规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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体外研究 (In Vitro) |
Tipifarnib 的 ED50 为 4 nM,是 Cruzi 锥虫的强抑制剂。对于核纤层蛋白 B 肽和 K-RasB 肽,替比法尼的 IC50 分别为 0.86 nM 和 7.9 nM,替比法尼抑制这两种生物分子的分离的人法尼基转移酶 [2]。对于侵袭性前列腺癌 (PCa),替比法尼可减少血管生成和细胞增殖,同时诱导细胞凋亡 [3]。替比法尼(0.25 μM、1 μM;48 小时)显着减少 C4-2B 和 PC-3 细胞中外泌体的数量 [3]。 Tipifarnib (1 μM) 可显着抑制 C4-2B 细胞中的 Alix、nSMase2 和 Rab27a 蛋白数量 [3]。当应用于 C4-2B 和 PC-3 细胞时,替比法尼 (0.25 μM) 强烈抑制 p-ERK(Ras/Raf/ERK 信号通路的下游效应分子)的激活,但不会减少总 ERK [3]。暴露于替比法尼 (1.25-5 μM) 30 分钟会导致 U937 细胞内质网应激,进而导致细胞内钙稳态失衡 [4]。
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体内研究 (In Vivo) |
在小鼠中,替比法尼(10 mg/kg;腹腔注射;单剂量)通过上调肝脏抗凋亡蛋白 Bcl-xL 抑制 GalN/LPS 引起的死亡率 [5]。
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动物实验 |
Animal/Disease Models: GalN/LPS challenge mouse[5]
Doses: 10 mg/kg; while chanllenge with GalN (400 mg/kg; IP) and LPS (32 g/kg) Route of Administration: IP; 60 min before challenge Experimental Results: Protected primary hepatocytes from GalN/tumor necrosis factor-induced cell death. Inhibited caspase 3 activation and upregulating antiapoptotic proteins. |
参考文献 |
[1]. Devendra S Puntambekar, et al. Inhibition of farnesyltransferase: a rational approach to treat cancer? J Enzyme Inhib Med Chem. 2007 Apr;22(2):127-40.
[2]. End DW, et al. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 2001 Jan 1;61(1):131-7 [3]. Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. |
分子式 |
C27H22CL2N4O
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分子量 |
489.4
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CAS号 |
192185-72-1
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相关CAS号 |
Tipifarnib (S enantiomer);192185-71-0
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SMILES |
O=C1N(C2=C(C(C3=CC=CC(Cl)=C3)=C1)C=C(C=C2)[C@@](N)(C4=CN=CN4C)C5=CC=C(C=C5)Cl)C
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别名 |
R115777; R 115777; R-115777; LX81; NSC702818; D03720; trade name Zarnestra
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (2.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.43 mg/mL (2.92 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.43 mg/mL (2.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 15% Captisol+citrate vehicle: 5 mg/mL Solubility in Formulation 5: 10 mg/mL (20.43 mM) in 20% HP-β-CD/10 mM citrate pH 2.0 (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0433 mL | 10.2166 mL | 20.4332 mL | |
5 mM | 0.4087 mL | 2.0433 mL | 4.0866 mL | |
10 mM | 0.2043 mL | 1.0217 mL | 2.0433 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。