancer, and leukemia, this compound inhibits cell division, induces apoptosis, and suppresses tumor growth.
| Cas No. | 942918-07-2 |
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| Purity | ≥98% |
| Formula | C30H33N7O |
| Formula Wt. | 507.63 |
| IUPAC Name | 3-{4-[4-(2-{3-[(Dimethylamino)methyl]phenyl}-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-ethyl-1H-pyrazol-3-yl]phenyl}-1,1-dimethylurea |
| Synonym | GSK1070916 |
| Solubility | DMSO 93 mg/mL (183.2 mM) Ethanol 8 mg/mL (15.75 mM) Water Insoluble |
| Appearance | Yellow to off white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Adams ND, Adams JL, Burgess JL, et al. Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001. PMID: 20420387.
Hardwicke MA, Oleykowski CA, Plant R, et al. GSK1070916, 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. PMID: 19567821.