Tipifarnib

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抑制剂描述：

产品名称：Tipifarnib

产品别名：见爱必信官网

英文别名：Tipifarnib

靶点：Transferase

CAS：192185-72-1

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

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。

溶解性：Ethanol ：9.8 mg/mL (20 mM)
DMSO ：48.9 mg/mL (100 mM)

体外研究：

Using Tipifarnib 5 μM for 72 hours, the percentage of apoptotic cells is significantly higher in drug-treated compared to DMSO-treated LGL T-cells. Using T-cells from healthy donors, Tipifarnib reduces the percentage of IFNγ-positive cells in a time-dependent manner. Tipifarnib reduces the amount of activated Ras in precipitates compared to DMSO. Tipifarnib exerts selective in vitro toxicity against clonal MDS hematopoiesis at concentrations less than 10 nM the effect being more prominent in white cell progenitors. This action is not due to apoptosis induction as both normal and MDS progenitors displays equivalent DiOC3 and annexin V expression up to 72 hours after exposure to Tipifarnib. Combining Tipifarnib with 10 nM 4-OH-tamoxifen in the presence of E2 reduces the IC50 8-fold from 400 to 50 nM. Tipifarnib induces apoptosis in U937 cells. In addition, Tipifarnib inhibits isolated human farnesyltransferase for a lamin B peptide and for the K-RasB peptide with IC50 of 0.86 nM and 7.9 nM, respectively.

体内研究：Ki-67 is lower in the tumors treated with E2 withdrawal plus R115777 compared with E2 withdrawal alone. The combination of tamoxifen and R115777 results in significantly lower Ki-67 compared with either tamoxifen or R115777 alone (mean of 5% versus 16.9% and 67.3%, respectively). In contrast, no significant difference in apoptotic scores is seen between the treatment groups. R115777 alone also reduces the CTI compared with control. The combination of tamoxifen and R115777 or R115777 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.

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