GSK-1070916
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.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18929387
| Cas No. |
942918-07-2 |
|---|---|
| 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 |
| Appearance |
Yellow to off white powder |
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.
