Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FX1 是一种强效特异性BCL6抑制剂,IC50大约为 35 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 253 | 现货 | ||
2 mg | ¥ 353 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 2,660 | 现货 | ||
100 mg | ¥ 3,820 | 现货 | ||
200 mg | ¥ 5,520 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 638 | 现货 |
产品描述 | FX1 is an effective and selective BCL6 inhibitor (IC50: 35 μM). |
靶点活性 | BCL6 BTB:35 μM |
体外活性 | FX1 markedly reduces recruitment of SMRT and BCOR to all 3 BCL6 target genes. There is little presence of SMRT at these loci in the BCL6-negative DLBCL cell line, which is not affected by FX1. After treatment with 50 μM FX1 for 6 hours, the superior potency of FX1 versus 79-6 in disrupting BCL6 binding to SMRT is evident when these small molecules are compared head to head in quantitative ChIP assays in DLBCL cells. |
体内活性 | Total B cell abundance is unaffected by FX1. FX1 significantly deplete GC B cells (GL7+FAS+B220+). Staining with B220 antibody reveals normal B cell follicular structures, whereas staining for the GC B cell-specific marker peanut agglutinin shows profound loss of GCs. The half-life is estimated to be approximately 12 hours. No signs of toxicity, inflammation, or infection are evident from H&E-stained sections of spleen, lung, gastrointestinal tract, kidney, heart, liver, and bone marrow of the fixed organs from mice treated with FX1 compare with the vehicle. |
细胞实验 | Cell viability is determined with the fluorescent redox dye. Fluorescence is determined for 3 replicates per treatment condition or vehicle with the microplate reader. The drug effect as 100-percentage viability is calculated. Through dose-effect curves the drug concentration that inhibits the growth of cell lines by 50% compared with vehicle (GI50) is determined. Experiments are performed in triplicate. For combination treatments, cells are exposed to a dose curve of each drug alone or their combination in a constant ratio, and cell viability is determined. To compare different schedules of treatments, the cells are treated in triplicate as follows: FX1 and doxorubicin simultaneously and cells treated for 48 hours; FX1 first and 24 hours after doxorubicin is added and treats for an extra 48 hours; doxorubicin first and 24 hours after FX1 is added and treats for an extra 48 hours. Then, the software is used to plot dose-effect curves and calculate the dose-reduction index [1]. |
动物实验 | Cell viability is determined with the fluorescent redox dye. Fluorescence is determined for 3 replicates per treatment condition or vehicle with the microplate reader. Cell viability of the drug-treated cells is normalized to their vehicle-treated controls, and the results are expressed as percentage viability. The drug effect as 100-percentage viability is calculated. Through dose-effect curves the drug concentration that inhibits the growth of cell lines by 50% compare with vehicle (GI50) is determined. Experiments are performed in triplicate. For combination treatments, cells are exposed to a dose curve of each drug alone or their combination in constant ratio, and cell viability is determined. To compare different schedules of treatments, the cells are treated in triplicate as follows: FX1 and doxorubicin simultaneously and cells treated for 48 hours; FX1 first and 24 hours after doxorubicin is added and treats for an extra 48 hours; doxorubicin first and 24 hours after FX1 is added and treats for an extra 48 hours. Then, the software is used to plot dose-effect curves and calculate the dose-reduction index[1]. |
分子量 | 368.82 |
分子式 | C14H9ClN2O4S2 |
CAS No. | 1426138-42-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (67.79 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7113 mL | 13.5567 mL | 27.1135 mL | 67.7837 mL |
5 mM | 0.5423 mL | 2.7113 mL | 5.4227 mL | 13.5567 mL | |
10 mM | 0.2711 mL | 1.3557 mL | 2.7113 mL | 6.7784 mL | |
20 mM | 0.1356 mL | 0.6778 mL | 1.3557 mL | 3.3892 mL | |
50 mM | 0.0542 mL | 0.2711 mL | 0.5423 mL | 1.3557 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。
FX1 1426138-42-2 Apoptosis BCL inhibit Bcl-2 Family FX-1 FX 1 Inhibitor inhibitor