替吡法尼
| CAS号 | 192185-72-1 | 货号 | BCP02262 |
| 中文名 | 替吡法尼 | ||
| 英文名 | Tipifarnib | ||
| 中文别名 | |||
| 英文别名 | Zarnestra;IND 58359;R115777;IND-58359;IND58359;R-115777;R 115777; | ||
| 分子式 | C27H22Cl2N4O | 分子量 | 489.4 |
| 生物活性 | 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. [5] 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 | ||
| 信号通路 | Protease/Metabolic Enzyme | ||
| 靶 点 | FTase | ||
结构式
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