Lonafarnib

    
99%

Lonafarnib

源叶(MedMol)
S80506 一键复制产品信息
193275-84-2
C27H31Br2ClN4O2
638.82
SCH66336;1-Piperidinecarboxamide, 4-[2-[4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-
货号 规格 价格 上海 北京 武汉 南京 购买数量
S80506-5mg 99% ¥490.00 5 - - -
S80506-10mg 99% ¥740.00 10 - - -
S80506-50mg 99% ¥2000.00 2 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities.

产品描述: Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities.
靶点: IC50: 1.9 nM (H-ras), 5.2 nM (K-ras), 2.8 nM (N-ras);Raf;Transferase;Autophagy;Ras
体内研究: 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)
参考文献: 1. Liu M, 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 Res. 1998 Nov 1;58(21):4947-56. 2. Chaponis D, et al. Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas. J Neurooncol. 2011 Aug;104(1):179-89. 3. Koh C,et al. Oral prenylation inhibition with lonafarnib in chronic hepatitis D infection: a proof-of-concept randomised, double-blind, placebo-controlled phase 2A trial. Lancet Infect Dis. 2015 Oct;15(10):1167-1174.
溶解性: DMSO  :  50  mg/mL  (78.27  mM;  Need  ultrasonic)
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.565 ml 7.827 ml 15.654 ml
5 mM 0.313 ml 1.565 ml 3.131 ml
10 mM 0.157 ml 0.783 ml 1.565 ml
50 mM 0.031 ml 0.157 ml 0.313 ml
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参考文献

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