| 货号 | 18269-1mg |
| 描述 | BIIB021 is a potent, orally-available inhibitor of Hsp90 (Ki = 1.7 nM) that induces the degradation of oncoproteins, including HER2 (EC50 = 38 nM), while up-regulating the expression of Hsp70 and Hsp27.1,2 It is cytotoxic to cancer cells and, when administered orally to mice, inhibits growth of xenograft tumors.1,2,3 BIIB021 suppresses growth in various lymphoma cells but not in normal lymphocytes and induces apoptosis in a myelodysplastic syndrome cell line.4,5,3 |
| 别名 | CNF2024; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kasibhatla, S.R.,Hong, K.,Biamonte, M.A., et al. Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. Journal of Medicinal Chemistry 50(12), 2767-2778 (2007). 2.Lindgren, K.,Zhang, H.,Brekken, J., et al. BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Molecular Cancer Therapeutics 8(4), 921-929 (2009). 3.Lin, S.,Li, J.,Zhou, W., et al. BIIB021, an Hsp90 inhibitor, effectively kills a myelodysplastic syndrome cell line via the activation of caspases and inhibition of PI3K/Akt and NF-κB pathway proteins. Exp.Ther.Med. 7, 1539-1544 (2014). 4.Böll, B.,Eltaib, F.,Reiners, K.S., et al. Heat shock protein 90 inhibitor BIIB021 (CNF2024) depletes NF-kappaB and sensitizes Hodgkin’s lymphoma cells for natural killer cell-mediated cytotoxicity. Clinical Cancer Research 15(16), 5108-5116 (2009). 5.Suzuki, M.,Takeda, T.,Nakagawa, H., et al. The heat shock protein 90 inhibitor of BIIB021 suppresses the growth of T and natural killer cell lymphomas. Frontiers in Microbiology 6(280), 1-10 (2015). | |
| 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 | 318.8 |
| 分子式 | C14H15ClN6O |
| CAS号 | 848695-25-0 |
| 稳定性 | ≥ 2 years |
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