Lonafarnib | 洛那法尼 | MedChemExpress (MCE)
品牌 | 厂商性质 | 产地 | 货期 | 价格 |
---|---|---|---|---|
MedChemExpress (MCE) | 生产商 | 美国 | 现货 | 1546 |
性能特点
Lonafarnib (Sch66336) 是一种有效的,具有口服活性的法尼基蛋白转移酶 (FPTase) 抑制剂,作用于 H-ras,K-ras 和 N-ras,IC50 分别为 1.9 n
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
10 mM * 1 mL | 193275-84-2 | ¥1,546.00 | 询底价 |
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Lonafarnib
CAS No. : 193275-84-2
MCE 国际站:Lonafarnib
产品活性:Lonafarnib (Sch66336) 是一种有效的,具有口服活性的法尼基蛋白转移酶 (FPTase) 抑制剂,作用于 H-ras,K-ras 和 N-ras,IC50 分别为 1.9 nM,5.2 nM 和 2.8 nM。Lonafarnib 具有抗肝炎三角洲病毒 (HDV) 的活性。
研究领域:Metabolic Enzyme/Protease | GPCR/G Protein | MAPK/ERK Pathway | Autophagy
作用靶点:Farnesyl Transferase | Ras | Autophagy
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. All treatment groups containing Lonafarnib (10 μM) show a significantly higher level of unfarnesylated H-Ras (116-137%) compared to control treatment.
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. 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).
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