| 货号 | 10459-25mg |
| 描述 | PKC 412 is a cell-permeable, reversible inhibitor of several serine/threonine and tyrosine kinases, including conventional PKC isoforms (α, β, and γ), Syk, FLK1, Akt, PKA, c-Kit, C-Fgr, c-Src, FLT3, PDFRβ, VEGFR1, and VEGFR2 with IC50 values ranging from 80-500 nM.1,2,3,4 It also upregulates the expression of endothelial nitric oxide synthase (eNOS) in mice.5 PKC 412 inhibits growth or induces apoptosis in many cancer cell types, blocks angiogenesis in tumors, and sensitizes cancer cells to ionizing radiation, supporting its use in cancer therapy.1,6,7 |
| 别名 | N-Benzoylstaurosporine;CGP 41231;CGP 41251;Midostaurin; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Fabbro, D.,Buchdunger, E.,Wood, J., et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent. Pharmacology & Therapeutics 82, 293-301 (1999). 2.Ozaki, H.,Seo, M.S.,Ozaki, K., et al. Blockade of vascular endothelial cell growth factor receptor signaling is sufficient to completely prevent retinal neovascularization. American Journal of Pathology 156(2), 697-707 (2000). 3.Tenzer, A.,Zingg, D.,Rocha, S., et al. The phosphatidylinositide 3-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C. Cancer Research 61, 8203-8210 (2001). 4.Andrejauskas-Buchdunger, E. and Regenass, U. Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251. Cancer Research 52, 5353-5358 (1992). 5.Li, H.,Hergert, S.M.,Schäfer, S.C., et al. Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse. Nitric Oxide: Biology and Chemistry 12, 231-236 (2005). 6.Marmy-Conus, N.,Hannan, K.M. and Pearson, R.B. Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70s6k/p85s6k : Implications for the analysis of S6K signalling. FEBS Letters 519, 135-140 (2002). 7.El Fitori, J.,Su, Y.,Büchler, P., et al. PKC412 small-molecule tyrosine kinase inhibitor: Single-compound therapy for pancreatic cancer. Cancer 110, 1457-1468 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 570.6 |
| 分子式 | C35H30N4O4 |
| CAS号 | 120685-11-2 |
| 稳定性 | ≥ 2 years |
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