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Lonafarnib

CAS No. : 193275-84-2

MCE 國際站：Lonafarnib

產品活性：Lonafarnib (Sch66336) 是一種有效的，具有口服活性的法尼基蛋白轉移酶 (FPTase) 抑制劑，作用于 H-ras，K-ras 和 N-ras，IC₅₀ 分別為 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。

研究領域：Metabolic Enzyme/Protease  |  GPCR/G Protein  |  Autophagy

作用靶點：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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