| 货号 | 17385-1mg |
| 描述 | Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.1 BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM).2,3 It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice.2 It shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.4 BI-2536 is also an inhibitor of BRD4 (IC50 = 25 nM), suppressing BRD4-dependent c-Myc expression in MM.1S multiple myeloma cells.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Schöffski, P. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist 14(6), 559-570 (2009). 2.Steegmaier, M.,Hoffmann, M.,Baum, A., et al. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Current Biology 17(4), 316-322 (2007). 3.Peifer, C. and Alessi, D.R. Small-molecule inhibitors of PDK1. ChemMedChem 3(12), 1810-1838 (2008). 4.Danovi, D.,Folarin, A.,Gogolok, S., et al. A high-content small molecule screen identifies sensitivity of glioblastoma stem cells to inhibition of polo-like kinase 1. PLoS One 8(10), 1-13 (2013). 5.Ciceri, P.,Müller, S.,OMahony, A., et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nature Chemical Biology 10(4), 305-312 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 521.7 |
| 分子式 | C28H39N7O3 |
| CAS号 | 755038-02-9 |
| 稳定性 | ≥ 2 years |
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