| 货号 | 18130-1mg |
| 描述 | UCN-01 is a synthetic derivative of staurosporine (Item No. 81590) with antiproliferative activity against several in vitroandin vivo cancer models. It inhibits a variety of kinases, including Akt, protein kinase C (IC50 = 30 nM), PDK1 (IC50 = 6 nM) and cyclin-dependent kinases (IC50s = 300-600 nM for Cdk1 and Cdk2).1,2,3 UCN-01 arrests tumor cells in the G1/S phase of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase Chk1 (IC50 = 7 nM), leading to apoptosis.1,4,5,6 |
| 别名 | NSC 638850;7-hydroxy Staurosporine; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kawabe, T. G2 checkpoint abrogators as anticancer drugs. Molecular Cancer Therapeutics 3(4), 513-519 (2004). 2.Peifer, C., and Alessi, D.R. Small-molecule inhibitors of PDK1. ChemMedChem 3(12), 1810-1838 (2008). 3.Senderowicz, A.M., and Sausville, E.A. Preclinical and clinical development of cyclin-dependent kinase modulators. Journal of the National Cancer Institute 92(5), 376-387 (2000). 4.Wang, Q.,Fan, S.,Eastman, A., et al. UCN-01: A potent abrogator of G2 checkpoint function in cancer cells with disrupted p53. Journal of the National Cancer Institute 88(14), 956-965 (1996). 5.Yamauchi, T.,Keating, M.J., and Plunkett, W. UCN-01 (7-hydroxystaurosporine) inhibits DNA repair and increases cytotoxicity in normal lymphocytes and chronic lymphocytic leukemia lymphocytes. Molecular Cancer Therapeutics 1, 287-294 (2002). 6.Facchinetti, M.M.,De Siervi, A.,Toskos, D., et al. UCN-01-induced cell cycle arrest requires the transcriptional induction of p21waf1/cip1 by activation of mitogen-activated protein/extracellular signal-regulated kinase kinase/extracellular signal-regulated kinase pathway. Cancer Research 64, 3629-3637 (2004). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥99% |
| 计算分子量 | 482.5 |
| 分子式 | C28H26N4O4 |
| CAS号 | 112953-11-4 |
| 稳定性 | ≥ 2 years |
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