| 货号 | 18498-50mg |
| 描述 | Regorafenib is an orally-bioavailable multi-kinase inhibitor that is structurally related to sorafenib (BAY 43-9006; Item No. 10009644), another multi-kinase inhibitor with applications in cancer.1 Regorafenib inhibits c-Raf, B-Raf, VEGFR1, VEGFR2, VEGFR3, Tie2, PDGFRβ, FGFR1, c-Kit, and RET with IC50 values of 2.5, 28, 13, 4.2, 46, 311, 22, 202, 7, and 1.5 nM, respectively, as well as other kinases.1,2,3 It also inhibits soluble epoxide hydrolase (IC50 = 0.5 nM).4 Regorafenib has value against a range of cancers, including advanced colorectal cancer.5 |
| 别名 | BAY 73-4506; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Wilhelm, S.M.,Dumas, J.,Adnane, L., et al. Regorafenib (BAY 73-4506): A new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. International Journal of Cancer 129(1), 245-255 (2011). 2.Uitdehaag, J.C.M.,de Roos, J.A.D.M.,van Doornmalen, A.M., et al. Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use. PLoS One 9(3), 1-13 (2014). 3.Ravi, S., and Singal, A.K. Regorafenib: An evidence-based review of its potential in patients with advanced liver cancer. Core Evid. 9, 81-87 (2014). 4.Hwang, S.H.,Wecksler, A.T.,Zhang, G., et al. Synthesis and biological evaluation of sorafenib - and regorafenib-like sEH inhibitors. Bioorganic & Medicinal Chemistry Letters 23(13), 3732-3737 (2013). 5.Sastre, J.,Argiles, G.,Benavides, M., et al. Clinical management of regorafenib in the treatment of patients with advanced colorectal cancer. Clin.Transl.Oncol. 16, 942-953 (2014). | |
| 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 | 482.8 |
| 分子式 | C21H15ClF4N4O3 |
| CAS号 | 755037-03-7 |
| 稳定性 | ≥ 2 years |
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