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。
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 |
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 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 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，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
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 |
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