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Tipifarnib 替吡法尼

目录号 M1885 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Tipifarnib 是一种有效的,特异性farnesyltransferase (FTase)抑制剂,作用于H-ras或N-ras突变细胞,具有最显著的抗增殖作用效果。

Tipifarnib结构式

别名:R115777

包装 价格 库存状态
10mM*1mL 原价 ¥ 1300
促销价 ¥ 1235
中国库存现货
5mg 原价 ¥ 1200
促销价 ¥ 1140
中国库存现货
10mg 原价 ¥ 2000
促销价 ¥ 1900
中国库存现货
50mg 原价 ¥ 6300
促销价 ¥ 5985
中国库存现货
100mg 原价 ¥ 9800
促销价 ¥ 9310
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
生物活性

Tipifarnib(R115777)是一种有效的,特异性farnesyltransferase(FTase)抑制剂,作用于H-ras或N-ras突变细胞,具有最显著的抗增殖作用效果。与DMSO处理的LGL T细胞相比,用5 μM Tipifarnib处理72小时,凋亡细胞百分率明显高很多。使用健康捐赠者提供的T细胞,Tipifarnib按剂量依赖性降低IFNγ阳性细胞百分率。在沉淀物中,与DMSO相比,Tipifarnib降低激活型Ras的数量。

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 MCF-7 cells line
方法 Cell Growth Assays.
Steroid-depleted cells were seeded into 12-well plates at a density of ∼1 × 104 cells per well or into 96-well plates at a density of 4,000 cells per well, in dextran-coated charcoal medium. After 24 h, monolayers were treated with E2 plus inhibitors either alone or in combination. The 12-well plates were treated for 6 days with daily changes. Cell number was then determined using a Z1 Coulter counter (Beckman Coulter). The 96-well plates were treated with a single dose and left for 96 h at which time cell viability was measured using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay as described previously (15). The interaction between R115777 and 4-OH-tamoxifen was analyzed by the median effect plot method described by Chou and Talalay (16). Calculation of the combination index took into account a nonfixed drug ratio and was based on the assumption that the action of the two drugs was mutually nonexclusive for the strict detection of synergism. A combination index < 1 indicates synergism, combination index = 1 indicates additivity, and a combination index > 1 indicates antagonism. Experiments were repeated thrice.
浓度 0~1000 nM
处理时间 96 h
动物实验
动物模型 MCF-7 xenografts in Female ovariectomized Ncr foxhead nude mice
配制 20% w/v β-cyclodextrin (pH 2.5)
剂量 50 mg/kg twice daily for 5 consecutive days followed by a 2-day rest period, for a total of 19 days
给药处理 oral gavage
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 489.39
分子式 C27H22Cl2N4O
CAS号 192185-72-1
纯度 100.0%
溶解性(25°C) DMSO 14 mg/mL
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.0434 mL 10.2168 mL 20.4336 mL
5 mM 0.4087 mL 2.0434 mL 4.0867 mL
10 mM 0.2043 mL 1.0217 mL 2.0434 mL
使用AbMole产品发表的文献
参考文献

A randomized phase 3 study of tipifarnib compared with best supportive care, including hydroxyurea, in the treatment of newly diagnosed acute myeloid leukemia in patients 70 years or older.
Harousseau JL, et al. Blood. 2009 Aug 6;114(6):1166-73. PMID: 19470696.

Phase II trial of tipifarnib as maintenance therapy in first complete remission in adults with acute myelogenous leukemia and poor-risk features.
Karp JE, et al. Clin Cancer Res. 2008 May 15;14(10):3077-82. PMID: 18483374.

The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with tamoxifen acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo.
Martin LA, et al. Mol Cancer Ther. 2007 Sep;6(9):2458-67. PMID: 17876043.

Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma.
Alsina M, et al. Blood. 2004 May 1;103(9):3271-7. PMID: 14726402.

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关键词:Tipifarnib, R115777, Tipifarnib供应商, Transferase抑制剂, 购买Tipifarnib, Tipifarnib结构式

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