CAS NO: | 193275-84-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | Lonafarnib (Sch66336) is a potent and orally activefarnesyl transferase(FTase)inhibitor. Lonafarnib inhibits the activities ofH-ras,K-rasandN-raswithIC50values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities. | ||||||||||||||||
IC50& Target | IC50: 1.9 nM (H-ras), 5.2 nM (K-ras), 2.8 nM (N-ras)[1] | ||||||||||||||||
体外研究 (In Vitro) | Lonafarnib (Sch66336) potently inhibits Ha-Ras processing in whole cells and blocks the trans formed growth properties of fibroblasts and human tumor cell lines expressing activated Ki-Ras proteins[1]. All treatment groups containing Lonafarnib (10 μM) show a significantly higher level of unfarnesylated H-Ras (116-137%) compared to control treatment[2]. | ||||||||||||||||
体内研究 (In Vivo) | In mouse, rat, and monkey systems, Lonafarnib (Sch66336) has excellent oral bioavailability and pharmacokinetic properties. In the nude mouse, Lonafarnib demonstrates potent oral activity in a wide array of human tumor xenograft models including tumors of colon, lung, pancreas, prostate, and urinary bladder origin[1]. Lonafarnib alone (80 mg/kg by oral gavage, once daily) has limited ability to inhibit orthotopic U87 tumors compared to vehicle treated control animals (T/C of 0.67). The combination of XRT/Tem (2.5Gy/day for 2 days; 5 mg/kg by oral gavage 90 min prior to XRT) is designed to produce modest tumor growth inhibition in vivo(T/C of 0.42). Concurrent Lonafarnib/XRT/Tem (Lonafarnib 80 mg/kg by oral gavage, once daily, XRT 2.5Gy/day for 2 days, and Tem 5 mg/kg by oral gavage 90 min prior to XRT) provides the strongest growth reduction (T/C of 0.02) and is significantly more effective than XRT/Tem (p<0.04), with the majority of animals demonstrating a decrease in tumor volume (p<0.05) after two weeks and persisting after 4 weeks (p<0.05)[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 638.82 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H31Br2ClN4O2 | ||||||||||||||||
CAS 号 | 193275-84-2 | ||||||||||||||||
中文名称 | 洛那法尼 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(78.27 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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