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FX1

FX1

产品编号 T4089   CAS 1426138-42-2

FX1 是一种强效特异性BCL6抑制剂,IC50大约为 35 μM。

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FX1 Chemical Structure
FX1, CAS 1426138-42-2
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: FX1 (T4089)
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纯度: 99.68%
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 25 mg/mL (67.79 mM), Sonication is recommended.

溶液配制表

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

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TargetMol Library Books参考文献

1. Mariano G et al. Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma. J Clin Invest. 2016 Sep 1; 126(9): 3351–3362.

TargetMol Library Books文献引用

1. Cai Z, You S, Liu Z, et al.Selective deletion of E3 ubiquitin ligase FBW7 in VE-cadherin-positive cells instigates diffuse large B-cell lymphoma in mice in vivo.Cell Death & Disease.2024, 15(3): 212.
AZD-8055 Isatuximab alpha-Mangostin PI3Kδ-IN-16 3,4-Dicaffeoylquinic acid FMAU Lupiwighteone Concanavalin A

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 抑制剂库 铜死亡化合物库 表型筛选靶点鉴定库 经典已知活性库 抗癌化合物库 线粒体靶向库 转录因子库 细胞凋亡化合物库 PPI抑制剂库

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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。

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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。

Keywords

FX1 1426138-42-2 Apoptosis BCL inhibit Bcl-2 Family FX-1 FX 1 Inhibitor inhibitor

 

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