Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tipifarnib (IND 58359) 能够抑制法尼基转移酶 (FTase),IC50=0.86 nM,具有潜在抗肿瘤特性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 342 | 现货 | ||
2 mg | ¥ 488 | 现货 | ||
5 mg | ¥ 875 | 现货 | ||
10 mg | ¥ 1,290 | 现货 | ||
25 mg | ¥ 2,350 | 现货 | ||
50 mg | ¥ 3,880 | 现货 | ||
100 mg | ¥ 5,530 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 980 | 现货 |
产品描述 | Tipifarnib (IND 58359) is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis. |
靶点活性 | FTase:0.6 nM |
体外活性 | 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. [2] 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. [3] Combining Tipifarnib with 10 nM 4-OH-tamoxifen in the presence of E2 reduces the IC50 8-fold from 400 to 50 nM. [4] 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 nM, respectively. [6] |
体内活性 | 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). [4] 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. [4] |
细胞实验 | MACS-selected CD34+ cells are seeded in Methocult 4435 'complete' 1% bovine serum albumin, 3 U/mL recombinant human (rh) erythropoietin, 0.1 mM 2-mercaptoethanol, 2 mM L-glutamine and the following cytokines: 50 ng/mL rh stem cell factor, 20 ng/mL rh GM-CSF, 20 ng/mL rh IL-3, 20 ng/mL rh IL-6 and 20 ng/mL h G-CSF. DMSO or Tipifarnib is added at the concentrations of 2.5, 10, 25 and 50 nM at day 1. All cultures are performed in duplicates and the numbers of colonies are scored after 14 days of incubation at 37 °C in a humidified incubator containing 5% CO2</sub(Only for Reference) |
别名 | 替吡法尼, R115777, Zarnestra, IND 58359 |
分子量 | 489.4 |
分子式 | C27H22Cl2N4O |
CAS No. | 192185-72-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 48.9 mg/mL (100 mM)
Ethanol: 9.8 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.0433 mL | 10.2166 mL | 20.4332 mL | 51.083 mL |
5 mM | 0.4087 mL | 2.0433 mL | 4.0866 mL | 10.2166 mL | |
10 mM | 0.2043 mL | 1.0217 mL | 2.0433 mL | 5.1083 mL | |
20 mM | 0.1022 mL | 0.5108 mL | 1.0217 mL | 2.5541 mL | |
DMSO | 50 mM | 0.0409 mL | 0.2043 mL | 0.4087 mL | 1.0217 mL |
100 mM | 0.0204 mL | 0.1022 mL | 0.2043 mL | 0.5108 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tipifarnib 192185-72-1 Metabolism Transferase Inhibitor Farnesyl Transferase inhibit 替吡法尼 R115777 Zarnestra R-115777 R 115777 IND-58359 Ftase IND 58359 IND58359 inhibitor