1. Apoptosis
  2. Bcl-2 Family Apoptosis
  3. FX1

FX1 是一种强效且特异性的 BCL6 抑制剂, IC50 大约为 35 μM。

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FX1 Chemical Structure

FX1 Chemical Structure

CAS No. : 1426138-42-2

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查看 Bcl-2 Family 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

FX1 is a potent and specific BCL6 inhibitor, with an IC50 of around 35 μM.

IC50 & Target

IC50: ~35 μM (BCL6)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DOHH-2 IC50
35.1 μM
Compound: 2; FX1
Antiproliferative activity against human DOHH2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human DOHH2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31895575]
Farage IC50
33.9 μM
Compound: 2; FX1
Antiproliferative activity against human Farage cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human Farage cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31895575]
L02 IC50
> 100 μM
Compound: 2; FX1
Cytotoxicity against human LO2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human LO2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31895575]
NCM460 IC50
> 100 μM
Compound: 2; FX1
Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31895575]
OCI-Ly7 IC50
39 μM
Compound: 2; FX1
Antiproliferative activity against human OCI-LY7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human OCI-LY7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31895575]
PNT1A IC50
> 100 μM
Compound: 2; FX1
Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31895575]
SUD4 IC50
51.3 μM
Compound: 2; FX1
Antiproliferative activity against human SUDHL4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human SUDHL4 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31895575]
Toledo IC50
65.3 μM
Compound: 2; FX1
Antiproliferative activity against BCL6-negative human Toledo cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against BCL6-negative human Toledo cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31895575]
体外研究
(In Vitro)

DLBCL 细胞暴露于 50 μM FX1 30 分钟。FX1 极大地减少了 BCOR 和 SMRT 对所有 3 个 BCL6 靶基因的募集,而阴性对照无响应。在不受 FX1 影响的 BCL6 阴性 DLBCL 细胞系中,这些位点几乎不存在 SMRT。在用 50 μM FX1 处理 6 小时后,在 DLBCL 细胞的定量 ChIP 测定中对这些小分子进行头对头比较时,FX1 与 79-6 在破坏 BCL6 与 SMRT 结合方面的优势是显而易见的。DLBCL 细胞暴露于 FX1,并在 4 个连续时间点收集 mRNA。与阴性对照相比,FX1 在 2 个独立的 DLBCL 细胞系中几乎总是诱导这些基因的显著去阻遏[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

FX1 处理小鼠的脾脏在宏观上与载体对照无法区分。通过流式细胞术测量的总 B 细胞丰度不受 FX1 的影响。GC B 细胞 (GL7+FAS+B220+) 因暴露于 FX1 而显著耗尽。IHC 检查脾脏结构。用 B220 抗体染色显示正常的 B 细胞滤泡结构,而 GC B 细胞特异性标记物花生凝集素染色显示 GC 严重丢失。半衰期估计约为 12 小时。最后,评估 FX1 是否可以在小鼠中引起毒性作用。与媒介物相比,用 FX1 处理的小鼠固定器官的肺、胃肠道、心脏、肾脏、肝脏、脾脏和骨髓的 H&E 染色切片没有明显的毒性、炎症或感染迹象[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

368.82

Formula

C14H9ClN2O4S2

CAS 号
性状

固体

颜色

Pink to red

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 10 mg/mL (27.11 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7113 mL 13.5567 mL 27.1135 mL
5 mM 0.5423 mL 2.7113 mL 5.4227 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.71 mM); 澄清溶液

    此方案可获得 ≥ 1 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: 50% PEG300    50% Saline

    Solubility: 50 mg/mL (135.57 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Six-to 8-week-old male mice are injected s.c. with 107 low-passage human SUDHL-6, OCI-Ly7, or Toledo cells. Alternatively, 6-to 8-week-old mice are injected with low-passage HBL-1 cells. When tumors reach a palpable size (approximately 100 mm3), mice are assigned in a randomized way to treatment groups and treated i.p. with 25 or 50 mg/kg/d of the drugs (including FX1). Drugs are reconstituted in PEG-400 and stored at -20°C until use. Tumor size is measured 3 times a week with an electronic digital caliper in 2 dimensions, and then tumor volume is calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 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
15 mM 0.1808 mL 0.9038 mL 1.8076 mL 4.5189 mL
20 mM 0.1356 mL 0.6778 mL 1.3557 mL 3.3892 mL
25 mM 0.1085 mL 0.5423 mL 1.0845 mL 2.7113 mL
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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