| 货号 | 17554-50mg |
| 描述 | Carfilzomib is a second-generation, irreversible, peptide epoxyketone class proteasome inhibitor that targets the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM) with minimal cross reactivity to other proteases.1,2 It can induce cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, lymphoma, and various solid tumors (IC50s = 2.4-20 nM).3,4 |
| 别名 | PR-171; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Dou, Q.P. and Zonder, J.A. Overview of proteasome inhibitor-based anti-cancer therapies: Perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system. Curr. Cancer Drug Targets 14(6), 517-536 (2014). 2.Zhou, H.J.,Aujay, M.A.,Bennett, M.K., et al. Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J. Med. Chem. 52(9), 3028-3038 (2009). 3.Zhang, W. and Sidhu, S.S. Development of inhibitors in the ubiquitination cascade. FEBS Letters 588(2), 356-367 (2014). 4.Demo, S.D.,Kirk, C.J.,Aujay, M.A., et al. Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. Cancer Res. 67(13), 6383-6391 (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 | 719.9 |
| 分子式 | C40H57N5O7 |
| CAS号 | 868540-17-4 |
| 稳定性 | ≥ 2 years |
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