Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LB42708 是一种口服有活力的特异性法尼基转移酶抑制剂。它对H-Ras、N-Ras 和K-Ras4B 的法尼基化均有抑制作用,其IC50分别为 0.8 nM、1.2 nM 和 2.0 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 262 | 现货 | ||
2 mg | ¥ 368 | 现货 | ||
5 mg | ¥ 697 | 现货 | ||
10 mg | ¥ 1,130 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 3,260 | 现货 | ||
100 mg | ¥ 4,660 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 915 | 现货 |
产品描述 | LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras). |
靶点活性 | FTase (H-ras):0.8 nM, FTase (K-Ras):2.0 nM, FTase (N-ras):1.2 nM |
体外活性 | 在脂多糖的小鼠中, LB42708(12.5 mg/kg,i.p.)抑制NO、前列腺素E2、TNF-α及IL-1β的产生,并抑制CIA的进程.在Ras野生型和突变型的肿瘤中,LB42708(20 mg/kg/day,i.p.)对肿瘤生长及血管新生有抑制作用. |
体内活性 | 在H-ras和K-ras-改变的大鼠肠内壁细胞中,LB42708对生长和诱导凋亡有不可逆的抑制作用。在肿瘤相关的内皮细胞中,通过阻断Ras依赖的MAPK 和PI3K/Akt信号通路,LB42708对VEGF诱导的肿瘤血管新生产生抑制作用。在鼠巨噬细胞系RAW264.7细胞中,LB42708对脂多糖 + IFN-γ诱导的细胞内法尼化蛋白p21ras过程有明显抑制作用。在免疫激活的成骨细胞和巨噬细胞中,LB42708抑制一氧化氮合酶、环氧合酶-2、TNF-α及IL-1β、NO和PGE(2)的产生。通过抑制IKK活性,LB42708对NF-κB激活和iNOS启动子活性产生抑制作用。 |
激酶实验 | Biochemical Assessment of PDGFRα Kinase Activity: Chinese hamster ovary (CHO) cells are transiently transfected with mutated or wild type PDGFRα constructs and treated with various concentrations of Crenolanib. Experiments involving recombinant DNA are performed using biosafety level 2 conditions in accordance with guidelines. Protein lysates from cell lines are prepared and subjected to immunoprecipitation using anti-PDGFRα antibodies followed by sequential immunoblotting for PDGFRα. Densitometry is performed to quantify drug effect using Photoshop software, with the level of phosphor- PDGFRα normalized to total protein. Densitometry and proliferation experimental results are analyzed using Calcusyn 2.1 software to mathematically determine the IC50 values. The Wilcoxon Rank Sum Test is used to compare the IC50 values of Crenolanib for a given mutation. |
细胞实验 | Cell growth is measured by MTT. Briefly, cells were seeded at 2 × 103 cells per well in 96-well culture plates in triplicate. After the addition of various concentrations of drugs, cells are incubated for 72 h. At the end of culture, the plates are washed twice with PBS, and cells are incubated with 200 μl of RPMI 1640 containing 10% FCS and 0.25 mg/ml of MTT at 37 °C for 3 h. The absorbance of each well is measured with Titer-Tech 96-well multiscanner at 570 nm. The viable cell number is proportional to the absorbance. (Only for Reference) |
分子量 | 555.47 |
分子式 | C30H27BrN4O2 |
CAS No. | 226929-39-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 55.6 mg/mL (100 mM)
DMSO: 55.6 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.8003 mL | 9.0014 mL | 18.0028 mL | 45.0069 mL |
5 mM | 0.3601 mL | 1.8003 mL | 3.6006 mL | 9.0014 mL | |
10 mM | 0.18 mL | 0.9001 mL | 1.8003 mL | 4.5007 mL | |
20 mM | 0.09 mL | 0.4501 mL | 0.9001 mL | 2.2503 mL | |
50 mM | 0.036 mL | 0.18 mL | 0.3601 mL | 0.9001 mL | |
100 mM | 0.018 mL | 0.09 mL | 0.18 mL | 0.4501 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。
LB42708 226929-39-1 Metabolism Transferase Ftase Apoptosis Inhibitor H-Ras orally active K-Ras4B N-Ras Farnesyl Transferase inhibit LB-42708 farnesyltransferase inhibitor LB 42708 inhibitor