货号	规格	价格	上海	北京	珠海	重庆	武汉
S80501-2mg买3赠1	99.20%	￥200.00 S80501-2mg ￥200.00 现货（买3赠1）	7 7	-	-	-	-
S80501-5mg买3赠1	99.20%	￥340.00 S80501-5mg ￥340.00 现货（买3赠1）	2 0 2	-	-	-	-
S80501-10mg买3赠1	99.20%	￥600.00 S80501-10mg ￥600.00 现货（买3赠1）	4 4	-	-	-	-
S80501-50mg买3赠1	99.20%	￥1960.00 S80501-50mg ￥1960.00 现货（买3赠1）	3 3	-	-	-	-
S80501-100mg买3赠1	≥98%	￥3100.00 S80501-100mg ￥3100.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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