| 货号 | 11746-1mg |
| 描述 | Farnesyltransferase drives the post-translational farnesylation of a number of target proteins, including Ras, a component of the MAPK and Akt signaling pathways involved in cell proliferation, and Ras homolog enriched in brain (Rheb), which stimulates mTOR activity.1 By arresting growth, farnesyltransferase inhibitors have great potential as antitumor agents. Lonafarnib is a farnesyltransferase inhibitor that blocks the post-translational lipid modification of oncogenic Ras isoforms H-Ras, N-Ras, and K-Ras (IC50s = 1.9, 2.8, and 5.2 nM, respectively) as well as Rheb (IC50 = 10-100 nM).2,3 It inhibits H-Ras signaling in whole cells (IC50 = 10 nM) and blocks the transformed growth properties of fibroblasts (IC50 = 75 nM) and human tumor cell lines (IC50 = 400 nM) expressing activated K-Ras proteins. In the nude mouse, lonafarnib demonstrates potent dose-dependent oral activity in an array of human tumor xenograft models including tumors originating from colon, lung, pancreas, prostate, and urinary bladder.2 Combination treatments with various cytotoxic agents (cyclophosphamide, 5-fluorouracil, and vincristine) or MAPK or Akt pathway inhibitors can enhance the in vivo efficacy of lonafarib.2,4 |
| 别名 | Sarasar;SCH 66336; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Appels, N.M.G.M.,Beijnen, J.H., and Schellens, J.H.M. Development of farnesyl transferase inhibitors: A review. Oncologist 10, 565-578 (2005). 2.Liu, M.,Bryant, M.S.,Chen, J., et al. Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and Wap-ras transgenic mice. Cancer Research 58, 4947-4956 (1998). 3.Basso, A.D.,Mirza, A.,Liu, G., et al. The farnesyl transferase inhibitor (FTI) SCH66336 (lonafarnib) inhibits Rheb farnesylation and mTOR signaling. Role in FTI enhancement of taxane and tamoxifen anti-tumor activity. The Journal of Biological Chemisty 280(35), 31101-31108 (2005). 4.Niessner, H.,Beck, D.,Sinnberg, T., et al. The farnesyl transferase inhibitor lonafarnib inhibits mTOR signaling and enforces sorafenib-induced apoptosis in melanoma cells. Journal of Investigative Dermatology 131(2), 468-479 (2011). | |
| 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 | 638.8 |
| 分子式 | C27H31Br2ClN4O2 |
| CAS号 | 193275-84-2 |
| 稳定性 | ≥ 2 years |
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