Tipifarnib

    
98%

Tipifarnib

源叶(MedMol)
S80501 一键复制产品信息
192185-72-1
C27H22Cl2N4O
489.4
R115777;(R)-6-(amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one
货号 规格 价格 上海 北京 武汉 南京 购买数量
S80501-2mg 98% ¥200.00 8 - - -
S80501-5mg 98% ¥360.00 3 - - -
S80501-10mg 98% ¥610.00 货期:2-3天 - - -
S80501-50mg 98% ¥1960.00 货期:2-3天 - - -
S80501-100mg 98% ¥3100.00 货期:2-3天 - - -
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

Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC50 of 0.86 nM. Antineoplastic activity

产品描述: Tipifarnib (IND 58359) binds to and inhibits farnesyltransferase (FTase) with an IC50 of 0.86 nM. Antineoplastic activity
靶点: IC50: 0.86 nM (FTase);Transferase
体内研究: Combined therapy with ICI 47699 and Tipifarnib (50 mg/kg, p.o.) produces greater tumor growth inhibition when compared with either drug alone. E2 deprivation and Tipifarnib in combination results in greater growth inhibition than either E2 deprivation or Tipifarnib alone. The combination of ICI 47699 and Tipifarnib results in significantly lower Ki-67 compared with either ICI 47699 or Tipifarnib alone. Tipifarnib alone also reduces the CTI compared with control. The combination of ICI 47699 and Tipifarnib or Tipifarnib coupled with E2 withdrawal is most effective at lowering the CTI (0.8 and 0.7, respectively), which may account for the decrease in tumor volume
参考文献: 1. Devendra S Puntambekar, et al. Inhibition of farnesyltransferase: a rational approach to treat cancer? J Enzyme Inhib Med Chem. 2007 Apr;22(2):127-40. 2. Martin LA, et al. The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with ICI 47699 acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo. Mol Cancer Ther. 2007 Sep;6(9):2 3. End DW, et al. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 2001 Jan 1;61(1):131-7 4. Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161.
溶解性: DMSO  :  100  mg/mL  (204.33  mM;  Need  ultrasonic)
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.043 ml 10.217 ml 20.433 ml
5 mM 0.409 ml 2.043 ml 4.087 ml
10 mM 0.204 ml 1.022 ml 2.043 ml
50 mM 0.041 ml 0.204 ml 0.409 ml
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参考文献

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