2. Epigenetics
  3. Epigenetic Reader Domain
  4. FL-411

FL-411  (Synonyms: BRD4-IN-1)

目录号: HY-111102 纯度: 99.05%
COA 产品使用指南

摩尔计算器

FL-411 是一种有效的选择性 BRD4 抑制剂，抑制 BRD4(1)，IC50 为 0.43±0.09 μM。

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FL-411 Chemical Structure

FL-411 Chemical Structure

CAS No. : 2118944-88-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1210
In-stock
1 mg ￥450
In-stock
5 mg ￥1100
In-stock
10 mg ￥1800
In-stock
25 mg ￥3600
In-stock
50 mg ￥6000
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

FL-411 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

FL-411 is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1).

IC50 & Target

BRD4(1)

0.43 μM (IC50)

体外研究
(In Vitro)

FL-411 is a selective BRD4 inhibitor. Binding affinities of FL-411 are measured by TR-FRET against the first and second bromodomains of BRD2(1), BRD4(1), and BRD4(2) with IC50s of 24.60±0.70 μM, 0.47±0.02 μM, 0.93±0.05 μM, respectively. FL-411 possesses a good BRD4(1) inhibition activity (IC50=0.43±0.09 μM), antiproliferative activity (MCF-7, IC50=1.62±0.06 μM; MDA-MB-231, IC50=3.27±0.14 μM), and autophagic activity (42.29% in MCF-7 cells), as well as displays a low toxicity against MCF10A cells). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction and thus activating AMPK-mTOR-ULK1-modulated autophagic pathway in breast cancer cells[1].

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

FL-411 相关抗体:
体内研究
(In Vivo)

To evaluate the antitumor activity of FL-411 in vivo, two breast tumor xenograft models, namely, MCF-7 and MDA-MB-231 cell lines models, are used. The in vivo study is conducted using three different doses of FL-411: 25 mg/kg, 50 mg/kg, and 100 mg/kg. In all the models, FL-411 shows significant tumor growth inhibition in a dose-dependent manner as determined by 80% and 76% tumor growth inhibition ratio in MCF-7 and MDA-MB-231 cell models, respectively. A remarkable loss of tumor weights is observed in all dose groups (p<0.001). FL-411 displays no obvious effects on the body weight of all the treatment groups. To examine whether FL-411-mediated inhibition of tumor growth in vivo is associated with reduced cell proliferation and the increased autophagy-associated cell death, tumor tissues from control and FL-411-treated mice are processed for the immunohistochemical analysis of Ki-67 and LC3. FL-411 treatment obviously reduces the number of Ki-67 (p<0.001) positive cells as well as increases autophagy levels, which is determined by increased LC3 expression (p<0.001)[1].

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

341.43

Formula

C18H19N3O2S
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 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 : 5.4 mg/mL (15.82 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 2.9289 mL 14.6443 mL 29.2886 mL
5 mM 0.5858 mL 2.9289 mL 5.8577 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: 1.25 mg/mL (3.66 mM); 悬浊液; 超声助溶

    此方案可获得 1.25 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 12.5 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。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.25 mg/mL (3.66 mM); 悬浊液; 超声助溶

    此方案可获得 1.25 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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

只
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

纯度: 99.05%

COA (192 KB) HNMR (136 KB) RP-HPLC (169 KB) LCMS (104 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

The MCF-7 and MDA-MB-231 cells are dispensed in 96-well flat bottom microtiter plates at a density of 5×104 cells/mL. After 24 h incubation, MCF-7 or MDA-MB-231 cells are treated with 1.5 and 3 μM FL-411, respectively. 3-MA (1 mM) is added 1 h before treated with FL-411. After treatment, cell viability is measured by the MTT assay. 5 mg/mL MTT is added to each well. After 4 h incubation, the medium is removed and 150 μL of DMSO is added to each well to dissolve the crystal formazan dye. Absorbance is measured at 570 nm on an enzyme-linked immunosorbent assay reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
52 female nude mice (BALB/c, 6-8 weeks, 20-22 g) are injected subcutaneously with MCF-7 cells or MDA-MB-231 cells (5×106 cells/mouse), respectively. When the tumors reach 100 mm3 in volume, the mice are divided into four groups for each cell line. Three groups are treated with different doses of FL-411 (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg) once a day by intragastric administration for 24 or 27 days, whereas the control group is treated with vehicle control. During the treatment, the tumor volumes and body weight are measured every 3 days until the end of the study. At the end of treatment, all mice are sacrificed. The tumor tissues are harvested, weighed, and photographed. Then, the tumor tissues are frozen in liquid nitrogen or fixed in formalin immediately[1].

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

FL-411 相关分类

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 2.9289 mL 14.6443 mL 29.2886 mL 73.2215 mL
5 mM 0.5858 mL 2.9289 mL 5.8577 mL 14.6443 mL
10 mM 0.2929 mL 1.4644 mL 2.9289 mL 7.3221 mL
15 mM 0.1953 mL 0.9763 mL 1.9526 mL 4.8814 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

FL-4112118944-88-8BRD4-IN-1FL411FL 411Epigenetic Reader DomainInhibitorinhibitorinhibit

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